Category: pharmacological
Aliases: Afinitor, Zortress, Votubia, RAD001
mTOR (mTORC1) inhibitor — binds FKBP12 → inhibits raptor-mTOR complex. Indications: HR+/HER2− breast cancer (with exemestane), advanced renal cell carcinoma, neuroendocrine tumors, TSC-associated SEGA and renal angiomyolipoma, immunosuppression in heart/kidney/liver transplant. CYP3A4 + P-gp substrate; therapeutic drug monitoring required at transplant doses (target trough 3-8 ng/mL). PK (Afinitor label, 10 mg PO qd oncology dose): Cmax 61.5 ng/mL (29.6% CV), AUC24 435 ng·h/mL (28.1% CV), Tmax 1-2 h, t½ 16-19 h, protein binding ~74%. Apparent CL/F 23 L/h, V/F 581 L. High-fat meal ↓AUC 22%, ↓Cmax 54%; light-fat meal ↓AUC 32%. CYP3A4 + P-gp substrate; therapeutic drug monitoring (target trough 3-8 ng/mL at transplant doses).
PO: 17.5h