아파티닙이말레산염

Afatinib tablets are a kinase inhibitor indicated for: • First-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have non-resistant epidermal growth factor receptor (EGFR) mutations as detected by an FDA-approved test ( 1.1 ) Limitations of Use : Safety and efficacy of afatinib tablets were not established in patients whose tumors have resistant EGFR mutations ( 1.1 ) • Treatment of patients with metastatic, squamous NSCLC progressing after platinum-based chemotherapy ( 1.2 ) 1.1 EGFR Mutation-Positive, Metastatic Non-Small Cell Lung Cancer Afatinib tablets are indicated for the first-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have non-resistant epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations as detected by an FDA-approved test [see Dosage and Administration (2.1), Clinical Pharmacology (12.1), Clinical Studies (14.1)]. Limitations of Use : The safety and efficacy of afatinib tablets have not been established in patients whose tumors have resistant EGFR mutations [ see Clinical Studies (14.1)] . 1.2 Previously Treated, Metastatic Squamous NSCLC Afatinib tablets are indicated for the treatment of patients with metastatic squamous NSCLC progressing after platinum-based chemotherapy.

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• Diarrhea : Diarrhea may result in dehydration and renal failure. Withhold afatinib for severe and prolonged diarrhea not responsive to anti-diarrheal agents. ( 2.3 , 5.1 ) • Bullous and exfoliative skin disorders : Severe bullous, blistering, and exfoliating lesions occurred in 0.2% of patients. Discontinue for life-threatening cutaneous reactions. Withhold afatinib for severe and prolonged cutaneous reactions. ( 2.3 , 5.2 ) • Interstitial lung disease (ILD) : Occurs in 1.6% of patients. Withhold afatinib for acute onset or worsening of pulmonary symptoms. Discontinue afatinib if ILD is diagnosed. ( 2.3 , 5.3 ) • Hepatic toxicity : Fatal hepatic impairment occurs in 0.2% of patients. Monitor with periodic liver testing. Withhold or discontinue afatinib for severe or worsening liver tests. ( 2.3 , 5.4 ) • Gastrointestinal perforation : Occurs in 0.2% of patients. Permanently discontinue afatinib in patients who develop gastrointestinal perforation. ( 2.3 , 5.5 ) • Keratitis : Occurs in 0.7% of patients. Withhold afatinib for keratitis evaluation. Withhold or discontinue afatinib for confirmed ulcerative keratitis. ( 2.3 , 5.6 ) • Embryo-fetal toxicit y: Can cause fetal harm when administered to a pregnant woman. Advise pregnant women and females of reproductive potential of the potential risk to the fetus and to use effective contraception. ( 5.7 ) 5.1 Diarrhea Diarrhea has resulted in dehydration with or without renal impairment across the clinical experience; some cases …

8.1 Pregnancy Risk Summary Based on findings from animal studies and its mechanism of action [ see Clinical Pharmacology ( 12.1 ) ], afatinib can cause fetal harm when administered to a pregnant woman. There are no available data on the use of afatinib in pregnant women. Administration of afatinib to pregnant rabbits during organogenesis at exposures approximately 0.2 times the exposure in humans at the recommended dose of 40 mg daily resulted in embryotoxicity and, in rabbits showing maternal toxicity, increased abortions at late gestational stages ( see Data ). Advise a pregnant woman of the potential risk to a fetus. The background risk of major birth defects and miscarriage for the …