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vemurafenib

Trade name: zelboraf

Small moleculeapprovedOrphan Drug FDA

Approved

Aug 17, 2011

Vemurafenib (trade name Zelboraf) is a low molecular weight, orally available kinase inhibitor. It inhibits of some mutated forms of BRAF serinethreonine kinase, including BRAF V600E and is indicated for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E mutation as detected by an FDA-approved test. Vemurafenib also inhibits other kinases in vitro such as CRAF, ARAF, wild-type BRAF, SRMS, ACK1, MAP4K5 and FGR at similar concentrations. Vemurafenib is not recommended for use in patients with wild-type BRAF melanoma. Zelboraf does not cure melanoma, but stops it's progression. Some 26% of patients in clinical trials developed a non melanoma form of skin cancer called cutaneous squamous cell carcinoma, which can usually be removed via relatively simple surgery. Other side effects include joint pain, rash, hair loss, fatigue, nausea, and skin sensitivity to sunlight. Patients taking Zelboraf must avoid sun exposure. It's not yet clear how long Zelboraf can increase melanoma survival. — NCATS

Clinical trial activity

148 trials · 115 clinical orgs · 2 marketing orgs

Phase 1
57
Phase 2
93
Phase 3
12
Phase 4
3

Earliest trial started Nov 1, 2006 (NCT00405587)

Timeline

2000s

  1. Jan 1, 2006

    Plexxikon — Earliest Phase 1 Sponsor(trial)

  2. Sep 1, 2006

    Plexxikon — IND Organization

  3. Sep 1, 2006

    Plexxikon — IND Organization

  4. Jan 1, 2009

    Roche — Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 1, 2010

    Roche — Earliest Phase 3 Sponsor(trial)

  2. Dec 20, 2010

    Orphan Drug Designation

  3. Aug 17, 2011

    Roche — Earliest FDA Approval

  4. Aug 17, 2011

    Roche — NDA Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedPriority reviewAug 17, 2011

Chemistry & pharmacology

Loading structure…

SMILES

CCCS(=O)(=O)NC1=C(F)C(C(=O)C2=CNC3=C2C=C(C=N3)C4=CC=C(Cl)C=C4)=C(F)C=C1
Mol. weight
489.922 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

First in class

Sources

Also known as

  • 1-propanesulfonamide, n-(3-((5-(4-chlorophenyl)-1h-pyrrolo(2,3-b)pyridin-3- yl)carbonyl)-2,4-difluorophenyl)-
  • braf(v600e) kinase inhibitor ro5185426
  • braf(v600e) kinase inhibitor ro5185426
  • n-(3-((5-(4-chlorophenyl)-1h-pyrrolo(2,3-b)pyridin-3-yl)carbonyl)-2,4- difluorophenyl)propane-1-sulfonamide
  • plx4032
  • plx4032
  • plx4032
  • plx 4032
  • plx-4032
  • plx-4032
  • plx-4032
  • plx-4032
  • plx-4032
  • r05185426
  • rg7204
  • rg 7204
  • rg-7204
  • rg-7204
  • rg-7204
  • ro5185426
  • ro5185426
  • ro 5185426
  • ro 51-85426
  • ro-5185426
  • ro-5185426
  • vemurafenib
  • vemurafenib
  • vemurafenib
  • vemurafenib
  • vemurafenib
  • vemurafenib
  • vemurafenib
  • vemurafenib
  • vemurafenib
  • vemurafenib
  • vermurafenib
  • zelboraf
  • zelboraf
  • zelboraf
  • zelboraf
  • zelboraf
  • zelboraf

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT06763029Phase 2Feb 26, 2025Fudan University
NCT06692491Phase 2Jan 1, 2025Peking University
NCT06561360Phase 2Sep 9, 2024Genentech, Memorial Sloan-Kettering Cancer Center
NCT06603376Phase 2Sep 1, 2024Second Military Medical University
NCT06008119Phase 3Nov 24, 2023Kechow Pharma
NCT05900219Phase 2Sep 24, 2023Chinese Academy of Medical Sciences, Kechow Pharma
NCT05768178Phase 2/Phase 3 (Phase 3)Mar 1, 2023Cancer Research UK, Roche, Royal Marsden Hospital NHS Trust, The Christie NHS Foundation Trust, University of Birmingham, University of Manchester
NCT05722886Phase 2/Phase 3 (Phase 3)Mar 1, 2023Cancer Research UK, Roche, Royal Marsden Hospital NHS Trust, The Christie NHS Foundation Trust, University of Birmingham, University of Manchester
NCT05238831Phase 2Dec 1, 2022Genentech, OHSU Knight Cancer Institute, Oregon Health and Science University
NCT05233332Phase 2Feb 28, 2022Kechow Pharma
NCT05388123Phase 2Jan 1, 2022Scripps
NCT05159245Phase 2Dec 10, 2021University of Helsinki
NCT05068752Phase 2Oct 28, 2021Bayer, Genentech, HonorHealth Research Institute
NCT05263453Phase 2Sep 6, 2021Kechow Pharma
NCT04801966N/AJun 30, 2021Peter MacCallum Cancer Centre
NCT05019534Phase 1May 1, 2021Sichuan University
NCT04943198Phase 2Apr 1, 2021Curie Institute, Institution of Mother and Child, Warsaw, Poland, Łukasiewicz Research Network, Wrocław University of Environmental and Life Sciences
NCT04551521Phase 2Nov 1, 2020German Cancer Research Center, NCT Studienzentrale
NCT04722575Phase 2Oct 12, 2020Clinical Research Technology S.r.l., Fondazione Melanoma Onlus
NCT04591431Phase 2Oct 7, 2020University of Roma La Sapienza
Showing 20 of 148 trials
Page 1 / 8

Organizations

Research & Development (115)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
RocheFor profit483342006
GenentechFor profit27542011
University of Texas at HoustonAcademic/Hospital9722012
Harvard UniversityAcademic/Hospital8322012
National Cancer Institute (NCI)Government7422012
Cornell UniversityAcademic/Hospital6432011
Bristol-Myers SquibbFor profit5222011
Kechow PharmaFor profit5532018
University of South FloridaAcademic/Hospital4422012
AstraZenecaFor profit3012016
BayerFor profit3012016
Fondazione Melanoma OnlusAcademic/Hospital3312014
Memorial Sloan-Kettering Cancer CenterAcademic/Hospital3322018
MerckFor profit3022013
Netherlands Cancer InstituteAcademic/Hospital3112014
PfizerFor profit3012016
Second Military Medical UniversityGovernment3312017
University of California, San FranciscoAcademic/Hospital3222012
University of PittsburghAcademic/Hospital3322013
Yale UniversityAcademic/Hospital3112013
115 organizations
Page 1 / 6

Marketing (2)

OrganizationOrg typeRelationshipDate
PlexxikonFor profitINDSep 1, 2006
RocheFor profitNDAAug 17, 2011