| Feature | Details |
|---|---|
| Class / Type | ALK and ROS1 tyrosine kinase inhibitor (first-generation) |
| Indication | – ALK-positive NSCLC (first-line or after chemotherapy) – ROS1-positive NSCLC |
| Mechanism of Action | Inhibits ALK, ROS1, and MET tyrosine kinase activity → prevents downstream signaling and tumor proliferation |
| Dosing | 250 mg orally twice daily (with or without food) |
| Key Adverse Effects | Visual disturbances (lights, trails), edema, nausea, vomiting, diarrhea, hepatotoxicity, QT prolongation, fatigue, bradycardia |
| Pharmacist Considerations | – Monitor LFTs and electrolytes (for QT prolongation) – Advise dose adjustment for hepatic impairment – Check for CYP3A4 interactions (strong inhibitors or inducers) – Monitor for visual disturbances and bradycardia |
| Monitoring | CBC, LFTs, electrolytes, ECG (for QTc), signs of edema, cardiac rate, visual symptoms |
| Clinical Pearls | – CNS penetration is limited → brain metastases can progress while on therapy – Visual disturbances are common but usually mild – Often replaced by alectinib or other second-gen ALK inhibitors in first-line due to better CNS activity and tolerability |
