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bortezomib

Trade name: velcade

Small moleculeapprovedOrphan Drug FDAFast Track FDA

Approved

May 13, 2003

Bortezomib is the therapeutic proteasome inhibitor. First, which is tested in humans. The boron atom in bortezomib binds the catalytic site of the 26S proteasome with high affinity and specificity. Bortezomib is approved in the U.S. for treating relapsed multiple myeloma and mantle cell lymphoma. The 26S proteasome degrades various proteins critical to cancer cell survival, such as cyclins, tumor suppressors, BCL-2, and cyclin-dependent kinase inhibitors. Inhibition of these degradations sensitizes cells to apoptosis. Bortezomib is a potent inhibitor of 26S proteasome, which sensitizes activity in dividing multiple myeloma and leukemic cells, thus inducing apoptosis. Most commonly reported adverse reactions (incidence ≥30%) in clinical studies include asthenic conditions, diarrhea, nausea, constipation, peripheral neuropathy, vomiting, pyrexia, thrombocytopenia, psychiatric disorders, anorexia and decreased appetite, neutropenia, neuralgia, leukopenia and anemia. Co-administration of ketoconazole, a potent CYP3A inhibitor, increased the exposure of bortezomib. Co-administration of melphalan-prednisone increased the exposure of bortezomib. However, this increase is unlikely to be clinically relevant. — NCATS

Clinical trial activity

916 trials · 475 clinical orgs · 26 marketing orgs

Phase 1
299
Phase 2
682
Phase 3
128
Phase 4
25

Earliest trial started Jul 1, 1999 (NCT00004002)

Timeline

1990s

  1. Jan 1, 1999

    Earliest Phase 1 Sponsor(trial)

2000s

  1. Jan 1, 2000

    Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2002

    Millennium Pharmaceuticals — Earliest Phase 3 Sponsor(trial)

  3. Jan 15, 2003

    Orphan Drug Designation

  4. May 13, 2003

    Millennium Pharmaceuticals — Earliest FDA Approval

  5. May 13, 2003

    Millennium Pharmaceuticals — NDA Secondary Org

  6. May 13, 2003

    Millennium Pharmaceuticals — NDA Organization

  7. May 13, 2003

    Takeda — Marketing Organization

  8. May 13, 2003

    Takeda — NDA Secondary Org

2010s

  1. Oct 20, 2016

    Actavis — NDA Secondary Org

  2. Oct 20, 2016

    Allergan PLC (2015) — NDA Secondary Org

  3. Apr 24, 2017

    Accord Research — Marketing Organization

  4. May 3, 2017

    Pharmasciences — Marketing Organization

  5. May 12, 2017

    Apotex — Marketing Organization

  6. Nov 6, 2017

    Fresenius — NDA Secondary Org

  7. Jul 12, 2018

    Hospira — NDA Secondary Org

  8. Nov 9, 2018

    Qilu Pharmaceutical Co., Ltd. — Marketing Organization

  9. Oct 4, 2019

    Dr. Reddy's Laboratories — Marketing Organization

  10. Oct 4, 2019

    Dr. Reddy's Laboratories — NDA Secondary Org

2020s

  1. May 7, 2021

    Jiangsu Hansoh Pharmaceutical Co., Ltd. — Marketing Organization

  2. May 21, 2021

    Waverley Pharma International Inc — Marketing Organization

  3. Jun 11, 2021

    Sandoz — Marketing Organization

  4. Jul 16, 2021

    Baxalta — Marketing Organization

  5. Aug 10, 2021

    Eugia Pharma — Marketing Organization

  6. May 2, 2022

    Hospira — Marketing Organization

  7. May 2, 2022

    Teva — Marketing Organization

  8. May 2, 2022

    Zydus Discovery DMCC — Marketing Organization

  9. May 2, 2022

    Fresenius — Marketing Organization

  10. May 2, 2022

    Pfizer — NDA Secondary Org

  11. May 2, 2022

    Ferring — Marketing Organization

  12. Jul 26, 2022

    Meitheal — Marketing Organization

  13. Jul 26, 2022

    MSN Laboratories — Marketing Organization

  14. Jul 26, 2022

    Pfizer — Marketing Organization

  15. Jul 26, 2022

    Novartis — Marketing Organization

  16. Jul 26, 2022

    Accord Research — NDA Secondary Org

  17. Jul 27, 2022

    Maia Pharms Inc — Marketing Organization

  18. Jul 27, 2022

    Maia Pharms Inc — NDA Secondary Org

  19. Oct 31, 2022

    Mylan — Marketing Organization

  20. Sep 26, 2023

    ScinoPharm Taiwan — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewAcceleratedFast trackMay 13, 2003

Chemistry & pharmacology

Loading structure…

SMILES

CC(C)C[C@H](NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)C2=CN=CC=N2)B(O)O
Mol. weight
384.237 g/mol
Chirality
Single Stereoisomer
Inorganic
No
Polymer
No
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

No

First in class

Sources

Also known as

  • [(1r)-3-methyl-1-({(2s)-3-phenyl-2-[(pyrazin-2-ylcarbonyl)amino]propanoyl}amino)butyl]boronic acid
  • [(1r)-3-methyl-1-({(2s)-3-phenyl-2-[(pyrazin-2-ylcarbonyl)amino]propanoyl}amino)butyl]boronic acid
  • bortezomib
  • bortezomib
  • bortezomib
  • bortezomib
  • bortezomib
  • bortezomib
  • bortezomib
  • bortezomib
  • bortezomib
  • bortezomib
  • bortizomib
  • jnj-26866138
  • ldp-341
  • ldp-341
  • ldp-341
  • ldp-341
  • ldp-341
  • ldp-341
  • n-[(1r)-1-(dihydroxyboryl)-3-methylbutyl]-n-(pyrazin-2-ylcarbonyl)-l-phenylalaninamide
  • n-[(1r)-1-(dihydroxyboryl)-3-methylbutyl]-n-(pyrazin-2-ylcarbonyl)-l-phenylalaninamide
  • ps-341
  • ps-341
  • ps-341
  • ps-341
  • radiciol
  • velcade
  • velcade
  • velcade
  • velcade
  • velcade

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07285239Phase 3May 31, 2026GlaxoSmithKline, Mayo Clinic, PrECOG, LLC.
NCT07247097Phase 2Apr 15, 2026Harvard University, Pfizer
NCT07072585Phase 2/Phase 3 (Phase 3)Mar 30, 2026National Cancer Institute (NCI)
NCT07222761Phase 3Jan 29, 2026Regeneron
NCT07227311Phase 2Jan 14, 2026GlaxoSmithKline
NCT07297329Phase 3Dec 31, 2025Sinocelltech Ltd.
NCT07224672Phase 2Dec 1, 2025GlaxoSmithKline
NCT07018050Phase 2Sep 12, 2025Qilu Pharmaceutical Co., Ltd.
NCT07025005Phase 4Aug 30, 2025Tanta University
NCT07085728Phase 2Aug 11, 2025Eastern Cooperative Oncology Group, ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI)
NCT06918002Phase 3Jul 9, 2025Intergroupe Francophone du Myelome, Pfizer
NCT07008638Phase 1/Phase 2 (Phase 2)Jul 7, 2025University of Minnesota
NCT07045909Phase 2Jun 30, 2025Clinica Universidad de Navarra, PETHEMA Foundation, University of Salamanca
NCT06799676Phase 1/Phase 2 (Phase 2)Feb 28, 2025Xiamen University
NCT06900647Phase 1Jan 1, 2025Sun Yat-Sen University
NCT06348147Phase 2Dec 31, 2024University of North Carolina at Chapel Hill
NCT06390319Phase 2Dec 31, 2024AbbVie, St. Jude Children's Hospital
NCT06656221Phase 2Dec 1, 2024Jiao Tong University
NCT06681922Phase 1/Phase 2 (Phase 2)Sep 23, 2024Northwell Health
NCT06572813Phase 1/Phase 2 (Phase 2)Sep 1, 2024Zhejiang University
Showing 20 of 916 trials
Page 1 / 46

Organizations

Research & Development (475)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
National Cancer Institute (NCI)Government2019541999
Millennium PharmaceuticalsFor profit1493252001
Johnson and JohnsonFor profit843652004
Janssen Pharmaceutica NVFor profit41442004
Harvard UniversityAcademic/Hospital393342003
CelgeneFor profit31832005
University of Texas at HoustonAcademic/Hospital312632000
Mayo ClinicAcademic/Hospital301631999
Cornell UniversityAcademic/Hospital231852000
Hoosier Cancer Research NetworkAcademic/Hospital232242001
GlaxoSmithKlineFor profit19932006
NovartisFor profit19742008
PETHEMA FoundationAcademic/Hospital171732004
Chinese Academy of Medical SciencesAcademic/Hospital161242010
MerckFor profit15532005
Emory UniversityAcademic/Hospital141132003
Bristol-Myers SquibbFor profit13742007
Ohio State UniversityAcademic/Hospital13732001
City of Hope National Medical CenterAcademic/Hospital11732002
European Myeloma NetworkAcademic/Hospital11922006
475 organizations
Page 1 / 24

Marketing (41)

OrganizationOrg typeRelationshipDate
Accord ResearchFor profitSYNJul 26, 2022
Accord ResearchFor profitMKTGApr 24, 2017
Accord ResearchFor profitNDA2Jul 26, 2022
ActavisFor profitNDA2Oct 20, 2016
Allergan PLC (2015)For profitNDA2Oct 20, 2016
ApotexFor profitSYNMay 2, 2022
ApotexFor profitMKTGMay 12, 2017
BaxaltaFor profitMKTGJul 16, 2021
Dr. Reddy's LaboratoriesFor profitSYNOct 4, 2019
Dr. Reddy's LaboratoriesFor profitSYNOct 4, 2019
Dr. Reddy's LaboratoriesFor profitMKTGOct 4, 2019
Dr. Reddy's LaboratoriesFor profitNDA2Oct 4, 2019
Eugia PharmaFor profitMKTGAug 10, 2021
FerringFor profitMKTGMay 2, 2022
FreseniusFor profitNDA2Nov 6, 2017
FreseniusFor profitMKTGMay 2, 2022
HospiraFor profitMKTGMay 2, 2022
HospiraFor profitNDA2Jul 12, 2018
Jiangsu Hansoh Pharmaceutical Co., Ltd.For profitMKTGMay 7, 2021
MSN LaboratoriesFor profitMKTGJul 26, 2022
Maia Pharms IncFor profitMKTGJul 27, 2022
Maia Pharms IncFor profitNDA2Jul 27, 2022
MeithealFor profitMKTGJul 26, 2022
Millennium PharmaceuticalsFor profitNDA2May 13, 2003
Millennium PharmaceuticalsFor profitNDAMay 13, 2003
MylanFor profitMKTGOct 31, 2022
NovartisFor profitMKTGJul 26, 2022
PfizerFor profitNDA2May 2, 2022
PfizerFor profitMKTGJul 26, 2022
PharmasciencesFor profitMKTGMay 3, 2017
Qilu Pharmaceutical Co., Ltd.For profitSYNMay 2, 2022
Qilu Pharmaceutical Co., Ltd.For profitMKTGNov 9, 2018
SandozFor profitMKTGJun 11, 2021
SandozFor profitSYNJul 26, 2022
ScinoPharm TaiwanFor profitMKTGSep 26, 2023
TakedaFor profitMKTGMay 13, 2003
TakedaFor profitNDA2May 13, 2003
TevaFor profitMKTGMay 2, 2022
Waverley Pharma International IncFor profitSYNOct 11, 2022
Waverley Pharma International IncFor profitMKTGMay 21, 2021
Zydus Discovery DMCCFor profitMKTGMay 2, 2022