Rhopressa

RHOPRESSA is indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension.

The recommended dosage is one drop in the affected eye(s) once daily in the evening.

If one dose is missed, treatment should continue with the next dose in the evening. Twice a day dosing is not well tolerated and is not recommended. If RHOPRESSA is to be used concomitantly with other topical ophthalmic drug products to lower IOP, administer each drug product at least 5 minutes apart [see Patient Counseling Information (17)].

Ophthalmic solution containing netarsudil 0.02% (0.2 mg/mL).

None.

Netarsudil is a Rho kinase inhibitor. Its chemical name is (S)-4-(3-amino-1-(isoquinolin-6-yl-amino)-1-oxopropan-2-yl) benzyl 2,4-dimethylbenzoate dimesylate. The molecular formula of the free base is C₂₈H₂₇N₃O₃ and the molecular formula of the dimesylate is C₃₀H₃₅N₃O₉S₂. The molecular weight of the free base is 453.54 and the molecular weight of the dimesylate is 645.74. The chemical structure is:

Netarsudil dimesylate is a light yellow-to-white powder that is freely soluble in water, soluble in methanol, sparingly soluble in dimethyl formamide, and practically insoluble in dichloromethane and heptane.

RHOPRESSA (netarsudil ophthalmic solution) 0.02% is supplied as a sterile, isotonic, buffered aqueous solution of netarsudil dimesylate with a pH of approximately 5 and an osmolality of approximately 295 mOsmol/kg. It is intended for topical application in the eye. Each mL of RHOPRESSA contains 0.2 mg of netarsudil (equivalent to 0.28 mg of netarsudil dimesylate). Benzalkonium chloride, 0.015%, is added as a preservative. The inactive ingredients are: boric acid, mannitol, sodium hydroxide to adjust pH, and water for injection.

RHOPRESSA 0.02% was evaluated in three randomized and controlled clinical trials, namely AR-13324-CS301 (NCT 02207491, referred to as Study 301), AR-13324-CS302 (NCT 02207621, referred to as Study 302), and AR-13324-CS304 (NCT 02558374, referred to as Study 304), in patients with open-angle glaucoma or ocular hypertension. Studies 301 and 302 enrolled subjects with baseline IOP lower than 27 mmHg and Study 304 enrolled subjects with baseline IOP lower than 30 mmHg. The treatment duration was 3 months in Study 301, 12 months in Study 302, and 6 months in Study 304.

The three studies demonstrated up to 5 mmHg reductions in IOP for subjects treated with RHOPRESSA 0.02% once daily in the evening. For patients with baseline IOP < 25 mmHg, the IOP reductions with RHOPRESSA 0.02% dosed once daily were similar to those with timolol 0.5% dosed twice daily (see Table 1). For patients with baseline IOP equal to or above 25 mmHg, however, RHOPRESSA 0.02% resulted in smaller mean IOP reductions at the morning time points than timolol 0.5% for study visits on Days 43 and 90; the difference in mean IOP reduction between the two treatment groups was as high as 3 mmHg, favoring timolol.

Table 1: Mean IOP Change from Baseline of Study Eye (mmHg) by Visit and Time

Study 301: Subjects with Baseline IOP < 25 mmHg	Study 301: Subjects with Baseline IOP >= 25 and < 27 mmHg
Study 302: Subjects with Baseline IOP < 25 mmHg	Study 302: Subjects with Baseline IOP >= 25 and < 27 mmHg
Study 304: Subjects with Baseline IOP < 25 mmHg	Study 304: Subjects with Baseline IOP >= 25 and < 30 mmHg

This table was produced based on the observed data from all randomized subjects who did not have major protocol violations. The treatment differences and two-sided CIs for comparing Rhopressa QD vs Timolol BID 0.5% were based on Analysis of Covariance (ANCOVA) adjusted for baseline IOP.

RHOPRESSA^® (netarsudil ophthalmic solution) 0.02% (0.2 mg per mL) is supplied sterile in opaque white low density polyethylene bottles and tips with white polypropylene caps.

2.5 mL fill in a 4 mL container
NDC # 70727-497-25

Storage: Store at 2°C to 8°C (36°F to 46°F) until opened. After opening, the product may be kept at 2°C to 25°C (36°F to 77°F) for up to 6 weeks. If after opening the product is kept refrigerated at 2°C to 8°C (36°F to 46°F), then the product can be used until the expiration date stamped on the bottle. During shipment, the bottle may be maintained at temperatures up to 40°C (104°F) for a period not exceeding 14 days.

Handling the Container

Instruct patients to avoid allowing the tip of the dispensing container to contact the eye, surrounding structures, fingers, or any other surface in order to minimize contamination of the solution. Serious damage to the eye and subsequent loss of vision may result from using contaminated solutions [see Warnings and Precautions (5.2)].

When to Seek Physician Advice

Advise patients that if they develop an intercurrent ocular condition (e.g., trauma, infection, or decreased vision with or without eye pain), have ocular surgery, or develop any ocular reactions, particularly conjunctivitis and eyelid reactions, they should immediately seek their physician’s advice concerning the continued use of RHOPRESSA.

Use with Contact Lenses

Advise patients that RHOPRESSA contains benzalkonium chloride, which may be absorbed by soft contact lenses. Contact lenses should be removed prior to instillation of RHOPRESSA and may be reinserted 15 minutes following its administration.

Use with Other Ophthalmic Drugs

Advise patients that if more than one topical ophthalmic drug is being used, the drugs should be administered at least 5 minutes between applications.

Missed Dose

Advise patients that if one dose is missed, treatment should continue with the next dose in the evening.

© 2024 Alcon Inc.

U.S. Pat.: www.alconpatents.com
ALCON LABORATORIES, INC.
6201 South Freeway Fort Worth, Texas 76134 USA
1-800-757-9195
Alcon.medinfo@alcon.com

NDC 70727-497-25

rhopressa ^®
     (netarsudil ophthalmic
      solution) 0.02%

For topical application
in the eye

Sterile
Rx only

2.5 mL

Alcon

Usual dosage:
One drop in the affected
eye(s) once daily in the
evening.

Each mL Rhopressa^®
ophthalmic solution contains:
Active: netarsudil mesylate
0.285 mg
Preservative:
benzalkonium chloride
0.15 mg
Inactives: mannitol, boric
acid, sodium hydroxide to
adjust pH and water for
injection.

Manufactured for:
ALCON LABORATORIES, INC.
Fort Worth, TX 76134 USA

U.S. Pat: www.alconpatents.com

Store at 2°C - 8°C
(36°F - 46°F) until opened.
After opening, the product
may be kept at 2°C - 25°C
(36°F - 77°F) for up to 6
weeks. If after opening the
product is kept refrigerated at
2°C - 8°C (36°F - 46°F), then
the product can be used until
the expiration date stamped
on the bottle. During
shipment, the bottle may be
maintained at temperatures
up to 40°C (104°F) for a
period not exceeding 14 days.

41079

NDC 70727-497-25       For topical application in the eye.

rhopressa ^®
(netarsudil ophthalmic
      solution) 0.02%

Rx only
Sterile 

2.5 mL                    Alcon                    41077  

See carton for storage conditions.
Manufactured for:
Alcon Laboratories, Inc.
Fort Worth, TX 76134


LOT:
EXP:

NDC 70727-497-99

SAMPLE - Not for Resale

rhopressa ^®
(netarsudil ophthalmic
      solution) 0.02%

For topical application in the eye

Sterile Rx only

2.5 mL

Alcon

Usual dosage:
One drop in the affected
eye(s) once daily in the
evening.

Each mL Rhopressa^®
ophthalmic solution contains:
Active: netarsudil mesylate
0.285 mg
Preservative:
benzalkonium chloride
0.15 mg
Inactives: mannitol, boric
acid, sodium hydroxide to
adjust pH and water for
injection.

Manufactured for:
ALCON LABORATORIES, INC.
Fort Worth, TX 76134 USA

U.S. Pat: www.alconpatents.com

Store at 2°C - 8°C
(36°F - 46°F) until opened.
After opening, the product
may be kept at 2°C - 25°C
(36°F - 77°F) for up to 6
weeks. If after opening the
product is kept refrigerated at
2°C - 8°C (36°F - 46°F), then
the product can be used until
the expiration date stamped
on the bottle. During
shipment, the bottle may be
maintained at temperatures
up to 40°C (104°F) for a
period not exceeding 14 days.

41080

NDC 70727-497-99   SAMPLE - Not for Resale    For topical application in the eye.

rhopressa ^®
(netarsudil ophthalmic
      solution) 0.02%

Rx only
Sterile 

2.5 mL                    Alcon                    41078

See carton for
storage conditions.
Manufactured for:
Alcon Laboratories, Inc.
Fort Worth, TX 76134


LOT:
EXP:

NDC 70727-497-25

rhopressa ^®
     (netarsudil ophthalmic
      solution) 0.02%

For topical application
in the eye

Sterile
Rx only           2.5 mL

Alcon

Usual dosage:
One drop in the affected eye(s) once
daily in the evening.

Each mL Rhopressa^® ophthalmic solution
contains:
Active: netarsudil mesylate 0.285 mg
Preservative:
benzalkonium chloride
0.15 mg
Inactives: mannitol, boric acid, sodium
hydroxide toadjust pH and water for
injection.

ALCON LABORATORIES, INC.
Fort Worth, TX 76134 USA

U.S. Pat: www.alconpatents.com

Store at 2°C - 8°C (36°F - 46°F) until
opened. After opening, the product may
be kept at 2°C - 25°C (36°F - 77°F) for up
to 6 weeks. If after opening the product is
kept refrigerated at 2°C - 8°C (36°F - 46°F),
then the product can be used until the
expiration date stamped on the bottle.
During shipment, the bottle may be
maintained at temperatures up to 40°C
(104°F) for a period not exceeding 14 days.

300069021-1224

NDC 70727-497-25       For topical application in the eye.

rhopressa ^®
(netarsudil ophthalmic
      solution) 0.02%

Rx only
Sterile 

2.5 mL                    Alcon                    

See carton for storage conditions.

Alcon Laboratories, Inc.
Fort Worth, TX 76134


LOT:           EXP.:

300069075
1224

NDC 70727-497-99

SAMPLE - Not for Resale

rhopressa ^®
      (netarsudil ophthalmic
      solution) 0.02%

For topical application
in the eye

Sterile
Rx only          2.5 mL

Alcon

Usual dosage:
One drop in the affected
eye(s) once daily in the
evening.

Each mL Rhopressa^®
ophthalmic solution contains:
Active: netarsudil mesylate
0.285 mg
Preservative:
benzalkonium chloride
0.15 mg
Inactives: mannitol, boric
acid, sodium hydroxide to
adjust pH and water for
injection.

ALCON LABORATORIES, INC.
Fort Worth, TX 76134 USA

U.S. Pat: www.alconpatents.com

Store at 2°C - 8°C
(36°F - 46°F) until opened.
After opening, the product may
be kept at 2°C - 25°C
(36°F - 77°F) for up to 6 weeks.
If after opening the product is
kept refrigerated at 2°C - 8°C
(36°F - 46°F), then the product
can be used until the
expiration date stamped on the
bottle. During shipment, the
bottle may be maintained at
temperatures up to 40°C
(104°F) for a period not
exceeding 14 days.

300069020-1124

NDC 70727-497-99   SAMPLE - Not for Resale    For topical application in the eye.

rhopressa ^®
     (netarsudil ophthalmic
      solution) 0.02%

Rx only
Sterile      2.5 mL                    Alcon                   

See carton for
storage conditions.

Alcon Laboratories, Inc.
Fort Worth, TX 76134 USA


LOT:            EXP.:

300069074
1124