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ANTINEOPLASTIC AND IMMUNOMODULATING AGENTS › ANTINEOPLASTIC AGENTS › PROTEIN KINASE INHIBITORS › Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors
icotinib
L01EB08
Adult Dosing
- Non-Small Cell Lung Cancer (NSCLC): 125 mg orally three times daily
- Administer continuously until disease progression or unacceptable toxicity
Pediatric Dosing
- Safety and efficacy in pediatric patients have not been established
Indications
- First-line or subsequent treatment of locally advanced or metastatic non-small cell lung cancer (NSCLC) harboring EGFR activating mutations (exon 19 deletion or exon 21 L858R mutation)
Mechanism of Action
- Selective, reversible epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor
- Inhibits EGFR autophosphorylation, blocking downstream signaling pathways involved in tumor cell proliferation and survival
Contraindications
- Hypersensitivity to icotinib or any excipients in the formulation
Adverse Reactions
- Rash (often maculopapular)
- Diarrhea
- Elevated transaminases (ALT, AST)
- Nausea and vomiting
- Pruritus
- Interstitial lung disease (ILD)-like events
- Fatigue
Drug Interactions
- CYP3A4 inducers (e.g., rifampin, carbamazepine, St. John's wort): May decrease icotinib plasma concentrations and efficacy
- CYP3A4 inhibitors (e.g., ketoconazole, erythromycin): May increase icotinib plasma concentrations and toxicity risk
Curated Content: Needs Vetting Before Put to Clinical Use