Oncology · FDA Approved
Carfilzomib (Kyprolis)
FDA-approved
01 · Overview
A tetrapeptide epoxyketone proteasome inhibitor that binds the proteasome irreversibly, with minimal off-target inhibition of other proteases in preclinical studies (PMID 21568676). By blocking proteasomal breakdown of ubiquitinated proteins, carfilzomib causes misfolded proteins to accumulate, leading to stress responses and death of malignant plasma cells.
Peripheral neuropathy was reported less often than with other proteasome inhibitors in early studies (PMID 21568676).
02 · Research summary & key findings
FDA-approved (Kyprolis, 2012) for relapsed or refractory multiple myeloma, with later expanded indications. In the ASPIRE trial, adding carfilzomib to lenalidomide and dexamethasone extended median progression-free survival from 17.6 to 26.3 months, a 31% lower risk of progression or death (Stewart et al., NEJM, 2015) (PMID 25482145). In ENDEAVOR, carfilzomib-dexamethasone roughly doubled median progression-free survival compared with bortezomib-dexamethasone (18.7 vs. 9.4 months) (PMID 26671818). A meta-analysis found cardiovascular adverse events, including heart failure and hypertension, in about 18% of treated patients (PMID 29285538).
03 · Regulatory status
Carfilzomib (Kyprolis) has received FDA approval and is available for clinical use under appropriate medical supervision. Consult a qualified healthcare provider for prescribing information.
Carfilzomib (Kyprolis) is an FDA-approved medicine prescribed for the conditions on its label. It is not part of our intake, so we do not propose protocols for it. If you think it may be relevant to you, talk to your own doctor. How to ask your doctor.
04 · Administration routes
- Intravenous
References
- [1]Carfilzomib: a novel second-generation proteasome inhibitor Future Oncol, 2011. PMID 21568676
- [2]Carfilzomib, lenalidomide, and dexamethasone for relapsed multiple myeloma N Engl J Med, 2015. PMID 25482145
- [3]Carfilzomib and dexamethasone versus bortezomib and dexamethasone for patients with relapsed or refractory multiple myeloma (ENDEAVOR): a randomised, phase 3, open-label, multicentre study Lancet Oncol, 2016. PMID 26671818
- [4]Carfilzomib-Associated Cardiovascular Adverse Events: A Systematic Review and Meta-analysis JAMA Oncol, 2018. PMID 29285538
Primary literature
- PubMed: "Carfilzomib"
Peer-reviewed literature indexed by the National Library of Medicine.
- ClinicalTrials.gov: "Carfilzomib"
Registered interventional and observational studies, including status and phase.
- PubChem: "Carfilzomib"
Chemical structure, molecular properties, and bioactivity data.
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