Carfilzomib (Kyprolis)
Overview
A tetrapeptide epoxyketone proteasome inhibitor that irreversibly binds the chymotrypsin-like (beta5) subunit of the 20S proteasome. By blocking proteasomal degradation of ubiquitinated proteins, carfilzomib causes accumulation of misfolded proteins, endoplasmic reticulum stress, and activation of the unfolded protein response, leading to apoptosis preferentially in malignant plasma cells. Its irreversible binding confers greater proteasome inhibition than bortezomib.
Key Research Findings
FDA-approved for relapsed or refractory multiple myeloma (2012, expanded 2015). ASPIRE trial demonstrated 31% improvement in progression-free survival when added to lenalidomide/dexamethasone vs. lenalidomide/dexamethasone alone (Stewart et al., NEJM, 2015). ENDEAVOR trial showed superior PFS vs. bortezomib. Cardiovascular toxicity (heart failure, hypertension) is a notable risk requiring monitoring.
Intravenous
FDA Approved
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