OncologyFDA Approved

Carfilzomib (Kyprolis)

Intravenous

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.

Mechanism of Action

Its irreversible binding confers greater proteasome inhibition than bortezomib..

Research Summary & Key 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.

Clinical Status

FDA Approved

Carfilzomib (Kyprolis) has received FDA approval and is available for clinical use under appropriate medical supervision. Consult a qualified healthcare provider for prescribing information.

Administration Routes

Intravenous

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Disclaimer: This information is provided for educational and research purposes only. It is not intended as medical advice, diagnosis, or treatment. Always consult a qualified healthcare provider before starting any peptide therapy. The Peptide Association does not endorse or recommend any specific treatment protocol.