Crizotinib
Brand: Xalkori (global)
Anticancer
ALK / ROS1 inhibitor (1st gen)
Pharmacokinetics
| Half-life | 42 hours |
| Tmax | 4 h |
| Protein Binding | 91 % |
| Volume of Distribution | 1772 L/kg (approx) |
| Clearance Route | hepatic |
| Active Metabolites | yes |
| Notes | Major CYP3A substrate; avoid strong CYP3A inhibitors/inducers. |
⚠️ Safety & Warnings
Severity: Moderate
Adverse Effects:
Visual disturbances (common), QT prolongation, hepatotoxicity, GI upset, bradycardia
Contraindications:
Severe hepatic impairment
Precautions:
ECG + LFT monitoring; counsel patient on visual symptoms (brightness trails)
Half life about 42 hours → 1.75 days
Dose: 250 mg twice daily = 500 mg/day