PeptideTrace
ApprovedProteasome Inhibitor (Boronic Acid)

Bortezomib

Velcade

A

Evidence Grade A — Regulatory approved. 11482 published studies. 1000 registered clinical trials.

1000 trials11,482 studiesUSEUCA

Licensed Indications

  • Multiple Myeloma
  • Mantle Cell Lymphoma

User Experience Reports

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Overview

Bortezomib (sold as Velcade) is a cancer treatment that fundamentally changed how multiple myeloma — a blood cancer of the bone marrow — is managed. It was the first drug in an entirely new class that works by blocking the cell's internal protein recycling system, causing cancer cells to essentially choke on their own waste. Before treatments like bortezomib, most myeloma patients survived about three years; many now live a decade or more.

Research Activity

11,482studies
Human 9058
Animal 485
In-vitro 1723
Reviews 2065

11,482 published studies: 9058 human, 485 animal, 1723 in-vitro, 2065 reviews

Regulatory Status

US
FDA-approved(FDA)
EU
EMA-authorised(EMA)
CA
Health Canada approved(Health Canada)

Legal Status

USPrescription drug (Rx)
EUPrescription medicine (EU centralised authorisation)
CAPrescription drug

Summary

Bortezomib is marketed as Velcade (approved May 2003) for multiple myeloma and mantle cell lymphoma. Generic versions are available. Originally given intravenously, subcutaneous injection is now preferred as it causes significantly less nerve damage.

The VISTA trial established bortezomib-based combination therapy as standard for newly diagnosed myeloma patients ineligible for transplant, with median time to disease progression of 24 months versus 16.6 months with older chemotherapy. Peripheral neuropathy (numbness and tingling in hands and feet) is the main dose-limiting side effect, affecting up to 30% of patients. Bortezomib transformed myeloma from a disease with a median survival of approximately 3 years to one where many patients live a decade or more with sequential treatments.

Mechanism of Action

Like carfilzomib, bortezomib disables the proteasome — the cell's protein recycling system. Myeloma cells produce vast quantities of antibody proteins and rely heavily on the proteasome to dispose of defective copies. When bortezomib blocks the proteasome, these waste proteins accumulate rapidly, triggering a stress response that overwhelms the cancer cell. Bortezomib also blocks the NF-kappaB pathway, which myeloma cells use to resist self-destruction. Unlike carfilzomib's permanent bond, bortezomib's attachment is reversible, which may contribute to its different side effect profile.

Research Summary

Bortezomib has over 20 years of clinical data from dozens of large trials. The VISTA trial established bortezomib-based combination therapy as the standard approach for newly diagnosed myeloma patients, extending the time before disease worsened from about 17 months (with older chemotherapy) to 24 months. Both intravenous and subcutaneous injection routes are available, with subcutaneous now preferred because it significantly reduces the main dose-limiting side effect: peripheral neuropathy (numbness and tingling in hands and feet, affecting up to 30-40% of patients). While bortezomib remains a backbone of myeloma treatment worldwide, second-generation drugs in the same class (such as carfilzomib and ixazomib) offer different side effect profiles and are increasingly used alongside or instead of bortezomib for certain patient groups. Generic versions are now available, making it more accessible globally.

Clinical Trials

NCT00265928Phase IITerminated

Bortezomib and Rituximab in Treating Patients With Relapsed or Refractory B-Cell Non-Hodgkin's Lymphoma

University of Virginia
NCT00129207Phase ICompleted

Ketoconazole Administration: How it is Affected by the Body and Broken Down and How it Acts on the Body When Used With Velcade

Millennium Pharmaceuticals, Inc.
NCT00799539N/AUnknown

A Study to Further Assess Safety and Effectiveness Data of the Bortezomib(Velcade)/Melphalan/Prednisone (BMP) Regimen in Previously Untreated and Transplant Ineligible Multiple Myeloma Patients

Janssen-Ortho Inc., Canada
NCT01250808N/AUnknown

Technology Platform and System Construction of Clinical Evaluation Studies on New Drugs of Hematological Malignancy

Peking University
NCT00995059Phase IIWithdrawn

Bortezomib Before Donor Stem Cell Transplant in Treating Patients With Multiple Myeloma

Mayo ClinicEndpoint: Tolerability as assessed by CTCAE v3.0 (Phase I)
View all 1000 trials on ClinicalTrials.gov →

Regulatory Timeline

2003
Regulatory

FDA ORIG 1

2004
Regulatory

FDA SUPPL 4

2005
Regulatory

FDA SUPPL 6

2005
Regulatory

FDA SUPPL 7

2006
Regulatory

FDA SUPPL 9

2006
Regulatory

FDA SUPPL 10

2007
Regulatory

FDA SUPPL 13

2008
Regulatory

FDA SUPPL 15

2009
Regulatory

FDA SUPPL 18

2009
Regulatory

FDA SUPPL 20

2009
Regulatory

FDA SUPPL 19

2010
Regulatory

FDA SUPPL 23

2011
Regulatory

FDA SUPPL 28

2011
Regulatory

FDA SUPPL 30

2011
Regulatory

FDA SUPPL 29

2012
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FDA SUPPL 27

2012
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FDA SUPPL 31

2012
Regulatory

FDA SUPPL 32

2013
Regulatory

FDA SUPPL 33

2013
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FDA SUPPL 35

2013
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FDA SUPPL 36

2014
Regulatory

FDA SUPPL 37

2014
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FDA SUPPL 38

2014
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FDA SUPPL 39

2014
Regulatory

FDA SUPPL 40

2015
Regulatory

FDA SUPPL 41

2015
Regulatory

FDA SUPPL 42

2016
Regulatory

EMA Marketing Authorisation

2017
Regulatory

FDA SUPPL 43

2018
Regulatory

Health Canada Market Authorisation

2019
Regulatory

FDA SUPPL 44

2021
Regulatory

FDA SUPPL 45

2021
Regulatory

FDA SUPPL 46

2022
Regulatory

FDA ORIG 1

2022
Regulatory

FDA ORIG 1

2022
Regulatory

FDA ORIG 1

2022
Regulatory

FDA ORIG 1

2022
Regulatory

FDA ORIG 1

2022
Regulatory

FDA ORIG 1

2024
Regulatory

FDA ORIG 1

2024
Regulatory

FDA ORIG 1

2025
Regulatory

FDA ORIG 1

Related Compounds

Corticotropin

Approved
Repository ACTH Preparation

Corticotropin is marketed as H.P. Acthar Gel (currently ANI Pharmaceuticals). It carries approximately 19 FDA-labelled indications including infantile spasms (its strongest evidence base), nephrotic syndrome, multiple sclerosis relapses, and rheumatic disorders. Acthar Gel has been at the centre of major pricing and legal controversies. The price rose from approximately $40 per vial in 2001 to over $40,000, driven by successive acquisitions and orphan-like positioning despite broad labelling. The former manufacturer Mallinckrodt agreed to a $260 million settlement over antitrust concerns. Clinically, the strongest evidence supports its use in infantile spasms, where it is considered a first-line treatment. For most other indications, debate continues over whether it offers meaningful advantages over far less expensive oral corticosteroids.

Enfuvirtide

Approved
HIV Fusion Inhibitor (Peptide)

Enfuvirtide is marketed as Fuzeon (approved March 2003). It requires twice-daily subcutaneous injections, and injection-site reactions occur in nearly all patients (98%). In clinical trials (TORO-1 and TORO-2), enfuvirtide combined with an optimised background regimen achieved significantly greater viral suppression than background regimen alone in treatment-experienced patients. Enfuvirtide represented a major advance when HIV drug resistance was a more pressing clinical challenge, but its use has declined substantially with the arrival of more convenient oral antiretrovirals. The twice-daily injection burden, injection-site reactions, high cost, and complex manufacturing (it is one of the largest synthetic peptides manufactured at scale) have limited its role to a last-resort option for patients with highly resistant HIV.

Vancomycin

Approved
Glycopeptide Antibiotic

Vancomycin is marketed as Vancocin and Firvanq (approved 1958, with oral solution Firvanq approved 2018). It is the standard treatment for serious MRSA infections (bloodstream infections, endocarditis, pneumonia, bone infections) and is first-line for severe C. difficile colitis. Vancomycin requires therapeutic drug monitoring — blood levels must be checked regularly to ensure the dose is effective without causing kidney damage or hearing loss. The rise of vancomycin-resistant enterococci (VRE) and occasional vancomycin-intermediate S. aureus (VISA) strains represent ongoing challenges. Despite being nearly 70 years old, vancomycin remains irreplaceable for many serious infections, though newer alternatives like daptomycin and the lipoglycopeptides offer advantages in specific settings.