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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
afatinib
L01EB03
Forms & Strengths
- Oral tablets: 20 mg
- Oral tablets: 30 mg
- Oral tablets: 40 mg
- Oral tablets: 50 mg
Adult Dosing
- Non-small cell lung cancer (NSCLC): 40 mg orally once daily taken at least 1 hour before or 2 hours after a meal until disease progression or unacceptable toxicity
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- First-line treatment of patients with metastatic non-small cell lung cancer (NSCLC) whose tumors have epidermal growth factor receptor (EGFR) exon 19 deletions or exon 21 (L858R) substitution mutations
- Treatment of metastatic squamous NSCLC progressing on or after platinum-based chemotherapy
Mechanism of Action
- Irreversible covalent inhibitor of the kinase activity of the ErbB family of receptors (EGFR/HER1, HER2, and HER4), blocking downstream signaling pathways essential for tumor growth and survival
Contraindications
- Known severe hypersensitivity to afatinib or any of its excipients
Adverse Reactions
- Diarrhea
- Rash / acneiform dermatitis
- Stomatitis / oral mucositis
- Paronychia
- Decreased appetite and weight loss
- Nausea and vomiting
- Pruritus
- Elevated alanine aminotransferase (ALT) and aspartate aminotransferase (AST)
Drug Interactions
- P-glycoprotein (P-gp) inhibitors (e.g., ritonavir, ketoconazole): May increase afatinib exposure; administer P-gp inhibitors prior to or concurrently with extreme caution
- P-gp inducers (e.g., rifampin, carbamazepine, St. John's wort): May significantly decrease afatinib exposure; avoid concurrent use
Curated Content: Needs Vetting Before Put to Clinical Use