A potent and irreversible proteasome inhibitor. Synthetic analog of the microbial product epoxomcin. Compared to bortezomib it displays equal potency but greater selectivity for the chymotrypsin-like activity of the proteasome. In cell culture it is more cytotoxic than bortezomib and hematologic tumor cells exhibit greater sensitivity than solid tumor cells. Treatment of cells with carfilzomib results in the accumulation of proteasome substrates and induction of cell cycle arrest and/or apoptosis. Effective against multiple myeloma. Active in vivo.
References:
1. MK Bennett and CJ Kirk Curr. Opin. Drug Disc. Dev. 2008 11:616
2. M Hanada et al. J. Antibiot. (Tokyo) 1992 45:1746
3. SD Demo et al. Cancer Res. 2007 67:6383 4. DJ Kuhn et al. Blood 2007 110:3281
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