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Peptide

Bortezomib

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.

Research notice. This page is for education and research. Peptides may not be FDA-approved for human use and may only be legally available for research. Talk to a qualified clinician before considering any peptide.

Best evidence
Grade A
Conditions studied
1
Outcomes
14
Graded outcomes
6152

Evidence by condition

  • Strong
  • Moderate
  • Limited
  • Very limited

1 condition, plus general outcomes

Multiple Myeloma

Multiple Myeloma: outcomes studied for Bortezomib
GradeOutcomeEffectSizeStudiesPeopleStudies list
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.

Improves (the measure goes up)Large effect16 studies

Studies that measured response rate (relapsed mm)

and 6 more in the citations list

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.

Improves (the measure goes up)Moderate effect15 studies

Studies that measured overall survival

and 5 more in the citations list

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.

Improves (the measure goes up)Large effect15 studies

Studies that measured frontline treatment (elderly)

and 5 more in the citations list

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.

Worsens (the measure goes down)Large effect15 studies

Studies that measured peripheral neuropathy

and 5 more in the citations list

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.

Improves (the measure goes up)Moderate effect14 studies

Studies that measured time to progression

and 4 more in the citations list

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.

Worsens (the measure goes down)Moderate effect14 studies

General

General: outcomes studied for Bortezomib
GradeOutcomeEffectSizeStudiesPeopleStudies list
Safety/Tolerability

8 human trials and systematic reviews support this finding. Evidence includes systematic reviews/meta-analyses. Human clinical trial data available.

Improves (the measure goes up)Moderate effect14 studies

Studies that measured safety/tolerability

and 4 more in the citations list

Anti-Cancer Activity

7 systematic reviews and preclinical studies support this finding. Evidence includes systematic reviews/meta-analyses. Primarily preclinical evidence.

Improves (the measure goes up)Small effect15 studies

Studies that measured anti-cancer activity

and 5 more in the citations list

Immune Function

7 systematic reviews and preclinical studies support this finding. Evidence includes systematic reviews/meta-analyses. Primarily preclinical evidence.

Improves (the measure goes up)Small effect13 studies

Studies that measured immune function

and 3 more in the citations list

Liver Protection

4 preclinical studies support this finding. Primarily preclinical evidence.

Improves (the measure goes up)Small effect10 studies

Studies that measured liver protection

Kidney Function

3 systematic reviews and preclinical studies support this finding. Evidence includes systematic reviews/meta-analyses. Primarily preclinical evidence.

Improves (the measure goes up)Small effect9 studies

Studies that measured kidney function

Cancer Cell Apoptosis

3 human trials support this finding. Human clinical trial data available.

Improves (the measure goes up)Small effect9 studies
Pulmonary Function

2 preclinical studies support this finding. Primarily preclinical evidence.

Improves (the measure goes up)Small effect8 studies
Lipid Profile

2 preclinical studies support this finding. Primarily preclinical evidence.

Improves (the measure goes down)Small effect8 studies

Key findings

  • Response Rate (Relapsed MM)Multiple MyelomaImproves (the measure goes up)
  • Overall SurvivalMultiple MyelomaImproves (the measure goes up)
  • Frontline Treatment (Elderly)Multiple MyelomaImproves (the measure goes up)

Safety notes in the studies

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

Studies cited

48 studies from PubMed

  1. Bortezomib in cancer therapy: Mechanisms, side effects, and future proteasome inhibitors.Life sciences, 2024 · PMID 39413903
  2. Doxorubicin synergizes bortezomib-induced multiple myeloma cell death by inhibiting aggresome formation and augmenting endoplasmic reticulum/Golgi stress and apoptosis.Journal of translational medicine, 2024 · PMID 39623468
  3. 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.Clinical rheumatology, 2023 · PMID 36971919
  4. Selinexor-Bortezomib-Dexamethasone: A Review in Previously Treated Multiple Myeloma.Targeted oncology, 2023 · PMID 36622630
  5. Bortezomib-resistant multiple myeloma patient-derived xenograft is sensitive to anti-CD47 therapy.Leukemia research, 2022 · PMID 36113267
  6. Treatment with bortezomib for recurrent proliferative glomerulonephritis with monoclonal IgG deposits in kidney allograft. Case report and review of the literature.Journal of nephrology, 2022 · PMID 35522429
  7. Bortezomib-Induced Ovarian Toxicity in Mice.Toxicologic pathology, 2022 · PMID 35352576
  8. Foot drop in patients treated with bortezomib - a case series and review of the literature.Leukemia & lymphoma, 2022 · PMID 34702127
  9. Bortezomib limits renal allograft interstitial fibrosis by inhibiting NF-κB/TNF-α/Akt/mTOR/P70S6K/Smurf2 pathway via IκBα protein stabilization.Clinical science (London, England : 1979), 2021 · PMID 33289516
  10. Bortezomib-induced acute pancreatitis, an uncommon adverse event.Revista espanola de enfermedades digestivas, 2021 · PMID 33207901
  11. Bortezomib-loaded lipidic-nano drug delivery systems; formulation, therapeutic efficacy, and pharmacokinetics.Journal of microencapsulation, 2021 · PMID 33530812
  12. Bortezomib in anti-N-Methyl-d-Aspartate-Receptor (NMDA-R) encephalitis: A systematic review.Journal of neuroimmunology, 2021 · PMID 33975246
  13. Bortezomib - First Therapeutic Proteasome Inhibitor for Cancer Therapy: A Review of Patent Literature.Recent patents on anti-cancer drug discovery, 2020 · PMID 32234004
  14. Bortezomib for immune thrombocytopenia and autoimmune hemolytic anemia.Hematology/oncology and stem cell therapy, 2020 · PMID 31202670
  15. Bortezomib for autoimmune hemolytic anemia after intestinal transplantation.Pediatric transplantation, 2020 · PMID 32166874
  16. Biotinylated HPMA centered polymeric nanoparticles for Bortezomib delivery.International journal of pharmaceutics, 2020 · PMID 32097684
  17. Utilization of Lipid-based Nanoparticles to Improve the Therapeutic Benefits of Bortezomib.Anti-cancer agents in medicinal chemistry, 2020 · PMID 31985384
  18. Population-based meta-analysis of bortezomib exposure-response relationships in multiple myeloma patients.Journal of pharmacokinetics and pharmacodynamics, 2020 · PMID 31939004
  19. Bortezomib-based consolidation or maintenance therapy for multiple myeloma: a meta-analysis.Blood cancer journal, 2020 · PMID 32144237
  20. Spotlight on Bortezomib: potential in the treatment of hepatocellular carcinoma.Expert opinion on investigational drugs, 2019 · PMID 30474444
  21. The efficacy and safety of bortezomib-based chemotherapy for immunoglobulin light chain amyloidosis: A systematic review and meta-analysis.European journal of internal medicine, 2019 · PMID 31447275
  22. Bortezomib promotes apoptosis of multiple myeloma cells by regulating HSP27.Molecular medicine reports, 2019 · PMID 31322176
  23. Subcutaneous bortezomib might be standard of care for patients with multiple myeloma: a systematic review and meta-analysis.Drug design, development and therapy, 2019 · PMID 31190749
  24. The safety of bortezomib for the treatment of multiple myeloma.Expert opinion on drug safety, 2018 · PMID 30118610
  25. Subcutaneous versus Intravenous Bortezomib Administration for Multiple Myeloma Patients: a Meta-analysis.Current medical science, 2018 · PMID 30074150
  26. Efficacy and safety of bortezomib, thalidomide, and lenalidomide in multiple myeloma: An overview of systematic reviews with meta-analyses.Critical reviews in oncology/hematology, 2017 · PMID 28427509
  27. Efficacy and safety of bortezomib maintenance in patients with newly diagnosed multiple myeloma: a meta-analysis.Bioscience reports, 2017 · PMID 28706008
  28. Bortezomib-Induced Muscle Toxicity in Multiple Myeloma.Journal of neuropathology and experimental neurology, 2017 · PMID 28863457
  29. Bortezomib could down-regulate the expression of RANKL, inhibit cell proliferation and induce cell apoptosis in the human myeloma cell line RPMI 8226 by activating casepase-3.Cancer biomarkers : section A of Disease markers, 2017 · PMID 28869453
  30. Weekly versus biweekly bortezomib given in patients with indolent non-Hodgkin lymphoma: A meta-analysis.PloS one, 2017 · PMID 28531181
  31. Bortezomib-induced syndrome of inappropriate antidiuresis in a patient with multiple myeloma: A case report and literature review
.International journal of clinical pharmacology and therapeutics, 2017 · PMID 29092733
  32. Meta-analysis of incidence and risk of peripheral neuropathy associated with intravenous bortezomibSupport Care Cancer, 2015 · PMID 25676487
  33. Bortezomib in kidney transplantation.Current opinion in organ transplantation, 2015 · PMID 26536428
  34. Linking the activity of bortezomib in multiple myeloma and autoimmune diseases.Critical reviews in oncology/hematology, 2014 · PMID 24890785
  35. Bortezomib in combination with thalidomide or lenalidomide or doxorubicin regimens for the treatment of multiple myeloma: a meta-analysis of 14 randomized controlled trials.Leukemia & lymphoma, 2014 · PMID 23998282
  36. Persistent overall survival benefit and no increased risk of second malignancies with bortezomib-melphalan-prednisone versus melphalan-prednisone in patients with previously untreated multiple myelomaJ Clin Oncol, 2013 · PMID 23233713
  37. Effects of bortezomib on the immune system: a focus on immune regulation.Biology of blood and marrow transplantation : journal of the American Society for Blood and Marrow Transplantation, 2013 · PMID 23707853
  38. Subcutaneous versus intravenous administration of bortezomib in patients with relapsed multiple myeloma: a randomised, phase 3, non-inferiority studyLancet Oncol, 2011 · PMID 22258743
  39. Bortezomib as the First Proteasome Inhibitor Anticancer Drug: Current Status and Future PerspectivesCurr Cancer Drug Targets, 2011 · PMID 22047556
  40. Bortezomib plus melphalan and prednisone compared with melphalan and prednisone in previously untreated multiple myeloma: updated follow-up and impact of subsequent therapy in the phase III VISTA trialJ Clin Oncol, 2010 · PMID 20368561
  41. Bortezomib: a review of its use in patients with multiple myelomaDrugs, 2009 · PMID 19441872
  42. Bortezomib plus melphalan and prednisone for initial treatment of multiple myelomaN Engl J Med, 2008 · PMID 18799451
  43. Extended follow-up of a phase 3 trial in relapsed multiple myeloma: final time-to-event results of the APEX trialBlood, 2007 · PMID 17690257
  44. Incorporating bortezomib into the treatment of lung cancer.Clinical cancer research : an official journal of the American Association for Cancer Research, 2007 · PMID 17671158
  45. Bortezomib-induced peripheral neuropathy in multiple myeloma: a comprehensive review of the literatureJ Clin Oncol, 2006 · PMID 18574024
  46. Bortezomib: proteasome inhibition as an effective anticancer therapy.Annual review of medicine, 2006 · PMID 16409135
  47. Bortezomib or high-dose dexamethasone for relapsed multiple myelomaN Engl J Med, 2005 · PMID 15958804
  48. Preclinical data with bortezomib in lung cancer.Clinical lung cancer, 2005 · PMID 16250927