Anticancer Drugs Carfilzomib Oncology Pharmacology Physiotherapy

Carfilzomib (Mechanism of Action)

In this article we will discuss Carfilzomib (Mechanism of Action)

In this article, we will discuss Carfilzomib (Mechanism of Action). So, let’s get started.

Mechanism of Action

Carfilzomib is a tetrapeptide epoxyketone proteasome inhibitor that irreversibly binds to the  N-terminal threonine-containing active sites of the 20S proteasome, the proteolytic core particle within the 26S proteasome. Carfilzomib had antiproliferative and proapoptotic activities in vitro in solid and hematologic tumor cells. In animals, carfilzomib inhibited proteasome activity in blood and tissue and delayed tumor growth in models of multiple myeloma, hematologic, and solid tumors.


Intravenous carfilzomib administration resulted in suppression of proteasome chymotrypsin-like activity when measured in blood 1 hour after the first dose. On Day 1 of Cycle 1, proteasome inhibition in peripheral blood mononuclear cells (PBMCs) ranged from 79% to 89% at 15 mg/m², and from 82% to 83% at 20 mg/m². In addition, carfilzomib administration resulted in inhibition of the LMP2 and MECL1 subunits of the immunoproteasome ranging from 26% to 32% and 41% to 49%, respectively, at 20 mg/m². Proteasome inhibition was maintained for ≥ 48 hours following the first dose of carfilzomib for each week of dosing.

Leave a Reply

This site uses Akismet to reduce spam. Learn how your comment data is processed.