Category: pharmacological
Aliases: Torisel, CCI-779
mTOR inhibitor — ester prodrug rapidly hydrolyzed to sirolimus in vivo. Approved for advanced renal cell carcinoma (IV weekly infusion). CYP3A4 substrate (the parent ester and the sirolimus metabolite). Largely displaced by oral everolimus + kinase inhibitors (sunitinib, pazopanib, cabozantinib) in modern RCC regimens. PK (Torisel label, 25 mg IV weekly): mean Cmax 585 ng/mL (CV 14%), AUC 1627 ng·h/mL (CV 26%), t½ 17.3 h (parent); 54.6 h sirolimus metabolite. Vss 172 L in whole blood. Hydrolyzed in vivo to sirolimus (active mTOR-inhibiting metabolite); both species contribute to clinical effect. CYP3A4 substrate.
IV: 17.3h