Carfilzomib Carfilzomib;N-{(2S)-2-[(Morpholin-4-ylacetyl)aMino]-4-phenylbutanoyl}-L-leucyl-N-{(2S)-4-Methyl-1-[(2R)-2-Methyloxiran-2-yl]-1-oxopentan-2-yl}-L-phenylalaninaMide;CarfilzoMib salt;CarfilzoMib/PR 171;P 868540-17-4
Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM.
IC50: < 5 nM [1]
Carfilzomib, an irreversible proteasome inhibitor, has a favorable safety profile and significant anti-tumor activity in patients with relapsed and refractory multiple myeloma (MM). Here we summarize the clinical pharmacokinetics (PK), metabolism, and drug-drug interaction (DDI) profile of carfilzomib. The PK of carfilzomib, infused over 2-10 min, was evaluated in patients with solid tumors or MM. The proteasome has emerged as an important target for cancer therapy with the approval of bortezomib, a first-in-class, reversible proteasome inhibitor, for relapsed/refractory multiple myeloma (MM). Carfilzomib induced a dose- and time-dependent inhibition of proliferation, ultimately leading to apoptosis. Carfilzomib showed increased efficacy compared with bortezomib and was active against bortezomib-resistant MM cell lines and samples from patients with clinical bortezomib resistance. Carfilzomib has entered in a Phase II clinical trial in the treatment of multiple myeloma.
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