Selpercatinib
Brand: Retevmo (global)
Anticancer
RET inhibitor
Pharmacokinetics
| Half-life | 32 hours |
| Tmax | 2 h |
| Protein Binding | 97 % |
| Volume of Distribution | 191 L/kg (approx) |
| Clearance Route | hepatic |
| Active Metabolites | yes |
| Notes | Avoid strong CYP3A inhibitors/inducers; take with or without food but avoid high-fat meal. |
⚠️ Safety & Warnings
Severity: Moderate
Adverse Effects:
Hypertension, hepatotoxicity, QT prolongation, dry mouth, edema
Contraindications:
Uncontrolled hypertension
Precautions:
Monitor BP, LFT, QT interval periodically; adjust dose if severe hepatic impairment.
t½ ≈ 32 hours → 1.3 days
dose ~ 160 mg twice daily = 320 mg/day