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Carfilzomib (Kyprolis)

Peptide

Carfilzomib is a second-generation tetrapeptide epoxyketone proteasome inhibitor for multiple myeloma. FDA-approved 2012 (monotherapy), expanded 2015-2016 (combinations). ASPIRE Phase 3 (n=792): PFS 26.3 vs 17.6 months with KRd vs Rd (HR 0.69, P<0.001). OS improved to 48.3 vs 40.4 months. ENDEAVOR: PFS 18.7 vs 9.4 months vs bortezomib (HR 0.53). SAFETY: Significant cardiac toxicity - heart failure (4-16%), hypertension (9-27%), thromboembolism (24%). Requires cardiac monitoring.

Quick Answer

What it is

Carfilzomib is a second-generation tetrapeptide epoxyketone proteasome inhibitor for multiple myeloma. FDA-approved 2012 (monotherapy), expanded 2015-2016 (combinations).

Key findings

  • Grade A: Progression-Free Survival (KRd) (Multiple Myeloma)
  • Grade A: Overall Survival (Multiple Myeloma)
  • Grade A: PFS vs Bortezomib (Multiple Myeloma)

Safety

  • SAFETY: Significant cardiac toxicity - heart failure (4-16%), hypertension (9-27%), thromboembolism (24%).
  • Higher risk than bortezomib.
  • Consider in patients with cardiovascular risk factors.
⚠️ Research Notice

This peptide information is for educational and research purposes only. Peptides may not be FDA-approved for human use and may only be legally available for research purposes. Consult qualified healthcare professionals before considering any peptide compounds.

ℹ️ Quick Facts: Carfilzomib (Kyprolis)

Quick Facts: Carfilzomib (Kyprolis)

  • Best Evidence:Grade A
  • Conditions Studied:1
  • Research Outcomes:13
  • Grade A Findings:5
  • Grade B Findings:2
  • Key Effect:Multiple Myeloma
A5
B2
C5
D1
1 conditions · 13 outcomes

Detailed Outcomes

A
Progression-Free Survival (KRd)
ASPIRE (n=792): Median PFS 26.3 months with KRd vs 17.6 months with Rd (HR 0.69, P<0.001). 8.7 month improvement. Deep responders (≥CR) achieved 50.4 months PFS.
large↑Improves
A
Overall Survival
ASPIRE final analysis: OS 48.3 vs 40.4 months (HR 0.79, P=0.0045). 7.9 month survival benefit. ENDEAVOR vs bortezomib also showed OS advantage.
moderate↑Improves
A
PFS vs Bortezomib
ENDEAVOR (n=929): Median PFS 18.7 vs 9.4 months with Kd vs Vd (HR 0.53, P<0.0001). Nearly doubled PFS. Establishes superiority over first-generation proteasome inhibitor.
large↑Improves
A
Cardiac Toxicity
SAFETY CONCERN: Heart failure 4-16%, hypertension 9-27%, arrhythmias, QT prolongation (ROR 4.9). FDA FAERS: 38.6% cardiomyopathy-related, 22.7% cardiac failure. Requires baseline cardiac assessment and monitoring.
moderate↑Worsens
A
Thromboembolism
SAFETY CONCERN: 24% embolic/thrombotic events in FAERS database. DVT prophylaxis recommended. Higher risk than bortezomib. Consider in patients with cardiovascular risk factors.
moderate↓Worsens
B
Safety/Tolerability
12 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.
moderate↑Improves
B
Pulmonary Function
8 human trials support this finding. Human clinical trial data available.
moderate↑Improves
C
Anti-Cancer Activity
7 systematic reviews and preclinical studies support this finding. Evidence includes systematic reviews/meta-analyses. Primarily preclinical evidence.
small↑Improves
C
Immune Function
3 preclinical studies support this finding. Primarily preclinical evidence.
small↑Improves
C
Blood Pressure
3 human trials support this finding. Human clinical trial data available.
small↓Improves
C
Kidney Function
3 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.
small↑Improves
C
Cancer Cell Apoptosis
3 preclinical studies support this finding. Primarily preclinical evidence.
small↑Improves
D
Liver Protection
2 systematic reviews and preclinical studies support this finding. Evidence includes systematic reviews/meta-analyses. Primarily preclinical evidence.
small↑Improves

Research Citations (60)

Cancer targeting carfilzomib nanomedicine: a comprehensive review of delivery vehicles and efficacy.
(2025)
PMID: 41159240
Health-Related Quality of Life in Patients With Relapsed/Refractory Multiple Myeloma Treated With Carfilzomib, Dexamethasone, and Daratumumab Versus Carfilzomib and Dexamethasone: An Analysis of Patient-Reported Outcomes From the Phase 3 CANDOR Trial.
(2025)
PMID: 40087058
Carfilzomib-lenalidomide-dexamethasone versus lenalidomide-dexamethasone in patients with newly diagnosed myeloma ineligible for autologous stem-cell transplantation (EMN20): a randomised, open-label, multicentre, phase 3 trial.
(2025)
PMID: 40769686
Carfilzomib suppressed LDHA-mediated metabolic reprogramming by targeting ATF3 in esophageal squamous cell carcinoma.
(2024)
PMID: 38000560
Carfilzomib activates ER stress and JNK/p38 MAPK signaling to promote apoptosis in hepatocellular carcinoma cells.
(2024)
PMID: 38591121
HIV-protease inhibitors potentiate the activity of carfilzomib in triple-negative breast cancer.
(2024)
PMID: 38969867
Characteristics and outcomes of patients developing pulmonary hypertension associated with proteasome inhibitors.
(2024)
PMID: 38697649
An open-label phase 2 study treating patients with first or second relapse of multiple myeloma with carfilzomib, pomalidomide, and dexamethasone (KPd): SELECT study.
(2024)
PMID: 38497533
Comparative efficacy of carfilzomib, lenalidomide, and dexamethasone (KRd) versus bortezomib, lenalidomide, and dexamethasone (VRd) in newly-diagnosed multiple myeloma: A systematic review and meta-analysis.
(2024)
PMID: 38606993
Isatuximab plus carfilzomib-dexamethasone versus carfilzomib-dexamethasone in patients with relapsed multiple myeloma (IKEMA): overall survival analysis of a phase 3, randomised, controlled trial.
(2024)
PMID: 39067465

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