Bortezomib

Peptide

Bortezomib is the first-in-class proteasome inhibitor for multiple myeloma and mantle cell lymphoma. FDA-approved 2003 (relapsed MM), 2008 (frontline), 2014 (MCL). A-GRADE evidence: APEX Phase 3 (n=669) showed 38% vs 18% response rate vs dexamethasone (P<0.001), 80% vs 66% 1-year survival. VISTA (n=682): VMP superior to MP in transplant-ineligible elderly. SAFETY CONCERN: Peripheral neuropathy 31-45% (dose-limiting), thrombocytopenia 26-30%. Subcutaneous route reduces neuropathy vs IV. Neuropathy 75-81% reversible with dose modification. PRESCRIPTION ONLY - oncology setting.

Quick Answer

What it is

Bortezomib is the first-in-class proteasome inhibitor for multiple myeloma and mantle cell lymphoma. FDA-approved 2003 (relapsed MM), 2008 (frontline), 2014 (MCL).

Key findings

  • Grade A: Response Rate (Relapsed MM) (Multiple Myeloma)
  • Grade A: Time to Progression (Multiple Myeloma)
  • Grade A: Overall Survival (Multiple Myeloma)

Safety

  • No increased second malignancy risk.
  • Dose-limiting toxicity.
  • Prior neurotoxic therapy increases risk.
⚠️ 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: Bortezomib

Quick Facts: Bortezomib

  • Best Evidence:Grade A
  • Conditions Studied:1
  • Research Outcomes:14
  • Grade A Findings:6
  • Grade B Findings:1
  • Key Effect:Multiple Myeloma
A6
B1
C5
D2
1 conditions · 14 outcomes

Detailed Outcomes

A
Response Rate (Relapsed MM)
APEX (n=669): Combined CR+PR rate 38% with bortezomib vs 18% with high-dose dexamethasone (P<0.001). Superior response in relapsed MM after 1-3 prior therapies.
largeImproves
A
Time to Progression
APEX: Median TTP 6.22 months with bortezomib vs 3.49 months with dexamethasone. Nearly doubled time to progression. VISTA: VMP significantly prolonged TTP vs MP.
moderateImproves
A
Overall Survival
APEX: 1-year survival 80% vs 66% (P=0.003). VISTA: Persistent OS benefit with VMP vs MP maintained at extended follow-up. No increased second malignancy risk.
moderateImproves
A
Frontline Treatment (Elderly)
VISTA (n=682): VMP superior to MP in transplant-ineligible patients. Higher response rates, longer TTP, improved OS. Established standard of care for elderly MM.
largeImproves
A
Peripheral Neuropathy
SAFETY CONCERN: Incidence 31-45% in Phase 2/3 trials. Dose-limiting toxicity. Sensory > motor, painful, axonal. Subcutaneous route reduces incidence vs IV. 75-81% reversible with dose modification. Prior neurotoxic therapy increases risk.
largeWorsens
A
Thrombocytopenia
SAFETY CONCERN: Common adverse event, cyclical pattern following dosing. Grade 3-4 in 26-30%. Generally recovers during rest periods. May require dose adjustments or transfusions.
moderateWorsens
B
Safety/Tolerability
8 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.
moderateImproves
C
Anti-Cancer Activity
7 systematic reviews and preclinical studies support this finding. Evidence includes systematic reviews/meta-analyses. Primarily preclinical evidence.
smallImproves
C
Immune Function
7 systematic reviews and preclinical studies support this finding. Evidence includes systematic reviews/meta-analyses. Primarily preclinical evidence.
smallImproves
C
Liver Protection
4 preclinical studies support this finding. Primarily preclinical evidence.
smallImproves
C
Kidney Function
3 systematic reviews and preclinical studies support this finding. Evidence includes systematic reviews/meta-analyses. Primarily preclinical evidence.
smallImproves
C
Cancer Cell Apoptosis
3 human trials support this finding. Human clinical trial data available.
smallImproves
D
Pulmonary Function
2 preclinical studies support this finding. Primarily preclinical evidence.
smallImproves
D
Lipid Profile
2 preclinical studies support this finding. Primarily preclinical evidence.
smallImproves

Research Citations (48)

Bortezomib in cancer therapy: Mechanisms, side effects, and future proteasome inhibitors.
(2024)
PMID: 39413903
Doxorubicin synergizes bortezomib-induced multiple myeloma cell death by inhibiting aggresome formation and augmenting endoplasmic reticulum/Golgi stress and apoptosis.
(2024)
PMID: 39623468
Bortezomib is efficacious in the treatment of severe childhood-onset neuropsychiatric systemic lupus erythematosus with psychosis: a case series and mini-review of B-cell immunomodulation in antibody-mediated diseases.
(2023)
PMID: 36971919
Selinexor-Bortezomib-Dexamethasone: A Review in Previously Treated Multiple Myeloma.
(2023)
PMID: 36622630
Bortezomib-resistant multiple myeloma patient-derived xenograft is sensitive to anti-CD47 therapy.
(2022)
PMID: 36113267
Treatment with bortezomib for recurrent proliferative glomerulonephritis with monoclonal IgG deposits in kidney allograft. Case report and review of the literature.
(2022)
PMID: 35522429
Bortezomib-Induced Ovarian Toxicity in Mice.
(2022)
PMID: 35352576
Foot drop in patients treated with bortezomib - a case series and review of the literature.
(2022)
PMID: 34702127
Bortezomib limits renal allograft interstitial fibrosis by inhibiting NF-κB/TNF-α/Akt/mTOR/P70S6K/Smurf2 pathway via IκBα protein stabilization.
(2021)
PMID: 33289516
Bortezomib-induced acute pancreatitis, an uncommon adverse event.
(2021)
PMID: 33207901

Related Peptides