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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
gefitinib
L01EB01
Adult Dosing
- Non-small cell lung cancer (NSCLC): 250 mg orally once daily until disease progression or unacceptable toxicity
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- First-line treatment of metastatic non-small cell lung cancer (NSCLC) with EGFR exon 19 deletions or exon 21 (L858R) substitution mutations
Mechanism of Action
- Reversible inhibitor of the epidermal growth factor receptor (EGFR) tyrosine kinase, blocking signal transduction pathways essential for tumor growth and survival
Contraindications
- Known severe hypersensitivity to gefitinib or any product excipients
- Pregnancy and lactation
Adverse Reactions
- Diarrhea
- Skin reactions (rash, acne, dry skin, pruritus)
- Nausea and vomiting
- Elevated transaminases
- Interstitial lung disease (ILD)-like events
- Corneal erosion and ocular ulceration
Drug Interactions
- CYP3A4 inducers (e.g., rifampin, carbamazepine) decrease gefitinib plasma concentrations and efficacy
- CYP3A4 inhibitors (e.g., ketoconazole, itraconazole) increase gefitinib plasma concentrations and toxicity risk
- Drugs that elevate gastric pH (e.g., proton pump inhibitors, H2-receptor antagonists) may decrease gefitinib absorption and efficacy
Curated Content: Needs Vetting Before Put to Clinical Use