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trametinib

Trade name: mekinist

Small moleculeapprovedOrphan Drug FDAFast Track FDA

Approved

May 29, 2013

Trametinib is a reversible and specific inhibitor of mitogen-activated protein kinase kinases MEK1 and MEK2 which are involved in a RAS/RAF/MEK/ERK signaling pathway and control cell growth, survival, and differentiation. By inhibiting MEK1 and MEK2 trametinib blocks dual phosphorylation of ERK1/2 and stops cell cycling. In addition, trametinib blocks BRAF pathway in the cells with BRAF V600E mutations. Trametinib (as a single agent and in combination with dabrafenib) is approved for the treatment of unresectable or metastatic melanoma with BRAF V600E or V600K mutations. — NCATS

Clinical trial activity

245 trials · 171 clinical orgs · 4 marketing orgs

Phase 1
111
Phase 2
159
Phase 3
14
Phase 4
5

Earliest trial started Jul 1, 2008 (NCT00687622)

Timeline

2000s

  1. Jan 1, 2008

    GlaxoSmithKline — Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2009

    GlaxoSmithKline — Earliest Phase 2 Sponsor(trial)

2010s

  1. Jan 1, 2010

    GlaxoSmithKline — Earliest Phase 3 Sponsor(trial)

  2. Dec 20, 2010

    Orphan Drug Designation

  3. May 29, 2013

    GlaxoSmithKline — Earliest FDA Approval

  4. May 29, 2013

    GlaxoSmithKline — NDA Organization

  5. May 29, 2013

    Novartis — NDA Secondary Org

  6. May 29, 2013

    Novartis — Marketing Organization

2020s

  1. Aug 6, 2024

    SciTech Development, LLC — Marketing Organization

  2. Aug 6, 2024

    Hikma — Marketing Organization

Indications

Approved for

Studied for

Mechanism of action

Approval history

  • approvedFast trackMay 29, 2013

Chemistry & pharmacology

Loading structure…

SMILES

CC(=O)Nc1cccc(-n2c(=O)n(C3CC3)c(=O)c3c(Nc4ccc(I)cc4F)n(C)c(=O)c(C)c32)c1
Mol. weight
615.4 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No
Availability
Prescription Only

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • daborafenib plus trametinib
  • gsk1120212
  • gsk1120212
  • gsk1120212
  • gsk1120212
  • gsk1120212
  • gsk 1120212
  • gsk 1120212
  • gsk 1120212
  • gsk-1120212
  • gsk1120212b
  • gsk1120212b
  • gsk1120212b
  • gsk1120212b
  • gsk1120212b
  • gsk1120212b
  • jtp74057
  • jtp 74057
  • jtp-74057
  • jtp-74057
  • mekinist
  • mekinist
  • mekinist
  • mekinist
  • mekinist
  • tmt212
  • trametinib
  • trametinib
  • trametinib
  • trametinib
  • trametinib
  • trametinib
  • trametinib
  • trametinib
  • trametinib
  • trametinib
  • trametinib dimethyl sulfoxide
  • trametinib dimethyl sulfoxide
  • trametinib dimethyl sulfoxide
  • trametinib dimethyl sulfoxide
  • trametinib dimethyl sulfoxide
  • trametinibum
  • trametinibum

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT07110246Phase 2Nov 7, 2025Rising Tide Foundation, University of California, San Francisco
NCT07072403Phase 1/Phase 2 (Phase 2)Jul 7, 2025Sichuan University
NCT07010393Phase 4Jul 1, 2025Fujian Medical University
NCT07022834Phase 2Jun 1, 2025Sichuan University
NCT06962254Phase 1May 10, 2025China Medical University
NCT06895928Phase 2Mar 28, 2025Hengrui Therapeutics, Inc.
NCT06819605Phase 2/Phase 3 (Phase 3)Mar 1, 2025Jiao Tong University
NCT06967155Phase 2Mar 1, 2025Blokhin's Russian Cancer Research Center, Clinuvel Pharmaceuticals Limited, Government of Russia, The Loginov MCSC MHD
NCT06804824Phase 1Feb 25, 2025Vividion Therapeutics
NCT06754930Phase 1/Phase 2 (Phase 2)Feb 18, 2025Suzhou Suncadia Biopharmaceuticals Co., Ltd.
NCT06712875Phase 1/Phase 2 (Phase 2)Dec 31, 2024Northwestern University
NCT06563999Phase 2Dec 1, 2024Sun Yat-Sen University
NCT06739395Phase 2Nov 1, 2024Tianjin Medical University
NCT06475989Phase 3Sep 13, 2024ECOG-ACRIN Cancer Research Group, National Cancer Institute (NCI)
NCT06555237Phase 2Aug 1, 2024Medical University of Warsaw
NCT06456138Phase 1/Phase 2 (Phase 2)Jul 1, 2024BeOne Medicines, Jiangsu Chia-tai Tianqing Pharmaceutical Co.,Ltd, Jiao Tong University, Novartis
NCT06582745Phase 2Jun 24, 2024Cook Children's Medical Center
NCT06346067Phase 3Apr 29, 2024Erasca, Inc.
NCT06362694Phase 2Mar 25, 2024Saint-Petersburg State Medical University
NCT06054191Phase 2Feb 1, 2024Sun Yat-Sen University
Showing 20 of 245 trials
Page 1 / 13

Organizations

Research & Development (171)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
GlaxoSmithKlineFor profit544432008
NovartisFor profit541952010
National Cancer Institute (NCI)Government453232012
University of Texas at HoustonAcademic/Hospital131022012
Harvard UniversityAcademic/Hospital12622013
ECOG-ACRIN Cancer Research GroupAcademic/Hospital8222015
National Comprehensive Cancer NetworkAcademic/Hospital8022011
University of California, San FranciscoAcademic/Hospital6622013
University of TorontoAcademic/Hospital6322013
Bristol-Myers SquibbFor profit5222015
Cornell UniversityAcademic/Hospital5322013
Jiao Tong UniversityAcademic/Hospital5442020
MerckFor profit5122014
AmgenFor profit4222014
Melanoma Institute AustraliaAcademic/Hospital4322014
Ohio State UniversityAcademic/Hospital4222012
Southwest Oncology GroupAcademic/Hospital4012013
University of California, Los AngelesAcademic/Hospital4322014
Free University of BrusselsAcademic/Hospital3312014
Memorial Sloan-Kettering Cancer CenterAcademic/Hospital3312018
171 organizations
Page 1 / 9

Marketing (5)

OrganizationOrg typeRelationshipDate
GlaxoSmithKlineFor profitNDAMay 29, 2013
HikmaFor profitMKTGAug 6, 2024
NovartisFor profitNDA2May 29, 2013
NovartisFor profitMKTGMay 29, 2013
SciTech Development, LLCFor profitMKTGAug 6, 2024