Carfilzomib
Also known as: Carfilzomib, CFZ, Kyprolis, NPI‑0052, PR-171, PR‑171
Source Carfilzomib at Peptiology
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Summary
Carfilzomib is a synthetic tetrapeptide epoxyketone that selectively and irreversibly inhibits the 20S proteasome, approved for relapsed or refractory multiple myeloma.
Mechanism of Action
Irreversible covalent inhibition of the 20S proteasome chymotrypsin-like activity by binding to the N‑terminal threonine of the β5 subunit
Routes of Administration
Goals & Uses
- Proteasome pathway suppressionMechanistic/ResearchHigh
- Reduction of tumor burden in multiple myelomaOncologyHigh
- Multiple MyelomaOncologyHigh
- Treatment of newly diagnosed multiple myeloma (off-label/investigational)OncologyModerate
- Treatment of relapsed/refractory multiple myelomaOncologyHigh
Contraindications
- Severe cardiac dysfunction (ejection fraction < 40%)CardiovascularHigh
- Hypersensitivity to carfilzomibAllergyHigh
- Uncontrolled cardiac diseaseCardiovascularHigh
- Severe hepatic impairmentOrganModerateLiver function concerns
- Hypersensitivity to carfilzomib or any excipientsAllergyHigh
Adverse Effects
- Peripheral neuropathyNeurologicalUncommon
- HypertensionCardiovascularCommonHigh blood pressure
- ThrombocytopeniaHematologicCommonLow platelet count
- AnemiaHematologicCommonLow red blood cell count or hemoglobin
- FatigueGeneralCommonLow energy or tiredness
- Cardiac failureCardiovascularUncommon
- Infusion-related reactionsHypersensitivityUncommon
- Cardiac failure / cardiomyopathyCardiovascularUncommon
Drug Interactions
- Anticoagulants (e.g., warfarin)Moderate
- Antihypertensive agentsModerate
- Strong CYP3A4 inducers (e.g., rifampin)Moderate
- Strong CYP3A4 inhibitors (e.g., ketoconazole)Moderate
Population Constraints
- PregnancyReproductive SafetyAbsolute
- Renal impairmentOrgan ImpairmentRelative
- Pediatric patientsAgeRelative
- LactationReproductiveAbsolute
- Elderly patients (≥75 years)AgeRelative
- Severe renal impairment (CrCl < 30 mL/min)RenalRelative
Regulatory Status
- European UnionApprovedApproved: relapsed/refractory multiple myelomaEMA approval 2013
- United StatesApprovedApproved: relapsed/refractory multiple myelomaFDA approval 2012
- United KingdomApprovedApproved: relapsed/refractory multiple myelomaMHRA approval
FDA‑approved (2012) for multiple myeloma; also approved in EU and UK.
Evidence & Sources
No sources recorded yet.
Frequently Asked Questions
What is Carfilzomib?
Carfilzomib is a synthetic tetrapeptide epoxyketone that selectively and irreversibly inhibits the 20S proteasome, approved for relapsed or refractory multiple myeloma.
What is Carfilzomib used for?
Carfilzomib is educationally associated with: Proteasome pathway suppression, Reduction of tumor burden in multiple myeloma, Multiple Myeloma, Treatment of newly diagnosed multiple myeloma (off-label/investigational), Treatment of relapsed/refractory multiple myeloma. Educational only — not medical advice.
How is Carfilzomib administered?
Recorded routes of administration: Intravenous.
What are the potential side effects of Carfilzomib?
Reported adverse effects include: Peripheral neuropathy, Hypertension, Thrombocytopenia, Anemia, Fatigue, Cardiac failure, Infusion-related reactions, Cardiac failure / cardiomyopathy. This list is not exhaustive — consult a qualified clinician.
Who should avoid Carfilzomib?
Recorded contraindications: Severe cardiac dysfunction (ejection fraction < 40%), Hypersensitivity to carfilzomib, Uncontrolled cardiac disease, Severe hepatic impairment, Hypersensitivity to carfilzomib or any excipients. Consult a qualified clinician before use.