Carfilzomib in Multiple Myeloma

摘要

H&O What is carfilzomib (Kyprolis, Onyx Pharmaceuticals), and how does it differ from bortezomib (Velcade, Millennium Pharmaceuticals)? RV Carfilzomib is a novel potent, highly selective epoxyketone proteasome inhibitor that targets the chy-motrypsin-like activity of the 20S proteasome. Carfilzomib is believed to be more specific for the proteasome than bortezomib, which is a boronate. Whereas bortezomib is a reversible proteasome inhibitor, carfilzomib is an irreversible proteasome inhibitor, and this may account for a better potential efficacy profile of the drug. Furthermore, in laboratory models, carfilzomib appears to overcome bortezomib resistance in bortezomib-resistant cell lines. Thus, carfilzomib does have several potential advantages over bortezomib in terms of its structure and mechanism of action.