LETROZOLE

openFDA label record#

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Brand name
LETROZOLE
Generic name
LETROZOLE
Manufacturer
Chartwell RX, LLC
Product type
HUMAN PRESCRIPTION DRUG
SPL set ID
fa2d40a5-3504-44ef-8f5c-aa4c06308074
SPL ID
456ed484-059b-2ee9-e063-6294a90a3f83
Version
5
Effective date
2025-12-08
Source export date
2026-08-01
Applications, Product NDCs, Package NDCs table
ApplicationsProduct NDCsPackage NDCsRxCUIsUNIIsRoutes
ANDA20586962135-49162135-491-30, 62135-491-902000647LKK855W8IORAL

Warnings cross-check#

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warnings and cautions

5 WARNINGS AND PRECAUTIONS Decreases in bone mineral density may occur. Consider bone mineral density monitoring ( 5.1 ) Increases in total cholesterol may occur. Consider cholesterol monitoring. ( 5.2 ) Fatigue, dizziness and somnolence may occur. Exercise caution when operating machinery ( 5.4 ) Embryo-Fetal toxicity: Can cause fetal harm when administered to pregnant women. Obtain a pregnancy test in females of reproductive potential. Advise females of reproductive potential to use effective contraception ( 5.6 , 8.1 , 8.3 ) 5.1 Bone Effects Use of letrozole may cause decreases in bone mineral density (BMD). Consideration should be given to monitoring BMD. Results of a safety study to evaluate safety in the adjuvant setting comparing the effect on lumbar spine (L2 to L4) BMD of adjuvant treatment with letrozole to that with tamoxifen showed at 24 months a median decrease in lumbar spine BMD of 4.1% in the letrozole arm compared to a median increase of 0.3% in the tamoxifen arm (difference = 4.4%) ( P

Adverse reactions cross-check#

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adverse reactions

6 ADVERSE REACTIONS The following adverse reactions are discussed in greater detail in other sections of the labeling. Bone effects [see Warnings and Precautions (5.1) ] Increases in cholesterol [see Warnings and Precautions (5.2) ] Fatigue and Dizziness [see Warnings and Precautions (5.4) ] The most common adverse reactions (greater than 20%) were hot flashes, arthralgia; flushing, asthenia, edema, arthralgia, headache, dizziness, hypercholesterolemia, sweating increased, bone pain; and musculoskeletal ( 6 ). To report SUSPECTED ADVERSE REACTIONS, contact Chartwell RX, LLC. at 1-845-232-1683 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reactions 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. Adjuvant Treatment of Early Breast Cancer In study, BIG 1-98, the median treatment duration of adjuvant treatment was 60 months and the median duration of follow-up for safety was 96 months for patients receiving letrozole and tamoxifen. Certain adverse reactions were prospectively specified for analysis ( see Table 1 ), based on the known pharmacologic properties and side effect profiles of the two drugs. Adverse reactions were analyzed irrespective of whether a symptom was present or absent at baseline. Most adverse reactions reported (approximately 75% of patients who reported AEs) were Grade 1 or Grade 2 applying the Common Toxicity Criteria (CTC) Version 2.0/Common Terminology Criteria for Adverse Events (CTCAE), Version 3.0. Table 1 describes adverse reactions (Grades 1 to 4 and Grades 3 to 4) irrespective of relationship to study treatment in the adjuvant trial for the monotherapy arms analysis (safety population). Table 1: Patients with Adverse Reactions (CTC Grades 1 to 4) in the Adjuvant Study – Monotherapy Arms Analysis (Median Follow-up 96 Months; Median Treatment 60 Months) Grades 1 to 4 Grades 3 to 4 Letrozole Tamoxifen Letrozole Tamoxifen Adverse Reactions N = 2448 N = 2447 N = 2448 N = 2447 n (%) n (%) n (%) n (%) Patients with any adverse reaction 2309 (94.3) 2212 (90.4) 636 (26.0) 606 (24.8) Hypercholesterolemia* 1280 (52.3) 700 (28.6) 11 (0.4) 6 (0.2) Hot flashes* 819 (33.5) 929 (38.0) - - - - Arthralgia/arth...

adverse reactions table

Grades 1 to 4Grades 3 to 4LetrozoleTamoxifenLetrozoleTamoxifenAdverse ReactionsN = 2448N = 2447N = 2448N = 2447n (%)n (%)n (%)n (%)Patients with any adverse reaction2309(94.3)2212(90.4)636(26.0)606(24.8)Hypercholesterolemia*1280(52.3)700(28.6)11(0.4)6(0.2)Hot flashes*819(33.5)929(38.0)----Arthralgia/arthritis*621(25.4)504(20.6)84(3.4)50(2.0)Bone fractures 1361(14.7)280(11.4)----Night sweats*356(14.5)426(17.4)----Weight increase*317(12.9)378(15.4)27(1.1)39(1.6)Nausea*284(11.6)277(11.3)6(0.2)9(0.4)Bone fractures** 2249(10.2)175(7.2)----Fatigue (lethargy, malaise, asthenia)*235(9.6)250(10.2)6(0.2)7(0.3)Myalgia*221(9.0)212(8.7)18(0.7)14(0.6)Vaginal bleeding*129(5.3)320(13.1)1(< 0.1)8(0.3)Edema*164(6.7)160(6.5)3(0.1)1(< 0.1)Weight decrease140(5.7)129(5.3)8(0.3)5(0.2)Osteoporosis**126(5.1)67(2.7)10(0.4)5(0.2)Back pain125(5.1)136(5.6)7(0.3)11(0.4)Bone pain123(5.0)109(4.5)6(0.2)4(0.2)Depression119(4.9)114(4.7)16(0.7)14(0.6)Vaginal irritation*112(4.6)77(3.1)2(< 0.1)2(< 0.1)Headache*105(4.3)94(3.8)8(0.3)4(0.2)Pain in extremity103(4.2)79(3.2)6(0.2)4(0.2)Osteopenia*87(3.6)76(3.1)0-3(0.1)Dizziness/light-headedness*84(3.4)80(3.3)1(< 0.1)6(0.2)Alopecia83(3.4)84(3.4)----Vomiting*80(3.3)80(3.3)3(0.1)5(0.2)Cataract*49(2.0)54(2.2)16(0.7)17(0.7)Constipation*49(2.0)71(2.9)3(0.1)1(< 0.1)Myocardial infarction 142(1.7)28(1.1)----Breast pain*37(1.5)43(1.8)1(< 0.1)--Anorexia*20(0.8)20(0.8)1(< 0.1)1(< 0.1)Endometrial proliferation disorders*14(0.6)

adverse reactions table

Adverse ReactionsLetrozole N = 2049 n (%)Anastrozole N = 2062 n (%)Grade 3/4 n (%)All Grades n (%)Grade 3/4 n (%)All Grades n (%)Patients with at least one AR628 (30.6)2049 (100.0)591 (28.7)2062 (100.0)Arthralgia80 (3.9)987 (48.2)69 (3.3)987 (47.9)Hot flush17 (0.8)666 (32.5)9 (0.4)666 (32.3)Fatigue8 (0.4)345 (16.8)10 (0.5)343 (16.6)Osteoporosis5 (0.2)223 (10.9)11 (0.5)225 (10.9)Myalgia16 (0.8)233 (11.4)15 (0.7)212 (10.3)Back pain11 (0.5)212 (10.3)17 (0.8)193 (9.4)Osteopenia4 (0.2)203 (9.9)1 (0.0)173 (8.4)Pain in extremity9 (0.4)168 (8.2)3 (0.1)174 (8.4)Lymphoedema5 (0.2)159 (7.8)2 (0.1)179 (8.7)Insomnia7 (0.3)160 (7.8)3 (0.1)149 (7.2)Hypercholesterolaemia2 (0.1)155 (7.6)1 (0.0)151 (7.3)Hypertension25 (1.2)156 (7.6)20 (1.0)149 (7.2)Depression16 (0.8)147 (7.2)13 (0.6)137 (6.6)Bone pain10 (0.5)138 (6.7)9 (0.4)122 (5.9)Nausea6 (0.3)137 (6.7)5 (0.2)152 (7.4)Headache3 (0.1)130 (6.3)5 (0.2)168 (8.1)Alopecia2 (0.1)127 (6.2)0 (0.0)134 (6.5)Musculoskeletal pain6 (0.3)123 (6.0)9 (0.4)147 (7.1)Radiation skin injury11 (0.5)120 (5.9)6 (0.3)88 (4.3)Dyspnoea16 (0.8)118 (5.8)10 (0.5)96 (4.7)Cough1 (0.0)106 (5.2)1 (0.0)120 (5.8)Musculoskeletal stiffness2 (0.1)102 (5.0)2 (0.1)84 (4.1)Dizziness2 (0.2)94 (4.6)7 (0.3)109 (5.3)

adverse reactions table

Number (%) of Patients with Grade 1 to 4 Adverse ReactionsNumber (%) of Patients with Grade 3 to 4 Adverse ReactionsLetrozolePlaceboLetrozolePlaceboN = 2563N = 2573N = 2563N = 2573Any Adverse Reactions2232 (87.1)2174 (84.5)419 (16.3)389 (15.1)Vascular Disorders1375 (53.6)1230 (47.8)59 (2.3)74 (2.9) Flushing1273 (49.7)1114 (43.3)3 (0.1)0General Disorders 1154 (45)1090 (42.4)30 (1.2)28 (1.1) Asthenia862 (33.6)826 (32.1)16 (0.6)7 (0.3) Edema NOS471 (18.4)416 (16.2)4 (0.2)3 (0.1)Musculoskeletal Disorders978 (38.2)836 (32.5)71 (2.8)50 (1.9) Arthralgia565 (22)465 (18.1)25 (1)20 (0.8) Arthritis NOS173 (6.7)124 (4.8)10 (0.4)5 (0.2) Myalgia171 (6.7)122 (4.7)8 (0.3)6 (0.2) Back Pain129 (5)112 (4.4)8 (0.3)7 (0.3)Nervous System Disorders863 (33.7)819 (31.8)65 (2.5)58 (2.3) Headache516 (20.1)508 (19.7)18 (0.7)17 (0.7) Dizziness363 (14.2)342 (13.3)9 (0.4)6 (0.2)Skin Disorders830 (32.4)787 (30.6)17 (0.7)16 (0.6) Sweating Increased619 (24.2)577 (22.4)1 (< 0.1)0Gastrointestinal Disorders725 (28.3)731 (28.4)43 (1.7)42 (1.6) Constipation290 (11.3)304 (11.8)6 (0.2)2 (< 0.1) Nausea221 (8.6)212 (8.2)3 (0.1)10 (0.4) Diarrhea NOS128 (5)143 (5.6)12 (0.5)8 (0.3)Metabolic Disorders551 (21.5)537 (20.9)24 (0.9)32 (1.2) Hypercholesterolemia401 (15.6)398 (15.5)2 (< 0.1)5 (0.2)Reproductive Disorders303 (11.8)357 (13.9)9 (0.4)8 (0.3) Vaginal Hemorrhage123 (4.8)171 (6.6)2 (< 0.1)5 (0.2) Vulvovaginal Dryness137 (5.3)127 (4.9)00Psychiatric Disorders320 (12.5)276 (10.7)21 (0.8)16 (0.6) Insomnia149 (5.8)120 (4.7)2 (< 0.1)2 (< 0.1)Respiratory Disorders279 (10.9)260 (10.1)30 (1.2)28 (1.1) Dyspnea140 (5.5)137 (5.3)21 (0.8)18 (0.7)Investigations184 (7.2)147 (5.7)13 (0.5)13 (0.5)Infections and Infestations166 (6.5)163 (6.3)40 (1.6)33 (1.3)Renal Disorders130 (5.1)100 (3.9)12 (0.5)6 (0.2)

adverse reactions table

AdverseLetrozoleTamoxifenReactions2.5 mg20 mg(N = 455)(N = 455)%%General Disorders Fatigue1313 Chest Pain89 Edema Peripheral56 Pain NOS57 Weakness64Investigations Weight Decreased75Vascular Disorders Hot Flushes1916 Hypertension84Gastrointestinal Disorders Nausea1717 Constipation1011 Diarrhea84 Vomiting78Infections/Infestations Influenza64 Urinary Tract Infection NOS63Injury, Poisoning and Procedural Complications Post-Mastectomy Lymphedema77Metabolism and Nutrition Disorders Anorexia46Musculoskeletal and Connective Tissue Disorders Bone Pain2221 Back Pain1819 Arthralgia1615 Pain in Limb108Nervous System Disorders Headache NOS87Psychiatric Disorders Insomnia74Reproductive System and Breast Disorders Breast Pain77Respiratory, Thoracic and Mediastinal Disorders Dyspnea1817 Cough1313 Chest Wall Pain66

adverse reactions table

AdversePooledPooledMegestrolReactionsLetrozoleLetrozoleAcetateAminoglutethimide2.5 mg0.5 mg160 mg500 mg(N = 359)(N = 380)(N = 189)(N = 178)%%%%Body as a Whole Chest Pain6373 Peripheral Edema 15583 Asthenia4545 Weight Increase2293Cardiovascular Hypertension5756Digestive System Nausea1315914 Vomiting7759 Constipation6797 Diarrhea6534 Pain-Abdominal6598 Anorexia5355 Dyspepsia3465Infections/Infestations Viral Infection6563Lab Abnormality Hypercholesterolemia3306Musculoskeletal System Musculoskeletal 221223014 Arthralgia8883Nervous System Headache91297 Somnolence3229 Dizziness3573Respiratory System Dyspnea79165 Coughing6575Skin and Appendages Hot Flushes6543 Rash 354312 Pruritus1253