CDEK
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binimetinib

Trade name: mektovi

Small moleculeapprovedOrphan Drug FDA

Approved

Jun 27, 2018

Binimetinib (MEK162) is an oral small-molecule with potential antineoplastic activity. It is a selective mitogen-activated protein kinase 1 and 2 (MEK1/2) inhibitor, a key protein kinase in the RAS/RAF/MEK/ERK pathway, which regulates several key cellular activities including proliferation, differentiation, migration, survival and angiogenesis. Inappropriate activation of this pathway has been shown to occur in many cancers, in particular through mutations in BRAF, KRAS and NRAS. MEK162 at 6 mg/kg, BID combined with BEZ235 (dual PI3K/mTOR inhibitor) resulted in a significant reduction of tumor growth in immunodeficient mice injected with MCF7 cells. There are three ongoing Phase 3 trials with binimetinib in advanced cancer patients: NEMO (NRAS-mutant melanoma), COLUMBUS (encorafenib in combination with binimetinib in BRAF-mutant melanoma) and BEACON CRC (encorafenib, binimetinib and cetuximab in BRAF-mutant colorectal cancer). — NCATS

Clinical trial activity

122 trials · 110 clinical orgs · 3 marketing orgs

Phase 1
58
Phase 2
87
Phase 3
8
Phase 4
2

Earliest trial started Mar 1, 2008 (NCT00650767)

Timeline

2000s

  1. Jan 1, 2008

    Array BioPharma — Earliest Phase 2 Sponsor(trial)

  2. Jan 1, 2009

    Array BioPharma — Earliest Phase 1 Sponsor(trial)

2010s

  1. Jan 1, 2013

    Array BioPharma — Earliest Phase 3 Sponsor(trial)

  2. Nov 19, 2013

    Orphan Drug Designation

  3. Jun 27, 2018

    Array BioPharma — Earliest FDA Approval

  4. Jun 27, 2018

    Array BioPharma — NDA Secondary Org

  5. Jun 27, 2018

    Array BioPharma — NDA Organization

2020s

  1. Apr 26, 2024

    Alembic — Marketing Organization

  2. Dec 10, 2024

    Teva — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedJun 27, 2018

Chemistry & pharmacology

Loading structure…

SMILES

CN1C=NC2=C1C=C(C(=O)NOCCO)C(NC3=C(F)C=C(Br)C=C3)=C2F
Mol. weight
441.227 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Delivery
Oral
Availability
Prescription Only

Oral

Yes

Parenteral

No

Topical

No

Sources

Also known as

  • arry-162
  • arry-162
  • arry-438162
  • arry-438162
  • arry-438162
  • binimetinib
  • binimetinib
  • binimetinib
  • binimetinib
  • binimetinib
  • binimetinib
  • mek162
  • mek162
  • mek162
  • mek 162
  • mek 162
  • mek-162
  • mek-162
  • nvp-mek162
  • nvp-mek162

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07092410Phase 4Aug 31, 2025Pierre Fabre, SRH Wald-Klinikum Gera GmbH
NCT06887088Phase 2May 29, 2025Grupo Español Multidisciplinar de Melanoma, Hospital General Universitario Gregorio Marañon, MFAR Clinical Research, Pierre Fabre, Regeneron
NCT05615818Phase 3Jul 18, 2024Accord Research, Belgian Group of Digestive Oncology, Cancer Research UK, Center Eugene Marquis, Institut Mutualiste Montsouris, National Cancer Institute, France, Otsuka, Pierre Fabre, Servier, UNICANCER, Université catholique de Louvain, University of London, Zymeworks Inc.
NCT06207656Phase 2Apr 16, 2024Merck, Pierre Fabre, Spanish Cooperative Group for the Treatment of Digestive Tumours (TTD)
NCT05926960Phase 2Jun 13, 2023Merck, Pfizer
NCT06159478Phase 2Mar 29, 2023National Cancer Center, Japan, Ono Pharmaceuticals
NCT05286788Phase 2Dec 31, 2022Ohio State University, University of Colorado
NCT05554354Phase 2Dec 9, 2022National Cancer Institute (NCI), NRG Oncology
NCT05554367Phase 2Dec 9, 2022National Cancer Institute (NCI)
NCT05564377Phase 2Dec 9, 2022ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI)
NCT05564403Phase 2Dec 9, 2022National Cancer Institute (NCI)
NCT05810740Phase 1Aug 31, 2022Biotrial, Pierre Fabre
NCT05510895Phase 2Aug 22, 2022AIO-Studien-gGmbH, Merck Serono, Pierre Fabre, University of Hamburg
NCT05355701Phase 1Jul 5, 2022Pfizer
NCT05203172Phase 4Jul 5, 2022Pfizer
NCT05304546Phase 2Jun 30, 2022Tel Aviv University
NCT05195632Phase 2Jun 2, 2022Pierre Fabre, Sun Yat-Sen University
NCT05340621Phase 1/Phase 2 (Phase 2)May 11, 2022Harvard University, OnKure, Inc.
NCT05270044Phase 3May 2, 2022European Organisation for Research and Treatment of Cancer, Pierre Fabre
NCT05111561Phase 1Jan 17, 2022National Cancer Institute (NCI), University of Texas at Houston
Showing 20 of 122 trials
Page 1 / 7

Organizations

Research & Development (110)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Array BioPharmaFor profit492732008
National Cancer Institute (NCI)Government21922014
Pierre FabreFor profit18642016
PfizerFor profit17842014
Harvard UniversityAcademic/Hospital5322016
University of Texas at HoustonAcademic/Hospital5422014
Bristol-Myers SquibbFor profit4012017
ECOG-ACRIN Cancer Research GroupAcademic/Hospital4112015
MerckFor profit4132018
University of California, San FranciscoAcademic/Hospital4422019
University of TorontoAcademic/Hospital4422015
Cornell UniversityAcademic/Hospital3322013
University of California, Los AngelesAcademic/Hospital3322015
University of South FloridaAcademic/Hospital3322013
Academic and Community Cancer Research UnitedAcademic/Hospital2212019
BiotrialFor profit2012021
European Organisation for Research and Treatment of CancerAcademic/Hospital2122018
Grupo Español Multidisciplinar de MelanomaAcademic/Hospital2212019
Hospital General Universitario Gregorio MarañonAcademic/Hospital2012019
Institut Gustave RoussyAcademic/Hospital2012018
110 organizations
Page 1 / 6

Marketing (4)

OrganizationOrg typeRelationshipDate
AlembicFor profitMKTGApr 26, 2024
Array BioPharmaFor profitNDA2Jun 27, 2018
Array BioPharmaFor profitNDAJun 27, 2018
TevaFor profitMKTGDec 10, 2024