Gazyva

Manufacturer
Genentech, Inc. | Roche Diagnostics GmbH | F. Hoffmann-La Roche AG | Roche Diagnostics | Genentech, Inc. (Oceanside)
Effective date
2026-10-01
Label type
HUMAN PRESCRIPTION DRUG LABEL
Version
23
Source
daily-update
Hydrated at
2026-10-07 01:04:44

Label at a glance#

ProductGazyva
Active ingredientOBINUTUZUMAB
Label structure17 sections

Boxed warning

Hepatitis B Virus (HBV) reactivation, in some cases resulting in fulminant hepatitis, hepatic failure, and death, can occur in patients receiving CD20-directed cytolytic antibodies, including GAZYVA. Screen all patients for HBV infection before treatment initiation. Monitor HBV-positive patients during and after treatment with GAZYVA. Discontinue GAZYVA and concomitant medications in the event of HBV reactivation ...

Indications and uses

GAZYVA, in combination with chlorambucil, is indicated for the treatment of patients with previously untreated chronic lymphocytic leukemia. GAZYVA, in combination with bendamustine followed by GAZYVA monotherapy, is indicated for the treatment of patients with follicular lymphoma who relapsed after, or are refractory to, a rituximab-containing regimen . GAZYVA, in combination with chemotherapy followed by GAZYVA ...

Dosage and administration

Premedicate before each infusion [see Dosage and Administration (2.6) ] . Provide prophylactic hydration and anti-hyperuricemics to patients at high risk of tumor lysis syndrome [see Dosage and Administration (2.6) and Warnings and Precautions (5.5) ]. Administer only as an intravenous infusion through a dedicated line [see Dosage and Administration (2.8) ] . Do not administer as an intravenous push or bolus. Moni...

Storage and handling

GAZYVA (obinutuzumab) injection is a clear, colorless to slightly brown, preservative-free solution for intravenous use supplied as 1,000 mg/40 mL (25 mg/mL) in single-dose vials (NDC 50242-070-01). Store at 2°C to 8°C (36°F to 46°F). Do not use beyond expiration date stamped on carton. Protect from light. DO NOT FREEZE. DO NOT SHAKE.

Label contents#

Full prescribing information#

WARNING: HEPATITIS B VIRUS REACTIVATION and PROGRESSIVE MULTIFOCAL LEUKOENCEPHALOPATHY

BOXED WARNING SECTION

  • Hepatitis B Virus (HBV) reactivation, in some cases resulting in fulminant hepatitis, hepatic failure, and death, can occur in patients receiving CD20-directed cytolytic antibodies, including GAZYVA. Screen all patients for HBV infection before treatment initiation. Monitor HBV-positive patients during and after treatment with GAZYVA. Discontinue GAZYVA and concomitant medications in the event of HBV reactivation [see Warnings and Precautions (5.1)].
  • Progressive Multifocal Leukoencephalopathy (PML) including fatal PML, can occur in patients receiving GAZYVA [see Warnings and Precautions (5.2)].

1 INDICATIONS AND USAGE

INDICATIONS & USAGE SECTION

1.1 Chronic Lymphocytic Leukemia (CLL)

SPL UNCLASSIFIED SECTION

GAZYVA, in combination with chlorambucil, is indicated for the treatment of patients with previously untreated chronic lymphocytic leukemia.

1.2 Follicular Lymphoma (FL)

SPL UNCLASSIFIED SECTION

GAZYVA, in combination with bendamustine followed by GAZYVA monotherapy, is indicated for the treatment of patients with follicular lymphoma who relapsed after, or are refractory to, a rituximab-containing regimen.

GAZYVA, in combination with chemotherapy followed by GAZYVA monotherapy in patients achieving at least a partial remission, is indicated for the treatment of adult patients with previously untreated stage II bulky, III or IV follicular lymphoma.

1.3 Lupus Nephritis (LN)

SPL UNCLASSIFIED SECTION

GAZYVA is indicated for the treatment of adult patients with active lupus nephritis who are receiving standard therapy.

1.4 Childhood-Onset Idiopathic Nephrotic Syndrome (INS)

SPL UNCLASSIFIED SECTION

GAZYVA is indicated to reduce the risk of relapse in adult and pediatric patients 2 years of age and older with frequently relapsing or steroid dependent childhood-onset idiopathic nephrotic syndrome who are in complete remission.

2 DOSAGE AND ADMINISTRATION

DOSAGE & ADMINISTRATION SECTION

2.1 Important Dosing Information

SPL UNCLASSIFIED SECTION

2.7 Dosage Modifications for Adverse Reactions

SPL UNCLASSIFIED SECTION

SPL UNCLASSIFIED SECTION

Infusion-Related Reactions

If a patient experiences an IRR, adjust the infusion as follows [see Warnings and Precautions (5.3)]:

  • Grade 4 (life-threatening): Stop infusion immediately and permanently discontinue GAZYVA.
  • Grade 3 (severe): Interrupt infusion and manage symptoms.
    • For patients who experience Grade 3 IRRs during standard infusion, upon resolution of symptoms, consider restarting GAZYVA infusion at no more than half the previous rate (the rate being used at the time that the IRR occurred) for 30 minutes, and if patients do not experience any further IRR symptoms, the infusion rate escalation may resume at the increments and intervals as appropriate for the treatment cycle dose. Permanently discontinue treatment if patients experience a Grade 3 or higher IRR at rechallenge.
    • For patients with FL who experience Grade 3 IRRs during the approximately 90-minute infusion, upon resolution of symptoms, the infusion can be restarted at no more than half the previous rate (the rate being used at the time that the IRR occurred) and not greater than 400 mg/hr. Administer subsequent infusions at the standard rate. Permanently discontinue treatment if patients experience a Grade 3 or higher IRR at rechallenge.
    • For patients with CLL only, the Day 1 infusion rate may be increased back up to 25 mg/hr after 1 hour but not increased further.
  • Grade 1–2 (mild to moderate): Reduce infusion rate or interrupt infusion and manage symptoms. Upon resolution of symptoms, continue or resume GAZYVA infusion, and if patient does not experience any further IRR symptoms, infusion rate escalation may resume at the increments and intervals as appropriate for the treatment cycle dose.
    • For patients with CLL only, the Day 1 infusion rate may be increased back up to 25 mg/hr after 1 hour but not increased further.
    • For patients with LN or childhood-onset INS, reduce infusion rate to half the rate that was used at the time of the reaction and treat symptoms. Upon resolution of symptoms, the infusion should be kept at the reduced rate for an additional 30 minutes. If no further symptoms of IRR, infusion rate escalation may resume at the increments and intervals as appropriate for the treatment dose.
SPL UNCLASSIFIED SECTION

Other Adverse Reactions

Consider treatment interruption if patients experience an infection, Grade 3 or 4 cytopenia, or Grade 2 or higher non-hematologic toxicity.

2.8 Preparation and Administration

SPL UNCLASSIFIED SECTION

SPL UNCLASSIFIED SECTION

Preparation

Prepare the solution for infusion, using aseptic technique, as follows:

  • Inspect visually for any particulate matter and discoloration prior to administration.
  • Use a sterile needle and syringe to prepare GAZYVA.
  • Dilute into a 0.9% Sodium Chloride Injection, USP PVC or non-PVC polyolefin infusion bag.
    Chronic Lymphocytic Leukemia
    • Preparation of solution for infusion on day 1 (100 mg) and day 2 (900 mg) of Cycle 1:
      • Prepare day 1 (100 mg) and day 2 (900 mg) infusion bags at the same time using one vial (1,000 mg/40 mL) on day 1.
      • Withdraw 40 mL of GAZYVA solution from the vial.
      • Dilute 4 mL (100 mg) of GAZYVA into a 100 mL 0.9% Sodium Chloride Injection, USP infusion bag for immediate administration.
      • Dilute the remaining 36 mL (900 mg) into a 250 mL 0.9% Sodium Chloride Injection, USP infusion bag at the same time for use on day 2 and store in a refrigerator at 2°C to 8°C (36°F to 46°F) for up to 24 hours. After allowing the diluted bag to come to room temperature, use immediately.
      • Clearly label each infusion bag.
    • Preparation of solution for infusion on day 8 and 15 of Cycle 1 and day 1 of Cycles 2–6:
      • Withdraw 40 mL of GAZYVA solution from the vial.
      • Dilute 40 mL (1,000 mg) into a 250 mL 0.9% Sodium Chloride Injection, USP infusion bag.
    Follicular Lymphoma, Active Lupus Nephritis and Childhood-Onset Idiopathic Nephrotic Syndrome patients weighing 45 kg or more
    • Preparation of solution for infusion:
      • Withdraw 40 mL of GAZYVA solution from the vial.
      • Dilute 40 mL (1,000 mg) into a 250 mL 0.9% Sodium Chloride Injection, USP infusion bag.
    Childhood-Onset Idiopathic Nephrotic Syndrome patients weighing less than 45 kg
    • Preparation of solution for infusion:
      • Calculate the dose (mg) based on the patient's body weight and the total volume of GAZYVA solution required.
      • Final GAZYVA solution to add to the infusion bag (mL)=Patient weight (kg) x 20 mg/kg× 40 mL
        1,000 mg
      • Withdraw a volume equal to the required GAZYVA solution from a 250 mL infusion bag of 0.9% Sodium Chloride Injection, USP and discard it.
      • Add the required volume of GAZYVA solution slowly into the 0.9% Sodium Chloride Injection, USP infusion bag. Discard any unused portion of GAZYVA solution remaining in the vial.
  • Mix diluted solution by gentle inversion. Do not shake or freeze.
  • For microbiological stability, immediately use diluted GAZYVA infusion solution. If not used immediately, store in a refrigerator at 2°C to 8°C (36°F to 46°F) for up to 24 hours prior to use.

The product can be administered at a final concentration of 0.4 mg/mL to 4 mg/mL.

SPL UNCLASSIFIED SECTION

Storage

Use the diluted solution immediately. If not used immediately, store for up to 24 hours at 2°C to 8°C. Discard after 24 hours.

SPL UNCLASSIFIED SECTION

Administration

  • Administer as an intravenous infusion only.
  • Do not administer as an intravenous push or bolus.
  • Do not mix GAZYVA with other drugs.
  • No incompatibilities between GAZYVA and polyvinylchloride (PVC) or non-PVC polyolefin bags and administration sets have been observed.

3 DOSAGE FORMS AND STRENGTHS

DOSAGE FORMS & STRENGTHS SECTION

Injection: 1,000 mg/40 mL (25 mg/mL) clear, colorless to slightly brown solution in a single-dose vial.

4 CONTRAINDICATIONS

CONTRAINDICATIONS SECTION

GAZYVA is contraindicated in patients with known hypersensitivity reactions (e.g., anaphylaxis) to obinutuzumab or to any of the excipients, or serum sickness with prior obinutuzumab use [see Warnings and Precautions (5.4)].

5 WARNINGS AND PRECAUTIONS

WARNINGS AND PRECAUTIONS SECTION

5.1 Hepatitis B Virus Reactivation

SPL UNCLASSIFIED SECTION

GAZYVA can cause Hepatitis B virus (HBV) reactivation. Hepatitis B virus (HBV) reactivation, in some cases resulting in fulminant hepatitis, hepatic failure, and death, can occur in patients treated with anti-CD20 antibodies such as GAZYVA. HBV reactivation has been reported in patients who are hepatitis B surface antigen (HBsAg) positive and also in patients who are HBsAg negative but are hepatitis B core antibody (anti-HBc) positive. Reactivation has also occurred in patients who appear to have resolved hepatitis B infection (i.e., HBsAg negative, anti-HBc positive, and hepatitis B surface antibody [anti-HBs] positive).

HBV reactivation is defined as an abrupt increase in HBV replication manifesting as a rapid increase in serum HBV DNA level or detection of HBsAg in a person who was previously HBsAg negative and anti-HBc positive. Reactivation of HBV replication is often followed by hepatitis, i.e., increase in transaminase levels and, in severe cases, increase in bilirubin levels, liver failure, and death.

Screen all patients for HBV infection by measuring HBsAg and anti-HBc before initiating treatment with GAZYVA. For patients who show evidence of hepatitis B infection (HBsAg positive [regardless of antibody status] or HBsAg negative but anti-HBc positive), consult healthcare providers with expertise in managing hepatitis B regarding monitoring and consideration for HBV antiviral therapy.

Monitor patients with evidence of current or prior HBV infection for clinical and laboratory signs of hepatitis or HBV reactivation during and for several months following treatment with GAZYVA. HBV reactivation has been reported for other CD20-directed cytolytic antibodies following completion of therapy.

In patients who develop reactivation of HBV while receiving GAZYVA, immediately discontinue GAZYVA and any concomitant chemotherapy and institute appropriate treatment. Resumption of GAZYVA in patients whose HBV reactivation resolves should be discussed with healthcare providers with expertise in managing hepatitis B. Insufficient data exist regarding the safety of resuming GAZYVA in patients who develop HBV reactivation.

5.2 Progressive Multifocal Leukoencephalopathy

SPL UNCLASSIFIED SECTION

John Cunningham (JC) virus infection resulting in progressive multifocal leukoencephalopathy (PML), which can be fatal, occurred in patients treated with GAZYVA for CLL and NHL. Consider the diagnosis of PML in any patient presenting with new onset or changes to preexisting neurologic manifestations. Evaluation of PML includes, but is not limited to, consultation with a neurologist, brain MRI, and lumbar puncture. Discontinue GAZYVA therapy and consider discontinuation or reduction of any concomitant chemotherapy or immunosuppressive therapy in patients who develop PML.

5.4 Hypersensitivity Reactions Including Serum Sickness

SPL UNCLASSIFIED SECTION

Hypersensitivity reactions have been reported in patients treated with GAZYVA. Signs of immediate-onset hypersensitivity included dyspnea, bronchospasm, hypotension, urticaria and tachycardia. Late-onset hypersensitivity diagnosed as serum sickness has also been reported, with symptoms that include chest pain, diffuse arthralgia and fever. Hypersensitivity reactions may be difficult to clinically distinguish from IRRs. However, hypersensitivity very rarely occurs with the first infusion and, when observed, often occurs after previous exposure.

If a hypersensitivity reaction is suspected during or after an infusion, stop the infusion and permanently discontinue treatment. GAZYVA is contraindicated in patients with known hypersensitivity reactions to GAZYVA, including serum sickness with prior GAZYVA use [see Contraindications (4)].

5.5 Tumor Lysis Syndrome

SPL UNCLASSIFIED SECTION

Tumor lysis syndrome (TLS), including fatal cases, has been reported in patients with CLL and NHL receiving GAZYVA. Patients with high tumor burden, high circulating lymphocyte count (> 25 × 109/L) or renal impairment are at greater risk for TLS.

In patients with CLL and NHL at risk for TLS, administer appropriate tumor lysis prophylaxis with anti-hyperuricemics (e.g., allopurinol or rasburicase) and hydration prior to the infusion of GAZYVA [see Dosage and Administration (2.6)]. During the initial days of GAZYVA treatment, monitor the laboratory parameters of patients considered at risk for TLS. For treatment of TLS, correct electrolyte abnormalities, monitor renal function and fluid balance, and administer supportive care, including dialysis as indicated. TLS is not identified as a risk in LN or childhood-onset INS.

5.6 Serious, Including Fatal, Infections

SPL UNCLASSIFIED SECTION

Fatal and serious bacterial, fungal, and new or reactivated viral infections can occur during and following GAZYVA therapy. When GAZYVA is administered with chemotherapy followed by GAZYVA monotherapy as in the GALLIUM study, Grade 3 to 5 infections have been reported in up to 8% of patients during combination therapy, up to 13% of patients during monotherapy, and up to 8% of patients after treatment [see Adverse Reactions (6.1)].

SPL UNCLASSIFIED SECTION

Lupus Nephritis

In the pooled double-blind periods of REGENCY (Week 76) and NOBILITY (Week 52), the incidence of Grade 3-5 infections was 11% (22/200) in patients treated with GAZYVA and standard therapy compared to 9% (18/193) in patients receiving placebo and standard therapy, corresponding to an exposure-adjusted incidence rate (EAIR) of 8.9 and 7.9 per 100 patient years, respectively. The incidence of fatal infections was 1% (2/200) in patients treated with GAZYVA and 0.5% (1/193) in patients receiving placebo, corresponding to an EAIR of 0.8 and 0.4 per 100 patient years, respectively.

In 40 patients who crossed-over from placebo to GAZYVA and standard therapy at Week 76 in the REGENCY study and patients who continued treatment with GAZYVA and standard therapy, including additional treatment after Week 76, the EAIR of Grade 3-5 infections for the GAZYVA arm was 9.0 per 100 patient-years while the EAIR of fatal infections for the GAZYVA arm was 1.8 per 100 patient-years.

SPL UNCLASSIFIED SECTION

Idiopathic Nephrotic Syndrome

In the INSHORE study, the incidence of Grade 3 (severe or medically significant) infections was 11% (5/44) in patients randomized to GAZYVA compared to 5% (2/41) in the mycophenolate mofetil (MMF) arm. The most frequently reported Grade 3 infection related to study treatment in the GAZYVA arm was pneumonia (2/44 patients, 5%) [see Adverse Reactions (6.1)]. No Grade 4 or Grade 5 (life-threatening or fatal) infections were reported in either arm.

SPL UNCLASSIFIED SECTION

CLL and FL

In GALLIUM, more Grade 3 to 5 infections were reported in the recipients of GAZYVA and bendamustine (117/410 patients, 29%) as compared to GAZYVA plus CHOP or CVP (43/281 patients, 15%). More fatal infections were reported in patients treated with GAZYVA and bendamustine (3%), as compared to GAZYVA plus CHOP or CVP (< 1%), including during the monotherapy phase and after completion of treatment.

Do not administer GAZYVA to patients with an active infection. Patients with a history of recurring or chronic infections may be at increased risk of infection. In patients who develop a serious infection while receiving GAZYVA, immediately discontinue GAZYVA and institute appropriate treatment. Consider the risk and benefit of resuming treatment with GAZYVA following resolution of serious infections.

5.7 Neutropenia

SPL UNCLASSIFIED SECTION

Severe and life-threatening neutropenia, including febrile neutropenia, has been reported during treatment with GAZYVA. Monitor patients with Grade 3 to 4 neutropenia frequently with regular laboratory tests until resolution. Anticipate, evaluate, and treat any symptoms or signs of developing infection. Consider dose delays for Grade 3 or 4 neutropenia. Consider administration of granulocyte colony-stimulating factor (GCSF) in patients with Grade 3 or 4 neutropenia.

Neutropenia can also be of late onset (occurring more than 28 days after completion of treatment) and/or prolonged (lasting longer than 28 days). Patients with severe and long lasting (> 1 week) neutropenia are strongly recommended to receive antimicrobial prophylaxis until resolution of neutropenia to Grade 1 or 2. Consider antiviral and antifungal prophylaxis.

5.8 Thrombocytopenia

SPL UNCLASSIFIED SECTION

Severe and life-threatening thrombocytopenia has been reported during treatment with GAZYVA in combination with chemotherapy. Fatal hemorrhagic events have been reported in patients with NHL and CLL treated with GAZYVA in combination with chemotherapy, including during Cycle 1.

Monitor patients frequently for thrombocytopenia and hemorrhagic events, especially during the first cycle and if clinically indicated, evaluate laboratory coagulation parameters [see Warnings and Precautions (5.9)]. In patients with Grade 3 or 4 thrombocytopenia, monitor platelet counts more frequently until resolution and consider dose delays of GAZYVA and chemotherapy or dose reductions of chemotherapy. Transfusion of blood products (i.e., platelet transfusion) may be necessary. Consider withholding concomitant medications that may increase bleeding risk (platelet inhibitors, anticoagulants), especially during the first cycle.

5.9 Disseminated Intravascular Coagulation (DIC)

SPL UNCLASSIFIED SECTION

Fatal and severe DIC has been reported in patients receiving GAZYVA for treatment of CLL and NHL. The majority of DIC cases have involved changes in platelets and laboratory coagulation parameters following the first infusion, with spontaneous resolution usually occurring by Day 8. In some cases, DIC was associated with IRRs, TLS, or both [see Adverse Reactions (6.1)].

In patients with suspected DIC, evaluate potential causes, and monitor coagulation parameters, platelet counts, and for signs and symptoms of bleeding or thrombosis. Manage according to standard guidelines for DIC. Supportive care, including transfusion of blood products and other medical management, may be necessary.

5.10 Immunization

SPL UNCLASSIFIED SECTION

Because of its mechanism of action, GAZYVA may interfere with the immune responses to vaccines and increase the risk of infection from live vaccines. The safety and efficacy of immunization with live or attenuated viral vaccines during or following GAZYVA therapy have not been studied. Immunization with live virus vaccines is not recommended during treatment with GAZYVA, and until B-cell recovery (CD19+ B-cell counts ≥ lower limit of normal or return to baseline).

In patients with childhood-onset INS, administer all age-appropriate live vaccines at least 28 days prior to initiation of GAZYVA. Do not administer live virus vaccines during treatment or until B-cell recovery is confirmed. Monitor B-cell counts prior to resuming any live vaccination. [see Use in Specific Populations (8.4) and Clinical Pharmacology (12.2) ].

5.11 Embryo-Fetal Toxicity

SPL UNCLASSIFIED SECTION

Based on its mechanism of action and findings in animals, GAZYVA can cause B-cell depletion in infants exposed to obinutuzumab in-utero. Advise pregnant women of the potential risk to the fetus. Advise females of reproductive potential to use effective contraception while taking GAZYVA and for 6 months after the last dose [see Use in Specific Populations (8.1, 8.3)].

6 ADVERSE REACTIONS

ADVERSE REACTIONS SECTION

The following clinically significant adverse reactions are described elsewhere in the labeling:

6.1 Clinical Trials Experience

CLINICAL TRIALS EXPERIENCE SECTION

Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice.

SPL UNCLASSIFIED SECTION

Chronic Lymphocytic Leukemia

The data below are based on a safety population of 773 previously untreated patients with CLL in the CLL11 study. Patients were treated with chlorambucil alone, GAZYVA in combination with chlorambucil, or rituximab product in combination with chlorambucil. The Stage 1 analysis compared GAZYVA in combination with chlorambucil vs. chlorambucil alone and Stage 2 compared GAZYVA in combination with chlorambucil vs. rituximab product in combination with chlorambucil. Adverse reactions rates and laboratory abnormalities from the Stage 2 phase are presented below and are consistent with the rates in Stage 1. In addition to the adverse reactions observed in Stage 2, in Stage 1, back pain (5% vs. 2%), anemia (12% vs. 10%) and cough (10% vs. 7%) were observed at a higher incidence in the GAZYVA treated patients. The incidence of Grade 3 to 4 back pain (< 1% vs. 0%), cough (0% vs. < 1%) and anemia (5% vs. 4%) was similar in both treatment arms. With regard to laboratory abnormalities, in Stage 1 hyperkalemia (33% vs. 18%), creatinine increased (30% vs. 20%) and alkaline phosphatase increased (18% vs. 11%) were observed at a higher incidence in patients treated with GAZYVA with similar incidences of Grade 3 to 4 abnormalities between the two arms.

Patients received three 1,000 mg doses of GAZYVA on the first cycle and a single dose of 1,000 mg once every 28 days for 5 additional cycles in combination with chlorambucil (6 cycles of 28 days each in total). In the last 140 patients enrolled, the first dose of GAZYVA was split between day 1 (100 mg) and day 2 (900 mg) [see Dosage and Administration (2.2)]. In total, 81% of patients received all 6 cycles (of 28 days each) of GAZYVA-based therapy.

Adverse reactions in ≥ 10% of patients in the GAZYVA containing arm were infusion-related reactions, neutropenia, thrombocytopenia, and diarrhea. The most common Grade 3 to 4 adverse reactions (incidence ≥ 10%) in the GAZYVA containing arm were neutropenia, infusion-related reactions, and thrombocytopenia.

Table 8 Adverse Reactions (Incidence ≥ 5% and ≥ 2% Greater in the GAZYVA Arm) in Patients with CLL (Stage 2)
Body System
Adverse Reactions
GAZYVA + Chlorambucil
n = 336
Rituximab product + Chlorambucil
n = 321
All Grades
%
Grades 3 to 4
%
All Grades
%
Grades 3 to 4
%
Injury, Poisoning and Procedural Complications
Infusion-Related Reaction6620384
Blood and Lymphatic System Disorders*
Neutropenia38333228
Thrombocytopenia141073
Gastrointestinal Disorders
Diarrhea1028< 1
Constipation8050
General Disorders and Administration Site Conditions
Pyrexia9< 17< 1
Infections and Infestations
Nasopharyngitis6< 130
Urinary Tract Infection512< 1

* Adverse reactions reported under "Blood and lymphatic system disorders" reflect those reported by investigator as clinically significant.

Table 9 Post-Baseline Laboratory Abnormalities (Incidence ≥ 10% and ≥ 2% Greater in the GAZYVA Arm) in Patients with CLL (Stage 2)
Laboratory AbnormalitiesGAZYVA + Chlorambucil
n = 336
Rituximab product + Chlorambucil
n = 321
All Grades %Grades 3 to 4 %All Grades %Grades 3 to 4 %
Hematology
Leukopenia84356216
Lymphopenia80395016
Neutropenia76466941
Thrombocytopenia4813408
Anemia39103710
Chemistry
Hypocalcemia37332< 1
ALT increased282211
AST increased27221< 1
Hyponatremia267182
Hypoalbuminemia23< 116< 1
Hypokalemia14110< 1
SPL UNCLASSIFIED SECTION

Non-Hodgkin Lymphoma

SPL UNCLASSIFIED SECTION

GADOLIN Study

The GADOLIN study evaluated safety in 407 patients with relapsed or refractory NHL, including FL (81%), small lymphocytic lymphoma and marginal zone lymphoma (a disease for which GAZYVA is not indicated), who did not respond to or progressed within 6 months of treatment with rituximab product or a rituximab product-containing regimen. In the population of patients with FL, the profile of adverse reactions was consistent with the overall NHL population. Patients received either GAZYVA in combination with bendamustine (204 patients), followed by GAZYVA monotherapy in patients that had not progressed, or bendamustine alone (203 patients).

Patients randomized to the GAZYVA + bendamustine arm received three weekly 1,000 mg doses of GAZYVA in the first cycle and a single dose of 1,000 mg once every 28 days for 5 additional cycles, in combination with bendamustine 90 mg/m2 intravenously on Days 1 and 2 in all 6 cycles. Patients who did not progress on the combination received a single 1,000 mg dose of GAZYVA monotherapy every two months until progression or for a maximum of two years. The control arm received bendamustine 120 mg/m2 on Days 1 and 2 of each cycle for 6 cycles, with a cycle length of 28 days. In the GAZYVA arm, 78% of patients received 6 cycles of bendamustine and 82% received their full 6 cycles of GAZYVA; 72 (46%) of the 158 patients who began GAZYVA monotherapy received all planned doses. In the control arm, 72% of patients received 6 cycles of bendamustine.

Serious adverse reactions occurred in 45% of the GAZYVA arm and 37% of the bendamustine-only arm. Fatal adverse reactions within 90 days of treatment occurred in 3.4% and 2.5%, respectively. During treatment and follow-up combined, fatal adverse reactions occurred in 10% of GAZYVA recipients and in 7.4% of recipients of bendamustine alone, with infection and second primary malignancies being the leading causes.

Dose modification due to adverse reactions occurred in 50% of the GAZYVA arm and 42% of the control arm, and discontinuation of any study drug due to adverse reactions occurred in 20% and 17%, respectively.

Table 10 presents selected adverse reactions in GADOLIN. The most common adverse reactions (incidence ≥ 20%) in GAZYVA recipients included infusion-related reactions, fatigue, neutropenia, cough, upper respiratory tract infections, and musculoskeletal pain.

Table 10 Adverse Reactions (Incidence ≥ 10% and ≥ 2% Greater in the GAZYVA Arm) in Patients with Relapsed or Refractory NHL (GADOLIN)
Body System
Adverse Reactions* , †
GAZYVA + Bendamustine followed by GAZYVA monotherapy
n = 204
Bendamustine
n = 203
All Grades
%
Grades 3 to 5
%
All Grades
%
Grades 3 to 5
%
Procedural Complications
Infusion-Related Reaction‡ 6711635
General Disorders
Fatigue403363
Pyrexia191151
Blood and Lymphatic System Disorders
Neutropenia3735§ 2927
Infections and Infestations
Upper Respiratory Tract Infection363231
Respiratory Tract Infection, Unspecified14180
Urinary Tract Infection13370
Respiratory, Thoracic and Mediastinal Disorders
Cough31<1210
Musculoskeletal and Connective Tissue Disorders
Musculoskeletal Pain281200
Arthralgia12<150
Skin and Subcutaneous Tissue Disorders
Rash17<114<1
Pruritus11060

* Includes adverse reactions reported throughout study treatment and follow-up.

† Includes grouped terms.

‡ Except where noted, individual events that meet the definition of "infusion-related reaction" are excluded from Table 10 above, as they are included in the grouped term "Infusion-Related Reaction".

§ Includes 1 fatal event.

Infusion-related reactions are defined as any related adverse reaction that occurred during or within 24 hours of infusion.

Fatigue includes fatigue, lethargy, asthenia.

Pyrexia includes pyrexia, hyperthermia, body temperature increased.

Cough includes cough, productive cough, upper-airway cough syndrome.

Neutropenia includes neutropenia, agranulocytosis, granulocytopenia, neutrophil count decreased.

Upper respiratory tract infection includes upper respiratory tract congestion, upper respiratory tract inflammation, upper respiratory fungal infection, rhinovirus infection, and all terms containing: upper respiratory tract infection, laryngitis, nasopharyngitis, pharyngitis, rhinitis, tonsillitis, and sinusitis with the exception of sinobronchitis.

Respiratory tract infection unspecified includes respiratory tract infection, respiratory tract infection viral, influenza, influenza-like illness, sinobronchitis, respiratory syncytial virus infection.

Urinary tract infection includes all terms containing: urinary tract infection, cystitis, pyelonephritis.

Musculoskeletal pain includes non-cardiac chest pain, bone pain, spinal pain, myalgia, back pain, neck pain, musculoskeletal discomfort, pain in extremity, and all terms containing "musculoskeletal pain".

Rash includes drug eruption, skin reaction, all terms containing "rash", urticaria, and selected terms containing "dermatitis".

Pruritus includes pruritus, pruritus generalized.

Other clinically relevant adverse reactions (incidence < 10% and ≥ 2% greater in the GAZYVA arm) included:

  • Blood and lymphatic system disorders: febrile neutropenia (6%)
  • Infection: sepsis (7%)

During GAZYVA monotherapy (158 patients), adverse reactions in ≥ 10% of patients included upper and lower respiratory tract infections, cough, neutropenia, musculoskeletal pain, fatigue, diarrhea, rash, and urinary tract infection.

Table 11 presents selected new or worsening laboratory abnormalities in the GADOLIN trial.

Table 11 New or Worsening Laboratory Abnormalities (Incidence ≥ 10% and ≥ 2% Greater in the GAZYVA Arm*) in Patients with Relapsed or Refractory NHL (GADOLIN)
Laboratory AbnormalitiesGAZYVA + Bendamustine followed by GAZYVA monotherapy
n = 204
Bendamustine
n = 203
All Grades %Grades 3 to 4 %All Grades %Grades 3 to 4 %
Hematology
Lymphopenia97929684
Leukopenia84478734
Neutropenia76537542
Chemistry
Hypophosphatemia418387
Hypocalcemia393241
ALT/SGPT increased362313
Alkaline phosphatase increased270230
Hyperbilirubinemia212172
Hyperkalemia203180

* Two percent difference in either any-grade or Grade 3 to 4 laboratory abnormalities.

In the GAZYVA monotherapy phase, new or worsening grade 3 or 4 abnormalities included neutropenia in 25% of patients (Grade 4, 10%) and lymphopenia in 23% (Grade 4, 5%).

SPL UNCLASSIFIED SECTION

GALLIUM Study

A randomized, open-label multicenter trial (GALLIUM) evaluated the safety of GAZYVA as compared to rituximab product in 1385 patients with previously untreated follicular lymphoma (86%) or marginal zone lymphoma (14%). Patients received chemotherapy (bendamustine, CHOP, or CVP) combined with either GAZYVA (691 patients) or rituximab product (694 patients), followed in responding patients by GAZYVA or rituximab product monotherapy every two months until disease progression or for a maximum of two years. The study excluded patients having an absolute neutrophil count (ANC) < 1500 / µL, platelets < 75,000 / µL, CLcr < 40 mL/min and, unless attributable to lymphoma, hepatic transaminases > 2.5 × upper limit of normal.

The median age was 60 (range: 23-88), 47% were male, 82% were white, and 97% had an ECOG performance status of 0 or 1. The chemotherapy was bendamustine in 59%, CHOP in 31% and CVP in 10% of patients. Following combination therapy, 624 patients (90%) in the GAZYVA arm and 612 patients (88%) in the rituximab product arm received monotherapy.

Serious adverse reactions occurred in 50% of patients on the GAZYVA arm and 43% of patients on the rituximab product arm. Fatal adverse reactions were reported during treatment in 3% in the GAZYVA arm and 2% in the rituximab product arm, most often from infections in the GAZYVA arm. During treatment and follow-up combined, fatal adverse reactions were reported in 5% of the GAZYVA arm and 4% of the rituximab product arm, with infections and second malignancies being leading causes. In the GAZYVA arm, fatal infections occurred in 2% of patients compared to < 1% in the rituximab product arm.

During combination therapy, 93% of patients received all treatment cycles in the GAZYVA arm, and 92% received all treatment cycles in the rituximab product arm. Of the responding patients who began monotherapy with GAZYVA or rituximab product, 76% and 73%, respectively, completed the full course. Dose modification due to adverse reactions occurred in 74% of the GAZYVA arm and 63% of the rituximab product arm throughout study treatment, and discontinuation of any study drug due to adverse reactions occurred in 18% and 15%, respectively.

Throughout treatment and follow-up, the most common adverse reactions (incidence ≥ 20%) observed at least 2% more in the GAZYVA arm included infusion-related reactions, neutropenia, upper respiratory tract infections, constipation and diarrhea (Table 12). Neutropenia, infusion-related reactions, febrile neutropenia and thrombocytopenia were the most common Grade 3 to 5 adverse reactions (incidence ≥ 5%) observed more frequently in the GAZYVA arm.

Table 12 Adverse Reactions (Incidence ≥ 10% and ≥ 2% Greater in the GAZYVA Arm) in Patients with Previously Untreated NHL (GALLIUM)
Body System
Adverse Reactions * , †
GAZYVA + chemotherapy followed by GAZYVA monotherapy
n = 691
Rituximab product + chemotherapy followed by rituximab product monotherapy
n = 694
All Grades
%
Grades 3 to 5
%
All Grades
%
Grades 3 to 5
%
Injury, Poisoning and Procedural Complications
Infusion-Related Reaction ‡ 7212608
Blood and Lymphatic System Disorders
Neutropenia § 53494741
Thrombocytopenia § 14783
Infections and Infestations
Upper Respiratory Tract Infection503431
Herpesvirus Infection183141
Pneumonia147126
Respiratory, Thoracic and Mediastinal Disorders
Cough35< 128< 1
Gastrointestinal Disorders
Constipation32< 129< 1
Diarrhea303262
Nervous System Disorders
Headache18< 115< 1
Musculoskeletal and Connective Tissue Disorders
Arthralgia16014< 1
Psychiatric Disorders
Insomnia15< 112< 1
Metabolism and Nutrition Disorders
Decreased Appetite14< 112< 1
Skin and Subcutaneous Tissue Disorders
Pruritus11< 190

* Includes adverse reactions reported throughout study treatment and follow-up.

† Includes grouped terms.

‡ Except where noted, individual events that meet the definition of "infusion-related reaction" are excluded from Table 12 above, as they are already included in the grouped term "Infusion-Related Reaction". The most common individual terms within the grouped term "Infusion-Related Reaction" in decreasing order of frequency are nausea, chills, pyrexia and vomiting.

§ Includes adverse reactions reported as infusion-related reactions.

Infusion-related reactions are defined as any related adverse reaction that occurred during or within 24 hours of infusion.

Neutropenia includes neutropenia, agranulocytosis, granulocytopenia, and neutrophil count decreased.

Febrile neutropenia includes febrile neutropenia, neutropenic infection, neutropenic sepsis, and febrile bone marrow aplasia.

Thrombocytopenia includes thrombocytopenia and platelet count decreased.

Upper respiratory tract infection includes upper respiratory tract congestion, upper respiratory tract inflammation, upper respiratory tract infection, rhinovirus infection, and all terms containing: laryngitis, nasopharyngitis, pharyngitis, rhinitis, tonsillitis, and sinusitis with the exception of sinobronchitis.

Herpesvirus infection includes all terms containing "herpes" or "varicella."

Pneumonia includes all terms containing "pneumonia," bacterial, pneumonia haemophilus, pneumonia pneumococcal, pneumonia fungal, pneumocystis jirovecii infection, lung infection, and lung infiltration.

Diarrhea includes diarrhea, defecation urgency, frequent bowel movement, and all terms containing "gastroenteritis".

Headache includes all terms containing "headache" and migraine.

Insomnia includes all terms containing "insomnia" and sleep disorder.

Pruritus includes pruritus and pruritus generalized.

During the monotherapy period, the common adverse reactions (incidence ≥ 10%) observed at least 2% more with GAZYVA were upper respiratory tract infection (40%), cough (23%), musculoskeletal pain (20%), neutropenia (19%), and herpesvirus infection (13%).

Table 13 summarizes treatment-emergent laboratory abnormalities during treatment and follow-up. The Grade 3 to 4 abnormalities reported at least 2% more in the GAZYVA arm were lymphopenia, leukopenia, neutropenia, thrombocytopenia, and hyperuricemia. Patients in the GAZYVA arm, as compared to the rituximab product arm, had higher incidences of Grade 4 neutropenia (38% vs. 30%, respectively), Grade 4 lymphopenia (33% vs. 22%), and Grade 4 leukopenia (17% vs. 12%).

Table 13 New or Worsening Laboratory Abnormalities (Incidence ≥ 10% and ≥ 2% Greater in the GAZYVA Arm) in Patients with Previously Untreated NHL (GALLIUM)
Laboratory Abnormalities * GAZYVA+ chemotherapy followed by GAZYVA monotherapy
n = 691
Rituximab product + chemotherapy followed by rituximab product monotherapy
n = 694
All Grades %Grades 3 to 4 %All Grades %Grades 3 to 4 %
Hematology
Lymphopenia97839567
Leukopenia92498939
Neutropenia84597650
Thrombocytopenia6811504
Chemistry
ALT increased503432
AST increased441411
Hypophosphatemia365335
Hypoalbuminemia331251
Hypoproteinemia320300
Hypocalcemia321261
Hyperuricemia28282222
Hyponatremia264 203
Hyperkalemia231171
Hypernatremia16< 1130

* Includes lab abnormalities, reported throughout treatment and follow-up, that were new or worsening, or worsening from baseline unknown.

In the monotherapy phase, new-onset Grade 3 or 4 neutropenia was reported in 21% of patients in the GAZYVA arm (Grade 4, 10%) and 17% of patients in the rituximab product arm (Grade 4, 9%).

SPL UNCLASSIFIED SECTION

GAZELLE Study

GAZELLE (NCT03817853) is a single-arm study designed to characterize the safety of GAZYVA administered as a shortened-duration infusion (approximately 90 minutes) in patients with previously untreated FL. All patients received GAZYVA at the standard infusion rate with premedication during Cycle 1. If no Grade 3 or higher IRR occurred with any infusion during Cycle 1, GAZYVA was administered over approximately 90 minutes in Cycle 2 and subsequent cycles. The primary safety measure was the proportion of patients who experienced Grade 3 or higher IRRs with the 90-minute infusion at Cycle 2. GAZYVA was administered in combination with CHOP, CVP or bendamustine for 6 to 8 cycles (induction), followed by monotherapy for up to 2 years.

Of the 113 patients treated with GAZYVA, 99 (88%) received the 90-minute infusion starting in Cycle 2. In total, 97% of patients who received GAZYVA at either a standard or shorter infusion duration received premedication in Cycle 2. IRRs were observed in 63% of patients throughout induction (including IRRs observed after standard-duration infusion). In cycle 1, 58% of patients developed IRRs with the standard infusion rate (Grade ≥3 IRR, 5%). Of the patients who received the 90-minute infusion, 10% had IRRs of any grade in Cycle 2, with 8% and 2% of patients having a Grade 1 IRR or Grade 2 IRR, respectively. Following Cycle 2, one (1%) patient experienced a Grade 3 IRR, which occurred after the 90-minute infusion at Cycle 5.

SPL UNCLASSIFIED SECTION

Lupus Nephritis

The data below reflects exposure to GAZYVA administered intravenously in patients with ISN/RPS 2003 Class III or IV with or without concomitant Class V lupus nephritis in the REGENCY and NOBILITY studies, up to week 76.

REGENCY (NCT04221477) is a Phase III study which included 136 patients treated with GAZYVA plus standard therapy consisting of mycophenolate mofetil (MMF) and corticosteroids [see Clinical Studies (14.3) ].

NOBILITY (NCT02550652) is a Phase II study which included 64 patients treated with GAZYVA plus standard therapy consisting of MMF/mycophenolic acid (MPA) and corticosteroids.

The most common adverse reactions (incidence ≥ 5% in the GAZYVA arm) were upper respiratory tract infection, COVID-19, urinary tract infection, bronchitis, pneumonia, infusion related reactions and neutropenia.

The most common serious adverse reactions in the GAZYVA arm were: COVID-19 (11 patients [5.5%]), pneumonia (9 patients [4.5%]), neutropenia (7 patients [3.5%]), urinary tract infections (5 patients [2.5%]) and infusion-related reactions (1 patient [0.5%]). No serious adverse reactions were reported for bronchitis, herpes simplex and upper respiratory tract infections. Two fatal adverse reactions of COVID-19 were reported in the GAZYVA arm.

Adverse reaction rates are presented in Table 14.

Table 14 Adverse Reactions in Adults with Active Lupus Nephritis Treated with GAZYVA Versus Placebo (≥ 2% Greater in the GAZYVA Arm) in REGENCY and NOBILITY Studies
Body System
  Adverse Reactions
GAZYVA + standard therapy
n = 200
Placebo + standard therapy
n = 193
All Grades
(%)
Grades 3-5(%)All Grades
(%)
Grades 3-5
(%)
Infections and Infestations
Upper Respiratory Tract Infection290240
COVID-19235 * 160.5 *
Urinary Tract Infection213184
Bronchitis14080.5
Pneumonia10262
Herpes Simplex3000
Injury, Poisoning and Procedural Complications
Infusion Related Reaction142100.5
Blood and Lymphatic System Disorders
Neutropenia14760.5

* Includes 2 fatal events in the GAZYVA arm and 1 fatal event in the placebo arm

SPL UNCLASSIFIED SECTION

Childhood-Onset Idiopathic Nephrotic Syndrome

The data described in Table 15 reflect exposure to GAZYVA administered intravenously in patients with childhood-onset INS in the INSHORE study (NCT05627557). In INSHORE, 44 patients received GAZYVA, of which 41 patients were 4 to 18 years of age [see Clinical Studies (14.4)]. Adverse event severity was graded as Grades 1 to 5 defined as mild (1), moderate (2), severe (3), life-threatening (4), and fatal (5).

The most common adverse reactions (incidence ≥ 10% in the GAZYVA arm) are shown in Table 15. There were no Grade 5 adverse reactions in INSHORE.

Table 15 Adverse Reactions in Patients with Childhood-Onset Idiopathic Nephrotic Syndrome Treated with GAZYVA Versus Mycophenolate Mofetil (≥ 10% in the GAZYVA Arm) in the INSHORE study
Body System
   Adverse Drug Reactions
GAZYVA
n = 44
MMF
n = 41
All Grades
(%)
Grades 3-4
(%)
All Grades
(%)
Grades 3-4
(%)
NA: Not Applicable
Infections and Infestations
Upper Respiratory Tract Infection592632
Ear Infection322150
Pneumonia25950
Influenza200100
Bronchitis14250
COVID-19140120
Conjunctivitis14070
Urinary Tract Infection11000
Injury, Poisoning and Procedural Complications
Infusion Related Reaction360NANA
Blood and Lymphatic System Disorders
Neutropenia* 181622

* Total neutrophil counts < 1000 cells/µL occurred in 8 (18%) patients in the GAZYVA arm compared to 2 (5%) in the MMF arm.

SPL UNCLASSIFIED SECTION

Specific Adverse Reactions

SPL UNCLASSIFIED SECTION

Infusion-Related Reactions

SPL UNCLASSIFIED SECTION

Chronic Lymphocytic Leukemia

The incidence of IRRs in the CLL11 study was 65% with the first infusion of GAZYVA. The incidence of Grade 3 or 4 IRRs was 20% with 7% of patients discontinuing therapy. The incidence of reactions with subsequent infusions was 3% with the second 1,000 mg and < 1% thereafter. No Grade 3 or 4 IRRs were reported beyond the first 1,000 mg infused.

Of the first 53 patients receiving GAZYVA in CLL11, 47 (89%) experienced an IRR. After this experience, study protocol modifications were made to require pre-medication with a corticosteroid, antihistamine, and acetaminophen. The first dose was also divided into two infusions (100 mg on day 1 and 900 mg on day 2). For the 140 patients for whom these mitigation measures were implemented, 74 patients (53%) experienced a reaction with the first 1,000 mg (64 patients on day 1, 3 patients on day 2, and 7 patients on both days) and < 3% thereafter [see Dosage and Administration (2.2)].

SPL UNCLASSIFIED SECTION

Non-Hodgkin Lymphoma

Overall, 67% of patients in the GADOLIN study experienced an IRR (all grades) during treatment with GAZYVA in combination with bendamustine. The incidence of Grade 3 to 4 IRRs in GADOLIN was 11%. In Cycle 1, the incidence of IRRs (all grades) was 53% in patients receiving GAZYVA in combination with bendamustine of which 34 (9%) were Grade 3 to 4 in severity. In patients receiving GAZYVA in combination with bendamustine, the incidence of IRRs was highest on Day 1 (37%), and gradually decreased on Days 2, 8 and 15 (23%, 6% and 4%, respectively).

During Cycle 2, the incidence of IRRs was 24% in patients receiving GAZYVA in combination with bendamustine and decreased with subsequent cycles.

During GAZYVA monotherapy in GADOLIN, IRRs (all grades) were observed in 8% of patients. One Grade 3 and no Grade 4 IRRs were reported during GAZYVA monotherapy.

Overall, 2% of patients in GADOLIN experienced an IRR leading to discontinuation of GAZYVA.

In GALLIUM, 72% of patients in the GAZYVA treated arm experienced an IRR (all grades). The incidence of Grade 3 to 4 IRRs for these patients was 12%. In Cycle 1, the incidence of IRRs (all grades) was 62% in the GAZYVA treated arm with Grade 3 to 4 IRRs reported in 10%. The incidence of IRRs (all grades) was highest on Day 1 (60%) and decreased on Days 8 and 15 (9% and 6%, respectively).

During Cycle 2, the incidence of IRRs (all grades) in the GAZYVA treated arm was 13% and decreased with subsequent cycles.

During GAZYVA monotherapy treatment in GALLIUM, IRRs (all grades) were observed in 9% of patients.

Overall, 1% of patients in GALLIUM experienced an IRR leading to discontinuation of GAZYVA.

In GAZELLE, 10% of patients with FL experienced IRRs of any grade at Cycle 2 when GAZYVA was administered over approximately 90 minutes.

SPL UNCLASSIFIED SECTION

Lupus Nephritis

In the pooled REGENCY and NOBILITY studies, infusion-related reactions (IRRs) were reported in 14% of patients in the GAZYVA arm versus 10% of patients in the placebo arm. IRRs in both arms were predominantly Grade 1-2 and occurred during or after the first infusion. Grade 3-4 IRRs were reported in 1.5% of patients in the GAZYVA arm vs 0.5% of patients in the placebo arm. All Grade 3-4 events occurred during or after either the first or second infusion.

The incidence of IRRs in the GAZYVA arm decreased from 11% during the first infusion to 3% during the second infusion, decreasing further with subsequent infusions to 0.5% during the sixth infusion. The severity of IRRs in the GAZYVA arm also decreased with subsequent infusions with 1% patients reporting Grade 3-4 IRRs during the first infusion and 0.5% patients reporting Grade 3-4 IRRs during the second infusion. In subsequent infusions all IRRs were Grade 1-2 in severity. No Grade 5 IRRs were reported [see Warnings and Precautions (5.3)].

In the REGENCY study, most common IRR signs or symptoms included headache, nausea and vomiting. In the NOBILITY study, the most common IRR symptoms were pyrexia and tachycardia.

SPL UNCLASSIFIED SECTION

Childhood-Onset Idiopathic Nephrotic Syndrome

In the INSHORE study, all IRRs were Grade 1-2 (mild or moderate) and predominately occurred during/after the first infusion [see Table 15 and Warnings and Precautions (5.3)]. IRRs requiring GAZYVA infusion interruption, rate reduction, or stoppage occurred in 23% of patients. The most common IRR signs or symptoms included pyrexia, vomiting and nausea.

SPL UNCLASSIFIED SECTION

Neutropenia

SPL UNCLASSIFIED SECTION

Chronic Lymphocytic Leukemia

The incidence of neutropenia reported as an adverse reaction in CLL11 was 38% in the GAZYVA treated arm and 32% in the rituximab product treated arm, with the incidence of serious adverse reactions being 1% and < 1%, respectively (Table 9). Cases of late-onset neutropenia (occurring 28 days after completion of treatment or later) were 16% in the GAZYVA treated arm and 12% in the rituximab product treated arm.

SPL UNCLASSIFIED SECTION

Non-Hodgkin Lymphoma

The incidence of neutropenia in GADOLIN was higher in the GAZYVA plus bendamustine arm (37%) compared to the arm treated with bendamustine alone (30%). Cases of prolonged neutropenia (3%) and late onset neutropenia (8%) were also reported in the GAZYVA plus bendamustine arm. The incidence of neutropenia was higher during treatment with GAZYVA in combination with bendamustine (30%) compared to the GAZYVA monotherapy treatment phase (13%).

The incidence of neutropenia in GALLIUM was higher in the GAZYVA treated arm (53%) compared to the rituximab product treated arm (47%). Cases of prolonged neutropenia (1%) and late onset neutropenia (4%) were also reported in the GAZYVA treated arm. The incidence of neutropenia was higher during treatment with GAZYVA in combination with chemotherapy (45%) compared to the GAZYVA monotherapy treatment phase (20%).

SPL UNCLASSIFIED SECTION

Lupus Nephritis

In the pooled REGENCY and NOBILITY studies, neutropenia and related adverse reactions (i.e., leukopenia, lymphopenia, lymphocyte count decreased, febrile neutropenia, and neutrophil count decreased) were reported in 14% of patients in the GAZYVA arm versus 6% of patients in the placebo arm. Grade 3-4 neutropenia was reported in 7% of patients treated with GAZYVA versus 0.5% of patients in the placebo arm. Neutropenia and related adverse reactions resolved/improved spontaneously or with use of granulocyte colony-stimulating factor in 96% of patients [see Warnings and Precautions (5.7)].

SPL UNCLASSIFIED SECTION

Childhood-Onset Idiopathic Nephrotic Syndrome

In the INSHORE study, the majority of neutropenia and related adverse reactions (i.e., neutrophil count decreased and agranulocytosis) in both arms were Grade 3 or 4 (severe or life-threatening or due to neutrophil count < 1000 cells/µL; see Table 15). The majority of neutropenia and related events resolved/improved spontaneously and one event resolved with the use of granulocyte colony-stimulating factor [see Warnings and Precautions (5.7)].

SPL UNCLASSIFIED SECTION

Infection

SPL UNCLASSIFIED SECTION

Chronic Lymphocytic Leukemia

The incidence of infections was similar between GAZYVA and rituximab product treated arms. Thirty-eight percent of patients in the GAZYVA treated arm and 37% in the rituximab product treated arm experienced an infection, with Grade 3 to 4 rates being 11% and 13%, respectively. Fatal events were reported in 1% of patients in both arms.

SPL UNCLASSIFIED SECTION

Non-Hodgkin Lymphoma

The incidence of infection in GADOLIN was 68% in the GAZYVA plus bendamustine arm and 59% in the bendamustine arm, with Grade 3 to 4 events reported in 20% and 16%, respectively. Fatal events were reported in 3% of patients in the GAZYVA plus bendamustine arm and 3% in the bendamustine arm.

The incidence of infections in GALLIUM was 82% in the GAZYVA treated arm and 73% in the rituximab product treated arm, with Grade 3 to 4 events reported in 21% and 17%, respectively. In the GAZYVA arm, fatal infections occurred in 2% of patients compared to <1% in the rituximab product arm.

The incidence of Grade 3 to 4 infections in the GAZYVA and rituximab product treated arms was lower in patients receiving GCSF prophylaxis (14%; 16%) compared with patients not receiving GCSF prophylaxis (24%; 18%). The incidence of fatal infections in patients receiving GCSF prophylaxis in the GAZYVA and rituximab product treated arms was 2% and 0%, respectively, and was 2% and < 1% in patients not receiving GCSF prophylaxis.

SPL UNCLASSIFIED SECTION

Lupus Nephritis

In the pooled REGENCY and NOBILITY studies, infections were reported in 72% of patients in the GAZYVA arm versus 62% of patients in the placebo arm. The most frequently reported infections were upper and lower respiratory tract infections. Grade 3-5 infections were reported in 11% of patients in the GAZYVA arm versus 10% of patients in the placebo arm. Fatal infection events were reported in 1% of patients in the GAZYVA arm versus 0.5% of patients in the placebo arm [see Warnings and Precautions (5.6)].

SPL UNCLASSIFIED SECTION

Childhood-Onset Idiopathic Nephrotic Syndrome

In the INSHORE study, infections were reported in 89% of patients in the GAZYVA arm compared to 76% in the MMF arm. The most frequently reported infections are shown in Table 15 [see Warnings and Precautions (5.6)].

SPL UNCLASSIFIED SECTION

Thrombocytopenia

SPL UNCLASSIFIED SECTION

Chronic Lymphocytic Leukemia

The overall incidence of thrombocytopenia reported as an adverse reaction was higher in the GAZYVA treated arm (14%) compared to the rituximab product treated arm (7%), with the incidence of Grade 3 to 4 events being 10% and 3%, respectively (Table 8). The difference in incidences between the treatment arms is driven by events occurring during the first cycle. The incidence of thrombocytopenia (all grades) in the first cycle was 11% in the GAZYVA and 3% in the rituximab product treated arms, with Grade 3 to 4 rates being 8% and 2%, respectively. Four percent of patients in the GAZYVA treated arm experienced acute thrombocytopenia (occurring within 24 hours after the GAZYVA infusion).

The overall incidence of hemorrhagic events and the number of fatal hemorrhagic events were similar between the treatment arms, with 3 in the rituximab product and 4 in the GAZYVA treated arms. However, all fatal hemorrhagic events in patients treated with GAZYVA occurred in Cycle 1.

SPL UNCLASSIFIED SECTION

Non-Hodgkin Lymphoma

The incidence of thrombocytopenia in GADOLIN was lower in the GAZYVA plus bendamustine arm (15%) compared to the arm treated with bendamustine alone (25%). The incidence of hemorrhagic events in GAZYVA plus bendamustine treated patients compared to bendamustine alone was 12% and 11%, respectively. Grade 3 to 4 hemorrhagic events were similar in both treatment arms (4% in the GAZYVA plus bendamustine arm and 2% in the bendamustine arm).

In GALLIUM, thrombocytopenia was reported as an adverse reaction in 14% of the GAZYVA treated arm and 8% of the rituximab product treated arm, with the incidence of Grade 3 to 4 events being 7% and 3%, respectively. The difference in incidences between the treatment arms is driven by events occurring during the first cycle. The incidence of thrombocytopenia (all grades) in the first cycle was 9% in the GAZYVA and 3% in the rituximab product treated arms, with Grade 3 to 4 rates being 5% and 1%, respectively. In GALLIUM, both treatment arms had a 12% overall incidence of hemorrhagic events and a < 1% incidence of fatal hemorrhagic events.

SPL UNCLASSIFIED SECTION

Disseminated Intravascular Coagulation

In GALLIUM, DIC was reported as an adverse reaction in 0.3% of the GAZYVA treated patients. All events occurred within 1-2 days after the first infusion.

SPL UNCLASSIFIED SECTION

Tumor Lysis Syndrome

The incidence of Grade 3 or 4 tumor lysis syndrome in GAZYVA treated patients was 2% in CLL11, 0.5% in GADOLIN and 0.9% in GALLIUM.

SPL UNCLASSIFIED SECTION

Musculoskeletal Disorders

SPL UNCLASSIFIED SECTION

Chronic Lymphocytic Leukemia

Adverse reactions related to musculoskeletal disorders (all events from the body system), including pain, have been reported in the GAZYVA treated arm with higher incidence than in the rituximab product treated arm (18% vs. 15%).

SPL UNCLASSIFIED SECTION

Non-Hodgkin Lymphoma

In GADOLIN, adverse reactions related to musculoskeletal disorders (all events from the body system), including pain, have been reported in the GAZYVA plus bendamustine treated arm with higher incidence than in the bendamustine alone arm (44% vs. 30%).

In GALLIUM, musculoskeletal disorders were reported in 54% of patients in the GAZYVA treated arm and 49% of patients in the rituximab product treated arm.

SPL UNCLASSIFIED SECTION

Liver Enzyme Elevations

Hepatic enzyme elevations have occurred in CLL patients who received GAZYVA in clinical trials and had normal baseline hepatic enzyme levels (AST, ALT and ALP). The events occurred most frequently within 24–48 hours of the first infusion. In some patients, elevations in liver enzymes were observed concurrently with IRRs or tumor lysis syndrome. In the CLL11 study, there was no clinically meaningful difference in overall hepatotoxicity adverse reactions between all arms (4% of patients in the GAZYVA treated arm). Medications commonly used to prevent IRRs (e.g., acetaminophen) may also be implicated in these events. Monitor liver function tests during treatment, especially during the first cycle. Consider treatment interruption or discontinuation for hepatotoxicity.

SPL UNCLASSIFIED SECTION

Gastrointestinal Perforation

Cases of gastrointestinal perforation have been reported in patients receiving GAZYVA, mainly in NHL.

SPL UNCLASSIFIED SECTION

Worsening of Pre-existing Cardiac Conditions

Fatal cardiac events have been reported in patients treated with GAZYVA.

6.2 Postmarketing Experience

POSTMARKETING EXPERIENCE SECTION

The following adverse reactions have been identified during postapproval use of GAZYVA. Because these reactions are reported voluntarily from a population of uncertain size, it is not always possible to reliably estimate their frequency or establish a causal relationship to drug exposure.

  • Immune/Autoimmune Events: Serum sickness

8 USE IN SPECIFIC POPULATIONS

USE IN SPECIFIC POPULATIONS SECTION

8.1 Pregnancy

PREGNANCY SECTION

SPL UNCLASSIFIED SECTION

Risk Summary

Based on findings from animal studies and its mechanism of action, GAZYVA can cause fetal B-cell depletion [see Clinical Pharmacology (12.1)]. There are no data with GAZYVA use in pregnant women to inform a drug-associated risk. Monoclonal antibodies are transferred across the placenta. In animal reproduction studies, weekly intravenous administration of obinutuzumab to pregnant cynomolgus monkeys from day 20 of pregnancy until parturition which includes the period of organogenesis at doses with exposures up to 2.4 times the exposure at the clinical dose of 1,000 mg monthly produced opportunistic infections and immune complex mediated hypersensitivity reactions. No embryo-toxic or teratogenic effects were observed in the monkeys (see Data). Advise pregnant women of the potential risk to the fetus.

The background risk of major birth defects and miscarriage for the indicated population is unknown; however, the estimated background risk in the U.S. general population of major birth defects is 2% to 4% and of miscarriage is 15% to 20% of clinically recognized pregnancies.

SPL UNCLASSIFIED SECTION

Clinical Considerations

SPL UNCLASSIFIED SECTION

Disease-Associated Maternal and/or Embryo/Fetal Risk

Pregnant women with systemic lupus erythematosus (SLE) are at increased risk of adverse pregnancy outcomes, including worsening of the underlying disease, premature birth, miscarriage, and intrauterine growth restriction. Maternal LN increases the risk of hypertension and preeclampsia/eclampsia. Passage of maternal autoantibodies across the placenta may result in adverse neonatal outcomes, including neonatal lupus and congenital heart block.

SPL UNCLASSIFIED SECTION

Data

SPL UNCLASSIFIED SECTION

Animal Data

In a pre- and post-natal development study, pregnant cynomolgus monkeys received weekly intravenous doses of 25 or 50 mg/kg obinutuzumab from day 20 of pregnancy until parturition, which includes the period of organogenesis. The high dose results in an exposure (AUC) that is 2.4 times the exposure in patients with CLL at the recommended label dose. There were no embryo-toxic or teratogenic effects in animals. Secondary opportunistic infections, immune complex mediated hypersensitivity reactions, or a combination of both were observed in exposed dams. When first measured on day 28 postpartum, obinutuzumab was detected in offspring at levels in the range of maternal serum levels on the same day, and B-cells were completely depleted. The B-cell counts returned to normal levels, and immunologic function was restored within 6 months after birth.

8.2 Lactation

LACTATION SECTION

SPL UNCLASSIFIED SECTION

Risk Summary

There is no information regarding the presence of GAZYVA in human milk, the effects on the breastfed child, or the effects on milk production. However, low levels of obinutuzumab were present in the milk of lactating cynomolgus monkeys [see Data]. Human IgG is known to be present in human milk. Because of the potential of serious adverse reactions in the breastfed child, advise women not to breastfeed during treatment with GAZYVA and for 6 months after the last dose.

SPL UNCLASSIFIED SECTION

Data

Obinutuzumab was measured in the milk of lactating cynomolgus monkeys on day 28 postpartum after weekly intravenous administration from day 20 of pregnancy until parturition. Concentrations in milk were approximately 0.04% and 0.13% of concentrations in maternal serum in the 25 and 50 mg/kg groups, respectively.

8.3 Females and Males of Reproductive Potential

FEMALES & MALES OF REPRODUCTIVE POTENTIAL SECTION

SPL UNCLASSIFIED SECTION

Contraception

SPL UNCLASSIFIED SECTION

Females

Advise females of reproductive potential to use effective contraception during treatment with GAZYVA and for 6 months after the last dose.

8.4 Pediatric Use

PEDIATRIC USE SECTION

The safety and effectiveness of GAZYVA for reducing the risk of relapse in steroid dependent or frequently relapsing childhood-onset INS have been established in pediatric patients aged 2 years and older. Use of GAZYVA for this indication is supported by evidence from an adequate and well controlled trial that enrolled 81 pediatric patients aged 2 years and older [see Adverse Reactions (6.1), and Clinical Studies (14.4)]. The safety and effectiveness of GAZYVA for reducing the risk of relapse in pediatric patients less than 2 years of age with steroid dependent or frequently relapsing childhood-onset INS have not been established.

The safety and efficacy of GAZYVA in pediatric patients with chronic lymphocytic leukemia, follicular lymphoma, or active lupus nephritis have not been established.

8.5 Geriatric Use

GERIATRIC USE SECTION

SPL UNCLASSIFIED SECTION

Chronic Lymphocytic Leukemia

Of 336 patients with previously untreated CLL who received GAZYVA in combination with chlorambucil, 81% were 65 years and older, while 46% were 75 and older. Of the patients 75 years and older, 46% experienced serious adverse reactions and 7% experienced adverse reactions leading to death. Of the patients younger than 75, 33% experienced a serious adverse reaction and 2% an adverse reaction leading to death. No significant differences in efficacy were observed between younger and older patients [see Clinical Studies (14.1)].

SPL UNCLASSIFIED SECTION

Non-Hodgkin Lymphoma

Of 204 patients in GADOLIN with relapsed or refractory NHL treated with GAZYVA plus bendamustine, 44% were 65 and over, while 14% were 75 and over. In patients 65 and over, 55% of patients experienced serious adverse reactions and 28% experienced adverse reactions leading to treatment withdrawal while in patients under 65, 37% and 14% experienced serious adverse reactions and adverse reactions leading to treatment withdrawal, respectively. No clinically meaningful differences in efficacy were observed between these patients and younger patients in GADOLIN.

Of the 691 patients in GALLIUM treated with GAZYVA plus chemotherapy as first-line therapy, 33% were 65 and over, while 7% were 75 and over. Of patients 65 and over, 63% experienced serious adverse reactions and 26% experienced adverse reactions leading to treatment withdrawal, while in patients under 65, 43% experienced serious adverse reactions and 13% had an adverse reaction leading to treatment withdrawal. No clinically meaningful differences in efficacy were observed between these patients and younger patients in GALLIUM.

SPL UNCLASSIFIED SECTION

Lupus Nephritis and Childhood-Onset Idiopathic Nephrotic Syndrome

Clinical studies of GAZYVA in patients with active LN or childhood-onset INS did not include sufficient numbers of patients aged 65 years and older (1 patient and 0 patients, respectively) to determine whether they respond differently from younger adult patients.

10 OVERDOSAGE

OVERDOSAGE SECTION

There has been no experience with overdose in human clinical trials. For patients who experience overdose, treatment should consist of immediate interruption or reduction of GAZYVA and supportive therapy.

11 DESCRIPTION

DESCRIPTION SECTION

Obinutuzumab is a humanized anti-CD20 monoclonal antibody of the IgG1 subclass. It recognizes a specific epitope of the CD20 molecule found on B cells. The molecular mass of the antibody is approximately 150 kDa.

GAZYVA (obinutuzumab) injection is produced by mammalian cell (CHO) suspension culture. GAZYVA was engineered to have reduced fucose content as compared to a typical IgG1 produced in CHO cells. GAZYVA is a sterile, clear, colorless to slightly brown, preservative-free liquid concentrate for intravenous use. GAZYVA is supplied at a concentration of 25 mg/mL in 1,000 mg single-dose vials. Each vial contains in 40 mL: 1,000 mg obinutuzumab, L-histidine (57.6 mg), L-histidine hydrochloride monohydrate (89.6 mg), trehalose dihydrate (3632 mg), and poloxamer 188 (8 mg). The pH is 6.0.

12 CLINICAL PHARMACOLOGY

CLINICAL PHARMACOLOGY SECTION

12.1 Mechanism of Action

MECHANISM OF ACTION SECTION

Obinutuzumab is a monoclonal antibody that targets the CD20 antigen expressed on the surface of pre-B and mature B lymphocytes. Upon binding to CD20, obinutuzumab mediates B-cell lysis through (1) engagement of immune effector cells, (2) by directly activating intracellular death signaling pathways (direct cell death), and/or (3) activation of the complement cascade. The immune effector cell mechanisms include antibody-dependent cellular cytotoxicity (ADCC) and antibody-dependent cellular phagocytosis.

As an antibody with reduced fucose content, obinutuzumab induces greater ADCC activity than rituximab in vitro using human cancer cell lines. Obinutuzumab also demonstrated an increased ability to induce direct cell death when compared to rituximab. Obinutuzumab binds to FcγRIII using purified proteins with a higher affinity than rituximab. Obinutuzumab and rituximab bind with similar affinity to overlapping epitopes on CD20.

12.2 Pharmacodynamics

PHARMACODYNAMICS SECTION

SPL UNCLASSIFIED SECTION

Chronic Lymphocytic Leukemia

In patients with CLL, GAZYVA caused CD19 B-cell depletion (defined as CD19 B cell counts < 0.07 × 109/L). Initial CD19 B cell recovery was observed in some patients approximately 9 months after the last GAZYVA dose. At 18 months of follow-up, some patients remain B cell depleted.

Although the depletion of B cells in the peripheral blood is a measurable pharmacodynamic effect, it is not directly correlated with the depletion of B-cells in solid organs or in malignant deposits. B cell depletion has not been shown to be directly correlated to clinical response.

SPL UNCLASSIFIED SECTION

Lupus Nephritis

In patients with LN (REGENCY study), total peripheral CD19+ B cell levels below the defined threshold of 10 cells/µl were achieved in 99% of patients treated with GAZYVA by Week 4 after treatment initiation and remained below this threshold in 95% of patients at Week 76.

Reductions in circulating naive B, memory B, and plasmablasts/plasma cells were observed by Week 4 and remained low through Week 76 after treatment initiation.

Treatment with GAZYVA led to improvements in complement (C3 and C4) and anti-double-stranded DNA antibodies (anti-dsDNA) by Week 4 and Week 12, respectively. These changes were sustained through Week 76.

In patients with low C3 at baseline, normalization of C3 levels occurred in 49% (by Week 12) and in 62% (by Week 76) of patients receiving GAZYVA compared to 33% and 29%, respectively, in the placebo group. In patients with low C4 at baseline, normalization of C4 levels occurred in 75% (by Week 12) and in 88% (by Week 76) of patients receiving GAZYVA compared to 55% and 55%, respectively, in the placebo group. Among patients with positive anti-dsDNA at baseline, 32% and 56% of patients treated with GAZYVA seroconverted by Week 4 and Week 76, respectively, compared with 16% and 16% of patients receiving placebo. The clinical relevance of the above mentioned pharmacodynamic biomarkers has not been established.

SPL UNCLASSIFIED SECTION

Childhood-Onset Idiopathic Nephrotic Syndrome

In evaluable patients aged 4 years and older with childhood-onset INS who received GAZYVA in INSHORE, 100% (43 out of 43) were B-cell depleted (defined as CD19+ B cell counts < 10 cells/µL) at Week 4, and 95% (40 out of 42) remained depleted at Week 52. At Week 64, 73% (19 out of 26) remained B-cell depleted, and at Week 76, 36% (8 out of 22) remained depleted.

Mean counts of circulating B-cell subsets such as naïve B cells, memory B cells, and plasmablasts/plasma cells were 0 cells/µL by Week 2 after treatment initiation and remained low (near 0 cells/µL) through Week 52.

SPL UNCLASSIFIED SECTION

Cardiac Electrophysiology

The potential effects of GAZYVA on the QTc interval have not been studied.

12.3 Pharmacokinetics

PHARMACOKINETICS SECTION

The pharmacokinetic parameters of obinutuzumab after 100 mg on day 1 and 900 mg on day 2 of Cycle 1, 1,000 mg on day 8 and 15 of Cycle 1, and 1,000 mg on day 1 of Cycles 2-6 for CLL; after 1,000 mg on day 1, 8 and 15 of Cycle 1, 1,000 mg on day 1 of Cycles 2-6 or Cycles 2-8, and then 1,000 mg every 2 months for up to 2 years for NHL; 1,000 mg on day 1, week 2, 24, 26 and every 6 months for up to 76 Weeks for LN and childhood-onset INS are provided in Table 16. The dosing regimen is within the linear pharmacokinetic behavior of obinutuzumab.

Table 16 Obinutuzumab Pharmacokinetic Parameters
PK MeasureCLL* Relapsed or refractory FL* First line FL in combination with chemotherapyLN† Childhood-Onset INS‡
GAZYVA + Bendamustine* GAZYVA + CHOP or CVP§
Results are presented as geometric mean (% Coefficient of Variation).
Cmax, µg/mL466.3 (35)553.5 (32)513.4 (28)676.4 (30)463 (18)506 (17.7)
Ctrough, µg/mL192.5 (78)295 (56)255 (46)395 (44)0.91 (752)3.78 (282)
AUC, µg/mL*day8701 (51)11362 (41)10088 (35)10723 (37)8770 (38)13100 (26.7)

* Induction Cycle 6 of a 28-day cycle.

† Predicted steady state values following maintenance dosing every 6 months.

‡ Predicted steady state values

§ Induction Cycle 8 of a 21-day cycle.

SPL UNCLASSIFIED SECTION

Distribution and Elimination

SPL UNCLASSIFIED SECTION

CLL and NHL

The elimination of obinutuzumab is comprised of a linear clearance pathway and a time-dependent non-linear clearance pathway. As GAZYVA treatment progresses, the impact of the time-dependent pathway diminishes in a manner suggesting target-mediated drug disposition (TMDD) and saturation of the TMDD at the end of the treatment cycle at the proposed clinical dosing regimen. The distribution and elimination parameters of obinutuzumab in patients with CLL and NHL are provided in Table 17.

Table 17 Distribution and Elimination Parameters of Obinutuzumab
CLLNHL
Parameters are presented as geometric mean (% Coefficient of Variation).
Distribution
  Volume of Distribution*, L4.1 (20)4.3 (21)
Elimination
  Terminal Half-life, days25.5 (48)35.3 (35)
  Clearance, L/day0.11 (53)0.08 (41)

* At steady state.

SPL UNCLASSIFIED SECTION

LN and Childhood-Onset INS

The steady state clearance of obinutuzumab in LN and childhood-onset INS was approximately 0.13 and 0.058 L/day, respectively, with a terminal elimination t1/2 of 22.4 and 29.5 days, respectively.

GAZYVA elimination comprises two parallel pathways, a linear clearance pathway and a non-linear clearance pathway, which changes as a function of time. The time-varying clearance decreases with time with an exponential decay coefficient, likely related to CD20 target reduction and proteinuria improvement over time in patients with elevated baseline proteinuria, and a time-independent clearance related to the endogenous catabolic processes of IgG.

SPL UNCLASSIFIED SECTION

Specific Populations

SPL UNCLASSIFIED SECTION

CLL and NHL

Age (median [range]: 63 [22, 89] years) and baseline creatinine clearance (CLcr) (median [range] 84 [22, > 120] mL/min) did not affect the pharmacokinetics of GAZYVA. In patients with CLcr ≤ 30 mL/min, the pharmacokinetics of GAZYVA was unaffected. GAZYVA has not been studied in patients with hepatic impairment.

The volume of distribution and steady-state clearance increased with body weight; however, the expected change in exposure does not warrant a dosage modification.

SPL UNCLASSIFIED SECTION

LN and Childhood-Onset INS

The population pharmacokinetic analysis of GAZYVA did not identify CLcr (median [range] 108 [28.9 - 282 mL/min] in LN and 136 [62.3 - 346 mL/min] in childhood-onset INS) as a significant covariate on the pharmacokinetics of patients with LN or childhood-onset INS. The pharmacokinetics of obinutuzumab in patients with mild or moderate renal impairment were similar to those in patients with normal kidney function. The safety and efficacy of GAZYVA in patients with severe renal impairment has not been formally studied.

12.6 Immunogenicity

IMMUNOGENICITY

As with all therapeutic proteins, there is potential for immunogenicity. The detection of antibody formation is highly dependent on the sensitivity and specificity of the assay. Additionally, the observed incidence of anti-drug antibody (ADA) (including neutralizing antibody) positivity in an assay may be influenced by several factors including assay methodology, sample handling, timing of sample collection, concomitant medications, and underlying disease. For these reasons, comparison of the incidence of anti-drug antibodies in the studies described below with the incidence of anti-drug antibodies in other studies or to other products may be misleading.

Seven percent (18/271) of patients with CLL tested positive for anti-GAZYVA antibodies at one or more time points in CLL11. No patients developed anti-GAZYVA antibodies during or following GAZYVA treatment in GADOLIN, while 1 patient (1/564, 0.2%) developed anti-GAZYVA antibodies in GALLIUM. Neutralizing activity of anti-GAZYVA antibodies was not assessed.

In GAZYVA-treated patients in the LN studies, a total of 12 out of 200 (6%) had at least one ADA-positive sample recorded at any time during the studies. Six (3%) subjects had ADA-positive samples recorded at baseline in which two patients remained ADA-positive throughout the studies, one patient had a single post-baseline sample that was ADA-positive, and three patients had post-baseline samples that were all ADA-negative. Six (3%) patients with ADA-negative samples at baseline had a positive ADA titer post-baseline (treatment-induced ADA). None of the 12 patients with positive ADA titers at any time during the treatment period experienced an IRR or hypersensitivity reaction during the studies. Neutralizing activity of anti-GAZYVA antibodies was not assessed.

Because of the low occurrence of anti-drug antibodies in these studies, the effect of these antibodies on the pharmacokinetics, pharmacodynamics, safety and/or effectiveness of GAZYVA is unknown.

There is insufficient information to characterize the anti-GAZYVA antibody response in patients with childhood-onset INS.

13 NONCLINICAL TOXICOLOGY

NONCLINICAL TOXICOLOGY SECTION

13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility

CARCINOGENESIS & MUTAGENESIS & IMPAIRMENT OF FERTILITY SECTION

No carcinogenicity or genotoxicity studies have been conducted with obinutuzumab.

No specific studies have been conducted to evaluate potential effects on fertility; however, no adverse effects on male or female reproductive organs were observed in the 26-week repeat-dose toxicity study in cynomolgus monkeys.

14 CLINICAL STUDIES

CLINICAL STUDIES SECTION

14.1 Chronic Lymphocytic Leukemia

SPL UNCLASSIFIED SECTION

The efficacy of GAZYVA was evaluated in a three-arm, open-label, active-controlled, randomized, multicenter trial (CLL11; NCT01010061) in 781 patients with previously untreated CD20+ CLL requiring treatment who had coexisting medical conditions or reduced renal function as measured by creatinine clearance (CLcr) < 70 mL/min. Patients with CLcr < 30 mL/min, active infections, positive hepatitis B (HBsAg or anti-HBc positive; patients positive for anti-HBc could be included if hepatitis B viral DNA was not detectable) and hepatitis C serology, or immunization with live virus vaccine within 28 days prior to randomization were excluded from the trial. Patients were treated with chlorambucil control (Arm 1), GAZYVA in combination with chlorambucil (Arm 2), or rituximab product in combination with chlorambucil (Arm 3). The safety and efficacy of GAZYVA was evaluated in a Stage 1 comparison of Arm 1 vs. Arm 2 in 356 patients and a Stage 2 comparison of Arm 2 vs. Arm 3 in 663 patients.

The majority of patients received 1,000 mg of GAZYVA on days 1, 8 and 15 of the first cycle, followed by treatment on the first day of 5 subsequent cycles (total of 6 cycles, 28 days each). The first dose of GAZYVA was divided between day 1 (100 mg) and day 2 (900 mg) [see Dosage and Administration (2.2)], which was implemented in 140 patients. Chlorambucil was given orally at 0.5 mg/kg on day 1 and day 15 of all treatment cycles (1 to 6).

In CLL11, the median age was 73 years, 62% were male, and 95% were White. Sixty-five percent had a CLcr < 70 mL/min and 76% had multiple coexisting medical conditions. Twenty-two percent of patients were Binet stage A, 42% were stage B, and 36% were stage C. The median estimated CLcr was 62 mL/min. Eighty-one percent of patients treated with GAZYVA in combination with chlorambucil received all 6 cycles compared to 89% of patients in the rituximab product treated arm and 67% in the chlorambucil alone arm.

In the Stage 1 analysis of CLL11, the median progression-free survival (PFS) in the GAZYVA in combination with chlorambucil arm was 27.2 months and 11.2 months in the chlorambucil alone arm (median observation time 22.8 months) as assessed by independent review and is consistent with investigator-assessed PFS. The median overall survival (OS) was not yet reached with a total of 46 deaths: 22 (9%) in the GAZYVA in combination with chlorambucil arm and 24 (20%) in the chlorambucil arm. The hazard ratio for OS was 0.41 (95% CI: 0.23-0.74).

In the Stage 2 analysis of CLL11, the median PFS was 26.7 months in the GAZYVA arm and 14.9 months in the rituximab product arm with a median observation time of 18.7 months (HR: 0.42, 95% CI: 0.33-0.54, p-value < 0.0001). These results were assessed by independent review and are consistent with investigator-assessed PFS. Minimal residual disease (MRD) was evaluated using allele-specific oligonucleotide polymerase chain reaction (ASO-PCR). The cutoff for a negative status was one CLL cell per 104 leukocytes in the sample (i.e., an MRD value of < 10-4 was considered negative). Among patients who achieved complete response (CR) and complete response with incomplete marrow recovery (CRi; 94 patients in the GAZYVA arm and 34 patients in the rituximab product arm), 18 patients (19%) had negative MRD in the bone marrow in the GAZYVA arm compared to 2 patients (6%) in the rituximab product arm. Out of the patients who achieved CR and CRi, 39 patients (41%) in the GAZYVA arm, and 4 patients (12%) in the rituximab product arm were MRD negative in peripheral blood samples collected at least 3 months after the end of treatment.

Efficacy results are shown in Table 18 and Figures 1 and 2.

Table 18 Efficacy Results from CLL11
EndpointStage 1 of CLL11Stage 2 of CLL11
GAZYVA + Chlorambucil* ChlorambucilGAZYVA + Chlorambucil* Rituximab product + Chlorambucil
n = 238n = 118n = 333n = 330
Median Progression-Free Survival† 27.2 months11.2 months26.7 months14.9 months
(HR 0.19 [0.14; 0.27], p-value < 0.0001 stratified log-rank test)(HR 0.42 [0.33; 0.54], p-value < 0.0001 stratified log-rank test)
Overall Response Rate‡ 78.2%33.1%79.6%66.3%
  Complete Response28.2%026.1%8.8%
  Complete Response with Incomplete Marrow Recovery2.5%1.7%2.1%1.5%
  Partial Response45.0%30.5%48.6%54.1%
  Nodular Partial Response2.5%0.8%2.7%1.8%
Median Duration of Response22.4 months4.7 months19.6 months9.7 months
Overall SurvivalHR 0.41 [0.23; 0.74]Not Yet Mature

* All Stage 1 GClb patients (n = 238) were included in the Stage 2 GClb population (n = 333).

† As defined by independent review. Investigator-assessed PFS was consistent with data from independent review.

‡ Defined as best overall response rate (ORR = CR + CRi + PR + nPR).

Figure 1
Kaplan-Meier Curve of Overall Survival in Patients with CLL in CLL11 (Stage 1)
Figure 1Figure 1
Figure 2
Kaplan-Meier Curve of Progression-Free Survival in Patients with CLL in CLL11 (Stage 2)
Figure 2Figure 2

14.2 Follicular Lymphoma

SPL UNCLASSIFIED SECTION

SPL UNCLASSIFIED SECTION

GADOLIN

The efficacy of GAZYVA was evaluated in GADOLIN (NCT01059630), an open-label, multicenter, randomized study that included 335 patients with follicular lymphoma (FL) who had no response to or have progressed during or within 6 months of rituximab product or a rituximab product-containing regimen. These patients were randomized to receive either bendamustine alone (n = 171) or GAZYVA in combination with bendamustine (n = 164) for 6 cycles, each of 28 days duration. Patients in the GAZYVA plus bendamustine arm who did not have disease progression [patients with a complete response (CR), partial response (PR) or stable disease (SD)] at the end of the 6 cycles continued receiving GAZYVA monotherapy for 2 years. Patients were stratified according to the type of refractoriness to rituximab product (refractory to rituximab product monotherapy versus rituximab product in combination with chemotherapy), the number of prior therapies (≤ 2 versus > 2), and geographic region.

GAZYVA was given by intravenous infusion as a flat dose of 1,000 mg on Days 1, 8 and 15 of Cycle 1, on Day 1 of Cycles 2–6, and then every 2 months until disease progression for up to 2 years. Bendamustine was given intravenously on Days 1 and 2 for all treatment cycles (1–6) at 90 mg/m2/day when given in combination with GAZYVA or 120 mg/m2/day when given alone.

The primary analysis included 321 FL patients, including 166 patients randomized to bendamustine alone and 155 patients randomized to GAZYVA in combination with bendamustine. In the primary analysis, patients had a median age of 63 years, 88% were White and 56% were male. Thirty-four percent had bulky disease (> 6 cm), 15% had at least one B-symptom at baseline and 95% had an ECOG performance status of 0–1 at baseline. The median time since initial diagnosis was 3 years and the median number of prior therapies was 2 (range 1 to 10). Forty-six percent of patients received 1 prior therapy and 33% of patients received 2 prior therapies. Twenty percent of patients were refractory to prior rituximab product monotherapy, 37% of patients were refractory to prior rituximab product plus chemotherapy induction treatment, and 41% of patients were refractory to rituximab product maintenance treatment received following rituximab product plus chemotherapy induction. Seventy-nine percent of patients were refractory to both rituximab product and an alkylating agent during any prior regimen (double refractory).

The major efficacy outcome measure was PFS as determined by an independent review committee (IRC). At the time of the primary analysis, median observation time was 21.1 months. The median PFS in the bendamustine arm was 13.8 months. Median PFS was not reached in the GAZYVA plus bendamustine arm (PFS HR = 0.48, 95% CI: 0.34-0.68; stratified log-rank test p-value < 0.0001). The investigator assessed PFS result was consistent with the IRC-assessed PFS. The median investigator-assessed PFS in the bendamustine arm was 13.7 months and the median in the GAZYVA containing arm was 29.2 months (PFS HR = 0.48, 95% CI: 0.35-0.67; stratified log-rank test p-value < 0.0001).

Efficacy results are summarized in Table 19. The Kaplan-Meier curve for IRC-PFS is shown in Figure 3.

Table 19 Primary Analysis Efficacy Results from GADOLIN* , †
EndpointGADOLIN
GAZYVA + Bendamustine followed by GAZYVA monotherapy
n = 155
Bendamustine
n = 166
Median Progression-Free Survival (months)Not Reached13.8
(HR = 0.48 [0.34; 0.68], p-value < 0.0001 by stratified log-rank test)
Best Overall Response‡ 78.7%74.7%
  Complete Response15.5%18.7%
  Partial Response63.2%56.0%
Median duration of response (months)Not Reached11.6

* Based on FL population.

† As defined by independent review.

‡ Best response of PR or CR within 12 months of study start.

Figure 3
Kaplan-Meier Curve of IRC-Assessed Progression-Free Survival in Patients with FL
Figure 3Figure 3

The final analysis included a total of 335 patients with 171 randomized to bendamustine alone and 164 to GAZYVA in combination with bendamustine. With an overall median observation time of 52.2 months (range: 0-100.9 months), there were 66 deaths (40.2%) in the GAZYVA arm and 85 deaths (51.3%) in the bendamustine-alone arm (OS HR = 0.71, 95% CI: 0.51, 0.98). The Kaplan-Meier curve for OS is presented in Figure 4.

Figure 4
Kaplan-Meier Curve of Overall Survival in Patients with FL
Figure 4Figure 4
SPL UNCLASSIFIED SECTION

GALLIUM

The efficacy of GAZYVA was evaluated in GALLIUM (NCT01332968), a multicenter, open-label, randomized study that included 1202 patients with previously untreated, stage II bulky, III or IV FL. Patients were randomized 1:1 to receive either GAZYVA (n = 601) or rituximab product (n = 601) in combination with chemotherapy (CHOP, CVP, or bendamustine) for 6–8 cycles. Patients were stratified by chemotherapy (selected by each site; all patients at that site received the chosen chemotherapy regimen), FLIPI (Follicular Lymphoma International Prognostic Index) risk group and geographic region. Patients with at least PR to combination therapy received monotherapy with GAZYVA (1,000 mg) or rituximab product every two months until disease progression or for a maximum of two years. The study excluded patients with follicular lymphoma grade 3b or transformed disease; patients having an ANC < 1500 / µL, platelets < 75,000 / µL, or CLcr < 40 mL/min; and patients with hepatic transaminases > 2.5 × upper limit of normal unless attributable to lymphoma.

GAZYVA was given by intravenous infusion as a flat dose of 1,000 mg on Days 1, 8 and 15 of Cycle 1 and Day 1 of subsequent treatment cycles.

GAZYVA and bendamustine were given in six 28-day cycles. Bendamustine was administered at 90 mg/m2/day on Days 1 and 2 of each cycle, with prednisone 100 mg orally or equivalent on Day 1 of Cycle 1.

GAZYVA and CHOP were given in six 21-day cycles. Subsequently, two additional cycles of GAZYVA were given for a total of 8 GAZYVA cycles. CHOP consisted of cyclophosphamide 750 mg/m2 intravenously, doxorubicin 50 mg/m2, and vincristine 1.4 mg/m2 (maximum dose, 2 mg) on Day 1 and prednisone 100 mg orally on Days 1-5.

GAZYVA and CVP were given in eight 21-day cycles. CVP consisted of cyclophosphamide 750 mg/m2 intravenously and vincristine 1.4 mg/m2 (maximum dose, 2 mg) on Day 1 and prednisone 100 mg orally on Days 1-5.

Patients had a median age of 59 years, 81% were White and 53% were female; 7% had Stage II, 35% had Stage III, and 56% had Stage IV disease, with 44% having bulky disease (≥ 7 cm) overall; 79% had a FLIPI score of > 2; and 97% had an ECOG performance status of 0–1. The chemotherapy was bendamustine in 57%, CHOP in 33%, and CVP in 10% of patients.

Efficacy was based on PFS per IRC, with a median observation time of 38 months. Upon interim analysis, the risk of progression or death was significantly reduced in the GAZYVA containing arm compared to the rituximab product containing arm (Table 20). Kaplan-Meier curves for PFS are shown in Figure 5. Overall response and complete remission rates were similar.

Table 20 Efficacy in Previously Untreated Follicular Lymphoma (GALLIUM)
Endpoint per IRCGAZYVA + chemotherapy followed by GAZYVA monotherapy
n = 601
Rituximab product + chemotherapy followed by rituximab product monotherapy
n = 601
Progression-Free Survival *
  Number of events (%)
108 (18%)141 (23%)
HR = 0.72 [95% CI: 0.56, 0.93], p-value = 0.0118 †
Overall Response Rate ‡ 91%88%
Complete Remission Rate ‡ 28%27%

* Investigator-assessed PFS was consistent with data from independent review.

† Stratified log-rank test.

‡ After completion of combination therapy. Assessed by CT without positron emission tomography.

Figure 5
Kaplan-Meier Curves of Progression Free Survival in Patients with Previously Untreated FL

Figure 5Figure 5

14.3 Active Lupus Nephritis

SPL UNCLASSIFIED SECTION

SPL UNCLASSIFIED SECTION

Study Design and Population

The efficacy of GAZYVA was evaluated in REGENCY (NCT04221477), a Phase III, randomized, double-blind, placebo-controlled, parallel-group, multicenter study in 271 patients with ISN/RPS 2003 Class III or IV, with or without concomitant Class V lupus nephritis (LN), treated with standard therapy consisting of mycophenolate mofetil (MMF) and corticosteroids. Patients had active or active/chronic ISN/RPS 2003 Class III or IV, with or without concomitant Class V proliferative LN determined by kidney biopsy, current or past positive antinuclear antibody (ANA), urine protein-to-creatinine ratio (UPCR) ≥ 1 g/g, and had received at least one dose of pulse intravenous (IV) methylprednisolone (≥ 250 mg) or equivalent treatment for LN during the 6 months prior to screening or during screening.

Patients with estimated glomerular filtration rate (eGFR) <30 ml/min/1.73 m2 or in need of dialysis or transplantation, with sclerosis in > 50% of glomeruli on kidney biopsy, presence of rapidly progressive glomerulonephritis, evidence of active infection, receipt of anti-CD20 therapy < 9 months before or during screening, or receipt of cyclophosphamide, tacrolimus, ciclosporin, or voclosporin within 2 months of or during screening were excluded.

Patients were randomized 1:1 to receive GAZYVA 1,000 mg (N=135) or placebo (N=136) intravenously, in combination with MMF 2-2.5 g/day and a tapering course of corticosteroids and were evaluated over 76 weeks. Patients randomized to receive GAZYVA were further randomized in a 1:1 ratio to receive either GAZYVA 1,000 mg IV on Day 1, Weeks 2, 24, 26, 50, and 52 (Arm 1), or GAZYVA 1,000 mg IV on Day 1, Weeks 2, 24, 26, and 52 (Arm 2). The totality of the GAZYVA efficacy data combining both treatment arms is shown in Table 21.

All patients received oral prednisone 0.5 mg/kg/day (maximum 60 mg/day) and remained at this dose until Week 2. Beginning on Day 15, prednisone was tapered to achieve a target dose of 5 mg/day by Week 24. Prednisone was maintained at a low dose (5 mg/day) from Week 24 until Week 80.

The median age of patients was 31 years, 85% were female, 58% were Hispanic or Latino, 48% were White, 19% were American Indian or Alaska Native, 15% were Black or African American and 6% were Asian. The distribution by kidney biopsy class was 39% Class III, 61% Class IV and 31% had concomitant Class V. Mean (SD) eGFR at baseline 102.3 (±30.8) mL/min/1.73 m2. Mean (SD) UPCR at baseline was 3.3 (±2.9) mg/mg with 42% of patients exhibiting UPCR ≥3 mg/mg at baseline.

SPL UNCLASSIFIED SECTION

Efficacy Results

The primary endpoint measure was proportion of patients who achieved complete renal response (CRR) at Week 76, defined as meeting all of the following criteria: UPCR < 0.5 g/g; eGFR ≥ 85% of baseline, as calculated using the 2009 Chronic Kidney Disease Epidemiology Collaboration (CKD-EPI) equation; with no occurrence of the following intercurrent events: rescue therapy, treatment failure, death or early study withdrawal.

Key secondary endpoint measures included: proportion of patients who achieved CRR with successful prednisone taper at Week 76 (defined as achievement of CRR at Week 76 without receiving prednisone > 7.5 mg/day or equivalent from Week 64 through Week 76), proportion of patients who achieved a proteinuric response at Week 76 (defined as achievement of UPCR < 0.8g/g and no occurrence of the following intercurrent events: rescue therapy, treatment failure, death or early study withdrawal) and proportion of patients who experience "renal-related events or deaths" through Week 76 (defined as occurrence of death, treatment failure, ≥ 50% increase in UPCR to a value ≥ 3 g/g and/or ≥ 30% decrease in eGFR to < 60 ml/min/1.73 m2).

The proportion of patients achieving CRR at Week 76 was significantly greater in patients treated with GAZYVA in combination with standard therapy compared to patients who received placebo plus standard therapy. There were also a higher proportion of patients who achieved CRR with successful prednisone taper at Week 76 and proteinuric response at Week 76 in the GAZYVA plus standard therapy arm compared to the placebo plus standard therapy arm (see Table 21).

In the REGENCY study, patients who received GAZYVA were less likely to experience the outcome of "renal-related event or death" compared with placebo. Fewer patients in the GAZYVA arm experienced worsening kidney function or doubling of serum creatinine (see Table 22).

Table 21 Summary of Efficacy Results in Adult Patients with Active Lupus Nephritis (REGENCY Study)
GAZYVA + standard therapy
(N=135)
Placebo + standard therapy
(N=136)
Primary Endpoint
Complete renal response (CRR) at Week 76 (%)46.4 (38.0, 54.9)33.1 (25.2, 41)
   Treatment difference (95% CI)* 13.4 (2.0, 24.8)
   p-value0.0232
   Components of CRR:
     UPCR < 0.5 g/g 64 (47.4%)49 (36.0%)
     eGFR ≥ 85% at baseline113 (83.7%)103 (75.7%)
     No occurrence of intercurrent events120 (88.9%)102 (75%)
Key Secondary Endpoints
CRR with successful prednisone taper at Week 76 (%)42.7 (34.3, 51.1)30.9 (23.1, 38.7)
   Treatment difference (95% CI)11.9 (0.6, 23.2)
   p-value0.0421
Proteinuric response at Week 76 (%)55.5 (47.1, 64)41.9 (33.6, 50.2)
   Treatment difference (95% CI)13.7 (2.0, 25.4),
   p-value0.0227

* Primary and key secondary endpoints were analyzed using the Cochran-Mantel-Haenszel (CMH) test, adjusted for stratification factors race and region. Multiple Imputation handled missing data. For the primary endpoint CRR and the key secondary endpoint CRR with successful prednisone taper, missing data (not due to an Intercurrent Event (ICE)) occurred in four patients in the GAZYVA arm and one in the placebo arm. For the key secondary endpoint proteinuric response, four GAZYVA patients and two placebo patients had non-ICE-related missing data.

Table 22 Renal-Related Event or Death in Adult Patients with Active Lupus Nephritis (REGENCY Study) by Week 76
Week 0-76Hazard Ratio (HR) vs. Placebo (95% CI)
Week 76
GAZYVA + standard therapy
N=135 (%)
Placebo + standard therapy
N=136 (%)
Renal-Related Event or Death
Number (%) of patients with event24 (17.8%)46 (33.8%)
  Time to event0.5 (0.3, 0.8)
Components of Renal-Related Event or Death Endpoint
Percentage of patients with:
  Death3 (2.2%)1 (0.7%)
  Treatment failure* 6 (4.4%)25 (18.4%)
    End-stage renal disease (ESRD)1 02 (1.5%)
    Clinically significant, sustained worsening in UPCR and/or eGFR from Week 242 5 (3.7%)22(16.2%)
    Rescue Therapy except corticosteroid-only rescue3 5 (3.7%)22 (16.2%)
  Worsening proteinuria† 17 (12.6%)18 (13.2%)
  Worsening eGFR‡ 7 (5.2%)20 (14.7%)
Additional Renal-Related Events
Percentage of patients with event
  Doubling of serum creatinine from baseline through Week 764 (3.0%)8 (5.9%)

* Treatment failure was prospectively defined as any of the following: 1) new ESRD or need for chronic dialysis or renal transplantation, 2) clinically significant, sustained worsening in UPCR and/or eGFR from Week 24 onward that leads the investigator to conclude the patient failed the randomized treatment period, or 3) receipt of rescue therapy, except corticosteroid-only rescue.

† Worsening proteinuria was prospectively defined as a confirmed ≥ 50% increase in UPCR to a value ≥ 3 g/g.

‡ Worsening eGFR was prospectively defined as confirmed ≥ 30% decrease in eGFR to a value < 60mL/min/1.73m2.

SPL UNCLASSIFIED SECTION

Subgroup Analyses

In pre-specified subgroup efficacy analyses, the primary endpoint in patients was examined based on 24-hour UPCR at baseline (< 3 g/g or ≥ 3 g/g), lupus nephritis class at baseline (Class III or IV), and concomitant Class V at baseline. The results are displayed in Figure 6 below.

Figure 6
Forest Plot of CRR at Week 76 on Baseline Disease Characteristics, Efficacy-Evaluable Patients
Figure 6Figure 6

14.4 Childhood-Onset Idiopathic Nephrotic Syndrome

SPL UNCLASSIFIED SECTION

SPL UNCLASSIFIED SECTION

Study Design and Population

The efficacy and safety of GAZYVA were evaluated in INSHORE (NCT05627557), a Phase III, randomized, controlled, open-label, multicenter study in 85 patients 2 years of age and older with frequently relapsing or steroid dependent childhood-onset idiopathic nephrotic syndrome (INS).

Frequently relapsing nephrotic syndrome (FRNS) was defined as two or more relapses in the first 6 months after disease onset (or after remission of the initial episode) or three or more relapses per 12 months thereafter. Steroid dependent nephrotic syndrome (SDNS) was defined as two consecutive relapses while on prednisone or prednisolone or within 14-15 days of prednisone or prednisolone discontinuation.

Patients had to be diagnosed before the age of 18 years, have a normal estimated glomerular filtration rate (eGFR) for age, and be in complete remission at study entry, as defined by the absence of edema, a urine protein-to-creatinine ratio (UPCR) of 0.2 g/g or less at screening, and trace or negative urine dipstick on 3 consecutive days within a week prior to randomization. Patients had to have had at least one relapse in the 6 months before screening.

Patients were excluded if they had secondary, steroid resistant, or genetic causes of nephrotic syndrome, treatment failure while receiving mycophenolate mofetil (MMF) (2 or more relapses in a 6 month period), received immunosuppressive medications other than MMF or oral corticosteroids within 2 months prior to randomization, or received biologic B cell-depleting therapy within 9 months prior to baseline. Patients with an active infection, or history of severe allergic or anaphylactic reactions to monoclonal antibodies were also excluded.

A total of 85 patients were randomized 1:1 to intravenous GAZYVA 1,000 mg (or 20 mg/kg if weighing less than 45 kg) on Day 1, Day 15, Week 24, and Week 26, or oral MMF titrated to a target dose of 1200 mg/m2/day divided in two doses (maximum 2,000 mg/day) by Week 4. Patients receiving GAZYVA received premedication with methylprednisolone 80 mg IV (or 1.5 mg/kg if less than 45 kg), acetaminophen/paracetamol 15 mg/kg orally (PO) (maximum dose 1,000 mg) and diphenhydramine 0.5 to 1 mg/kg (maximum dose 50 mg) orally or intravenous equivalent.

Patients who were receiving oral prednisone (or prednisolone equivalent) at randomization were tapered off steroids by Weeks 4−6 (and no later than Week 8) and were to remain off steroids to Week 52.

At baseline, the median age of patients was 9 years (range 2 to 22 years), 64% were 2 years to less than 12 years of age, 65% were male, median disease duration was 46 months, 25% were Hispanic or Latino, 27 % were Asian, 14% were Black or African American, and 55% were White. The mean eGFR was 171 mL/min/1.73 m2, mean UPCR was 0.05 g/g, 45% had FRNS, and 55% had SDNS.

A total of 75% had received prior immunosuppressive therapy other than steroids for INS and 85% were receiving glucocorticoids at baseline. Of the 85 patients, 1 (2%) in the GAZYVA arm and 9 (22%) in the MMF arm discontinued their randomized treatment during the 52-week treatment period.

The primary endpoint was the proportion of patients who did not relapse after Week 8 and were in complete remission at one year, defined as first morning void UPCR ≤ 0.2 g/g at Week 52. Relapse was defined as any of the following: (1) UPCR ≥ 2 g/g, or (2) 3 consecutive daily (home-monitoring) urine dipstick readings of 3+ proteinuria and UPCR > 0.2 g/g in the last of those three urines, or (3) urine dipstick reading of 3+ proteinuria on any single day accompanied by edema and most recent UPCR > 0.2 g/g. In addition, patients were non-responders if they had (1) used systemic corticosteroids for > 14 days in a 30 day period (after Week 8), (2) initiated rescue therapy other than systemic corticosteroids prior to 52 weeks, (3) died prior to 52 weeks, (4) missing UPCR assessments at Week 52.

SPL UNCLASSIFIED SECTION

Efficacy Results

The proportion of patients who did not relapse after Week 8 and were in complete remission at Week 52 was significantly greater (95%) in the GAZYVA as compared to the MMF arm (73%) (see Table 23). Key secondary outcome measures are shown in Table 23.

Table 23 Summary of Efficacy in Patients with Childhood-Onset Idiopathic Nephrotic Syndrome (INSHORE study)
GAZYVA
(N=44)
MMF
(N=41)
CI: confidence interval; PY: patient years; UPCR: urine protein to creatinine ratio; INS, idiopathic nephrotic syndrome.
Primary endpoint
Proportion without relapse* , † after Week 8 and were in complete remission at Week 52, number of patients (%)42 (95%)30 (73%)
Adjusted difference (95% CI)22 (6, 38)
p-value0.004
Components of Primary Endpoint, n (%)
  UPCR of 0.2 or less at Week 5243 (98%)40 (98%)
  No relapsea after week 844 (100%)32 (78%)
  No systemic corticosteroids use† after Week 843 (98%)30 (73%)
  No use of rescue medication for INS† (other than systemic corticosteroids) prior to week 5244 (100%)32 (78%)
Key secondary endpoints
Number of patients with first relapse*,‡ (event rate per 100 PY)4 (7)15 (33)
Hazard ratio (95% CI)0.25 (0.08, 0.75)
p-value0.007
Total number of relapses* from randomization to Week 52424
Adjusted rate ratio (95% CI)0.16 (0.05, 0.44)
p-value0.0005

* Relapse was defined as any of the following (1) UPCR of 2 g/g or more, or (2) 3 consecutive daily (home-monitoring) urine dipstick readings of 3+ proteinuria and most recent UPCR greater than 0.2 g/g, or (3) urine dipstick reading of 3+ proteinuria on any single day accompanied by edema and most recent UPCR greater than 0.2 g/g.

† Patients were non-responders if they had used systemic corticosteroids for > 14 days in a 30-day period after Week 8, or initiated rescue therapy for INS other than systemic corticosteroids prior to 52 weeks.

‡ Based on all relapse events until the clinical cutoff date (when the last patient completed the Week 52 study visit).
Hazard ratio, 95% confidence intervals, and p-value are derived from the pre-specified time-to-event analysis using Cox regression considering all relapse events until the clinical cutoff date (when the last patient completed the Week 52 study visit).

16 HOW SUPPLIED/STORAGE AND HANDLING

HOW SUPPLIED SECTION

GAZYVA (obinutuzumab) injection is a clear, colorless to slightly brown, preservative-free solution for intravenous use supplied as 1,000 mg/40 mL (25 mg/mL) in single-dose vials (NDC 50242-070-01).

STORAGE AND HANDLING SECTION

Store at 2°C to 8°C (36°F to 46°F). Do not use beyond expiration date stamped on carton. Protect from light. DO NOT FREEZE. DO NOT SHAKE.

17 PATIENT COUNSELING INFORMATION

INFORMATION FOR PATIENTS SECTION

SPL UNCLASSIFIED SECTION

Hepatitis B Virus Reactivation

Advise patients to seek immediate medical attention if symptoms of hepatitis occur [see Warnings and Precautions (5.1)]. Advise patients of the need for hepatitis B virus screening and monitoring during treatment with GAZYVA.

SPL UNCLASSIFIED SECTION

Progressive Multifocal Leukoencephalopathy

Advise patients to seek immediate medical attention if new or changes in neurological symptoms occur [see Warnings and Precautions (5.2)].

SPL UNCLASSIFIED SECTION

Neutropenia, Thrombocytopenia and Disseminated Intravascular Coagulation

Advise patients to seek immediate medical attention if signs and symptoms of bleeding or thrombosis occur. Advise patients of the need for periodic monitoring of blood counts [see Warnings and Precautions (5.7, 5.8 and 5.9) and Adverse Reactions (6.1 and 6.2)].

SPL UNCLASSIFIED SECTION

Contraception

Advise females of reproductive potential to use effective contraception during treatment with GAZYVA and for 6 months after the last dose [see Use in Specific Populations (8.3)].

SPL UNCLASSIFIED SECTION

Lactation

Advise women not to breastfeed during treatment with GAZYVA and for 6 months after the last dose [see Use in Specific Populations (8.2)].

SPL UNCLASSIFIED SECTION

GAZYVA® (obinutuzumab)

Manufactured by:
Genentech, Inc.
A Member of the Roche Group
1 DNA Way
South San Francisco, CA 94080-4990
U.S. License No. 1048

GAZYVA is a registered trademark of Genentech, Inc.
© 2026 Genentech, Inc.

PRINCIPAL DISPLAY PANEL - 40 mL Vial Carton

PACKAGE LABEL.PRINCIPAL DISPLAY PANEL

NDC 50242-070-01

Gazyva®
(obinutuzumab)
Injection

1000 mg/40 mL
(25 mg/mL)

For Intravenous Infusion After Dilution.
Single-Dose Vial. Discard Unused Portion.
No preservative.

1 vial

Rx only

Genentech

10240530

Principal Display Panel - 40 mL Vial Carton
Principal Display Panel - 40 mL Vial Carton

DailyMed Product Concepts#

Product concept, Relation, Version table
Product conceptRelationVersionEffective
de75ec12-37b7-4fae-9b84-cafcfe64b2e8Product name120151014
0ca1d589-929b-4b33-bc5b-1d84abdafa6aProduct name120150324
fc363c46-397b-4476-ac0f-70e43e8e4592Product name120150324

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Package NDC, Billing unit, Product NDC table
Package NDCBilling unitProduct NDCDailyMed indexing SPLSPL versionEffective
50242-070-01ML - Milliliter50242-0701cea55db-6dcf-42e2-8138-c82199d4e73f12013-12-02

DailyMed Socrata Ingredients#

Ingredient, Type, UNII table
IngredientTypeUNIISPL versionUploaded
OBINUTUZUMABACTIVE INGREDIENTO43472U9X87
OBINUTUZUMABACTIVE MOIETYO43472U9X87
HISTIDINEINACTIVE INGREDIENT4QD397987E7
HISTIDINE MONOHYDROCHLORIDE MONOHYDRATEINACTIVE INGREDIENTX573657P6P7
POLOXAMER 188INACTIVE INGREDIENTLQA7B6G8JG7
TREHALOSE DIHYDRATEINACTIVE INGREDIENT7YIN7J07X47
WATERINACTIVE INGREDIENT059QF0KO0R7

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Product NDCPackage NDC
50242-07050242-070-01, 50242-070-86

Purple Book Biologic Products#

BLA, Proprietary name, Proper name table
BLAProprietary nameProper nameLicense typeStatusLatest source
125486Gazyvaobinutuzumab351(a)Rx2026-09-01

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VersionEffective dateSourceHydrated
222025-12-19full-release2026-05-31 21:52:25
212025-11-04monthly-update2026-06-03 17:43:04
192023-08-23full-release2026-05-31 20:52:32

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DailyMed ingredient, IID ingredient, UNII table
DailyMed ingredientIID ingredientUNIIDosage form / routePotencyMaximum daily exposureMatch
POLOXAMER 188POLOXAMER 188LQA7B6G8JGINJECTION / INTRAVENOUS6 mgExact identifier — unii+route
6 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTION, SUSPENSION, LIPOSOMAL / INTRAVENOUS0.16 %w/vExact identifier — unii+route
12 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTION, SUSPENSION, LIPOSOMAL / INTRAVENOUS0.16 %w/vExact identifier — unii+route
12 equally ranked IID candidates
POLOXAMER 188POLOXAMER 188LQA7B6G8JGINJECTION / INTRAVENOUS6 mgExact identifier — unii+route
6 equally ranked IID candidates
POLOXAMER 188POLOXAMER 188LQA7B6G8JGINJECTION / INTRAVENOUS6 mgExact identifier — unii+route
6 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTION, SOLUTION / INTRAVENOUS0.09 %w/vExact identifier — unii+route
12 equally ranked IID candidates
POLOXAMER 188POLOXAMER 188LQA7B6G8JGINJECTION, POWDER, FOR SOLUTION / INTRAVENOUS2.2 mgExact identifier — unii+route
6 equally ranked IID candidates
TREHALOSE DIHYDRATETREHALOSE DIHYDRATE7YIN7J07X4INJECTION, POWDER, FOR SOLUTION / SUBCUTANEOUS4 mgExact identifier — unii candidate
9 equally ranked IID candidates
TREHALOSE DIHYDRATETREHALOSE DIHYDRATE7YIN7J07X4INJECTION, POWDER, FOR SOLUTION / INTRADERMAL4 mgExact identifier — unii candidate
9 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTION, SOLUTION / INTRAVENOUS0.09 %w/vExact identifier — unii+route
12 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTION / INTRAVENOUS465 mgExact identifier — unii+route
12 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTION / INTRAVENOUS465 mgExact identifier — unii+route
12 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTION, SUSPENSION, LIPOSOMAL / INTRAVENOUS0.16 %w/vExact identifier — unii+route
12 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTION, SOLUTION / INTRAVENOUS0.09 %w/vExact identifier — unii+route
12 equally ranked IID candidates
TREHALOSE DIHYDRATETREHALOSE DIHYDRATE7YIN7J07X4INJECTION, POWDER, FOR SOLUTION / INTRADERMAL4 mgExact identifier — unii candidate
9 equally ranked IID candidates
POLOXAMER 188POLOXAMER 188LQA7B6G8JGINJECTION, POWDER, FOR SOLUTION / INTRAVENOUS2.2 mgExact identifier — unii+route
6 equally ranked IID candidates
TREHALOSE DIHYDRATETREHALOSE DIHYDRATE7YIN7J07X4INJECTION, POWDER, FOR SOLUTION / SUBCUTANEOUS4 mgExact identifier — unii candidate
9 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTABLE, LIPOSOMAL / INTRAVENOUS63 mgExact identifier — unii+route
12 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTION / INTRAVENOUS465 mgExact identifier — unii+route
12 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTABLE, LIPOSOMAL / INTRAVENOUS63 mgExact identifier — unii+route
12 equally ranked IID candidates
TREHALOSE DIHYDRATETREHALOSE DIHYDRATE7YIN7J07X4INJECTION, SOLUTION / SUBCUTANEOUS22 mgExact identifier — unii candidate
9 equally ranked IID candidates
POLOXAMER 188POLOXAMER 188LQA7B6G8JGINJECTION, POWDER, FOR SOLUTION / INTRAVENOUS2.2 mgExact identifier — unii+route
6 equally ranked IID candidates
TREHALOSE DIHYDRATETREHALOSE DIHYDRATE7YIN7J07X4INJECTION, SOLUTION / SUBCUTANEOUS22 mgExact identifier — unii candidate
9 equally ranked IID candidates
TREHALOSE DIHYDRATETREHALOSE DIHYDRATE7YIN7J07X4INJECTION, SOLUTION / SUBCUTANEOUS22 mgExact identifier — unii candidate
9 equally ranked IID candidates
TREHALOSE DIHYDRATETREHALOSE DIHYDRATE7YIN7J07X4INJECTION, POWDER, FOR SOLUTION / SUBCUTANEOUS4 mgExact identifier — unii candidate
9 equally ranked IID candidates
HISTIDINEHISTIDINE4QD397987EINJECTABLE, LIPOSOMAL / INTRAVENOUS63 mgExact identifier — unii+route
12 equally ranked IID candidates
TREHALOSE DIHYDRATETREHALOSE DIHYDRATE7YIN7J07X4INJECTION, POWDER, FOR SOLUTION / INTRADERMAL4 mgExact identifier — unii candidate
9 equally ranked IID candidates

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Brand, Generic, Manufacturer table
BrandGenericManufacturerSPL set IDEffective dateAvailable safety fieldsJoin
GazyvaOBINUTUZUMABGenentech, Inc.df12ceb2-5b4b-4ab5-a317-2a36bf2a3cda2025-12-19Boxed warning, Warnings, Adverse reactionsExact identifier
ndc (package): 50242-070-01
ndc (package): 50242-070-86
ndc (product): 50242-070
ndc11 (package): 50242007086
ndc11 (package): 50242007001
spl set id: df12ceb2-5b4b-4ab5-a317-2a36bf2a3cda

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