| Feature | Details |
|---|---|
| Class / Type | EGFR tyrosine kinase inhibitor (TKI), second-generation |
| Indication | First-line treatment for EGFR mutation-positive NSCLC (exon 19 deletion or exon 21 L858R mutation) |
| Mechanism of Action | Irreversibly inhibits EGFR (ErbB1), HER2 (ErbB2), and HER4 (ErbB4) tyrosine kinase activity, blocking downstream signaling and tumor growth |
| Dosing | 40 mg orally once daily (adjust based on tolerance or renal/hepatic function) |
| Key Adverse Effects | Diarrhea, rash/acneiform dermatitis, stomatitis/mucositis, paronychia, fatigue, hepatotoxicity, interstitial lung disease (rare) |
| Pharmacist Considerations | – CYP3A4 metabolism: check for drug interactions – Monitor LFTs and renal function – Dose modifications recommended for severe diarrhea, skin toxicity, or other grade ≥3 adverse events – Counsel patients on hydration, skin care, and adherence |
| Monitoring | CBC, LFTs, renal function, electrolytes, clinical signs of diarrhea and skin toxicity, pulmonary symptoms (ILD risk) |
| Clinical Pearls | – Oral therapy → adherence is critical – Rash may correlate with response – Often chosen over first-generation TKIs (erlotinib, gefitinib) in certain EGFR mutations due to irreversible binding and broader HER family inhibition |