Pharmacological effects of Carfilzomib

Carfilzomib (Carfilzomib) is a tetrapeptide epoxyketone proteasome inhibitor. Carfilzomib has in vitro antiproliferative and proapoptotic activities in solid and hematological tumor cells. In animals, carfilzomib inhibits proteasome activity in blood and tissues and delays tumor growth in multiple myeloma, hematologic disease, and solid tumor models. Intravenous administration of carfilzomib inhibits proteasomal chymotrypsin-like (CT-L) activity 1 hour after the first dose. Carfilzomib dose ≥15 mg/m2, with or without lenalidomide and dexamethasone, induces ≥80% inhibition of proteasome CT-L activity. Proteasome inhibition persisted for ≥48 hours after the first weekly dose of carfilzomib.