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Drug

Binimetinib

Approved · EMA
ClassDual specificity mitogen-activated protein kinase kinase 1 inhibitorEmerging researchLate-stage developmentRising momentum

Also known as Mektovi.

RxNorm2049122ChEMBLCHEMBL3187723ATCL01EE03UNII181R97MR71
4
Research papers
28
Active clinical trials
2
Protein targets
1
Regulatory events
Latest activity
beta

Recent clinical, regulatory, research and industry developments relating to this drug.

Phase I/Ib Study of Binimetinib, a MEK Inhibitor, in Combination With Pembrolizumab in Patients With Advanced Non-Small Cell Lung Cancer (NSCLC)

Clinical trial2026-08-01Primary completion · ClinicalTrials.gov

Molecular Analysis for Therapy Choice (MATCH)

Clinical trial2026-07-31Results expected Q4 2026 · ClinicalTrials.gov

A PHASE 1, OPEN-LABEL, DOSE ESCALATION AND DOSE EXPANSION STUDY TO EVALUATE THE SAFETY, TOLERABILITY, PHARMACOKINETICS, AND ANTI TUMOR ACTIVITY OF PF-07799933 (ARRY-440) AS A SINGLE AGENT AND IN COMBINATION THERAPY IN PARTICIPANTS 16 YEARS AND OLDER WITH ADVANCED SOLID TUMORS WITH BRAF ALTERATIONS

Clinical trial2026-07-09Results expected Q2 2028 · ClinicalTrials.gov

Molecular Analysis for Combination Therapy Choice (ComboMATCH)

Clinical trial2026-07-09Results expected Q3 2030 · ClinicalTrials.gov

FOLFOX in Combination With Binimetinib as 2nd Line Therapy for Patients With Advanced Biliary Tract Cancers With MAPK Pathway Alterations: A ComboMATCH Treatment Trial

Clinical trial2026-07-02Results expected Q4 2026 · ClinicalTrials.gov

Phase 2 Trial for Binimetinib for Patients With Relapsed/Refractory BRAF Wild Type Hairy Cell Leukemia and Variant

Clinical trial2026-06-18Results expected Q2 2028 · ClinicalTrials.gov

Palbociclib and Binimetinib in RAS-Mutant Cancers: A ComboMATCH Treatment Trial

Clinical trial2026-06-17Results expected Q3 2026 · ClinicalTrials.gov

Molecular profiling of BRAF-V600E-mutant metastatic colorectal cancer in the phase 3 BEACON CRC trial.

Research2024-09-23Nature medicine

Efficacy and safety of the combination of encorafenib/cetuximab with or without binimetinib in patients with BRAF V600E-mutated metastatic colorectal cancer: an AGEO real-world multicenter study.

Research2024-09-09ESMO open

Encorafenib, Binimetinib, and Cetuximab in <i>BRAF</i> V600E-Mutated Colorectal Cancer.

Research2019-09-30The New England journal of medicine

Approval: Mektovi (EMA)

Regulatory2018-09-20EMA

Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF-mutant melanoma (COLUMBUS): a multicentre, open-label, randomised phase 3 trial.

Research2018-03-21The Lancet. Oncology

Profile

Identifiers & mechanism

Canonical identifiers, marketed brand names and mechanism, resolved across RxNorm, ChEMBL and ATC.

Canonical name
Binimetinib
Aliases & brands
Mektovi
RxNorm CUI
2049122
ChEMBL ID
CHEMBL3187723
ATC codes
L01EE03
UNII
181R97MR71
Primary mechanism
Dual specificity mitogen-activated protein kinase kinase 1 inhibitor
Regulatory jurisdictions
ema

Pharmacology & targets

2 targets

Known molecular targets and mechanisms supported by curated pharmacology databases.

Dual specificity mitogen-activated protein kinase kinase 1
MAP2K1 · Q02750
INHIBITORDual specificity mitogen-activated protein kinase kinase 1 inhibitor
Dual specificity mitogen-activated protein kinase kinase 2
MAP2K2 · P36507
INHIBITORDual specificity mitogen-activated protein kinase kinase 2 inhibitor

Regulatory timeline

1 event

The complete regulatory record, grouped by authority — approvals, safety advisories and label changes. Each authority shows its most recent events; expand one to read its full history.

Earliest approval
2018-09-20
Latest approval
2018-09-20
Authorities
EMA
Total events
1
emaEuropean Medicines Agency· 1 event
2018-09-20Approval
Approval: Mektovi (EMA)
Indication: MelanomaBinimetinib in combination with encorafenib is indicated for the treatment of adult patients with unresectable or metastatic melanoma with a BRAF V600 mutation.Non-small… Show full indication

MelanomaBinimetinib in combination with encorafenib is indicated for the treatment of adult patients with unresectable or metastatic melanoma with a BRAF V600 mutation.Non-small cell lung cancer (NSCLC)Binimetinib in combination with encorafenib is indicated for the treatment of adult patients with advanced non-small cell lung cancer with a BRAF V600E mutation.

Evidence ↗

Contains information from the European Medicines Agency (European Medicines Agency), © EMA, reused under CC BY 4.0.

Clinical trials

76 trials

The current development programme across all trial phases — status mix, phase distribution and the late-stage studies shaping the evidence base.

Development programme
CLINICALTRIALS.GOV · LIVE REGISTRY
76
registered trials across all phases
LATEST COMPLETION 2026
28
Active studies
12
Recruiting
4
Late-stage (III+)
23
Completed
25
Discontinued
PHASE DISTRIBUTIONn = 76
Early Phase 12Phase 120Phase 1 / 211Phase 239Phase 33Phase N / A1

Late-stage studies

Phase III+ trials still open or recently active — where late-stage evidence is being generated.

Molecular Targeted Maintenance Therapy Versus Standard of Care in Advanced Biliary Cancer: an International, Randomised, Controlled, Open-label, Platform Phase 3 Trial

RecruitingPH IIIUNICANCERn=8002028

A PHASE 3, RANDOMIZED, DOUBLE-BLIND STUDY OF ENCORAFENIB AND BINIMETINIB PLUS PEMBROLIZUMAB VERSUS PLACEBO PLUS PEMBROLIZUMAB IN PARTICIPANTS WITH BRAF V600E/K MUTATION-POSITIVE METASTATIC OR UNRESECTABLE LOCALLY ADVANCED MELANOMA

Active, not recruitingPH IIIPfizern=2572026

A Multicenter, Randomized, Open-label, 3-Arm Phase 3 Study of Encorafenib + Cetuximab Plus or Minus Binimetinib vs. Irinotecan/Cetuximab or Infusional 5-Fluorouracil (5-FU)/Folinic Acid (FA)/Irinotecan (FOLFIRI)/Cetuximab With a Safety Lead-in of Encorafenib + Binimetinib + Cetuximab in Patients With BRAF V600E-mutant Metastatic Colorectal Cancer

CompletedPH IIIPfizern=7022022

Recent completions

Trials that read out recently, adding to the completed evidence base.

Binimetinib Plus Hydroxychloroquine in KRAS Mutant Metastatic Pancreatic Cancer

CompletedPH IM.D. Anderson Cancer Centern=342026

Phase I Study of the CDK4/6 Inhibitor Palbociclib (PD-0332991) in Combination With the MEK Inhibitor Binimetinib (MEK162) for Patients With Advanced KRAS Mutant Non-Small Cell Lung Cancer

CompletedPH IDana-Farber Cancer Instituten=342025

A Phase 2, Open-label Study of Encorafenib + Binimetinib in Patients With BRAFV600-mutant Non-small Cell Lung Cancer

CompletedPH IIPfizern=982025

Overcoming Primary Resistance to Immunotherapy in Metastatic Melanoma Patients by Transient Addition of BRAF and MEK Inhibitors Followed by Pembrolizumab: A Pivotal Open Label, Single-site Study

CompletedPH IIDr. Ronnie Shapiran=12025

Neoadjuvant Encorafenib, Binimetinib and Cetuximab for Patients With BRAF V600E Mutated/pMMR Localized Colorectal Cancer

CompletedPH IIAIO-Studien-gGmbHn=22025

Combination of MEK Inhibitor Binimetinib and CDK4/6 Inhibitor Palbociclib in KRAS and NRAS Mutant Metastatic Colorectal Cancers

CompletedPH IIAcademic and Community Cancer Research Unitedn=1022024

Research activity

4 papers

Key research shaping understanding of this drug, combining the latest publications with the most influential evidence.

Publications over time
20182024
Major research themes8
Mutation3Antineoplastic Combined Chemotherapy Protocols2Colorectal Neoplasms2Proto-Oncogene Proteins B-raf2Benzimidazoles1Carbamates1Cetuximab1Gene Expression Profiling1
Journals, researchers & institutions
Top journals
  • ESMO open1
  • Nature medicine1
  • The Lancet. Oncology1
  • The New England journal of medicine1
Leading researchers
  • Ciardiello F2
  • Desai J2
  • Kopetz S2
  • Sandor V2
  • Tabernero J2
  • Van Cutsem E2
  • Yaeger R2
  • Yoshino T2
Leading institutions
free-text, unnormalised
  • Begin Teaching Military Hospital1
  • Cancer Center1
  • Centre Hospitalier Universitaire de Bordeaux1
  • Centre Hospitalier Universitaire de Toulouse1
  • Centre Léon Bérard1
  • Charité-Universitätsmedizin Berlin1

Related diseases

2 conditions

Regulator-approved indications and conditions co-mentioned with this drug across the research literature. Number shows shared papers.

Related drugs

3 matches

Drugs sharing diseases, protein targets and literature with this one. Ranked by graph evidence (shared targets + diseases weighted above co-mentions).

Encorafenib

Studied across 4 of the same disease areas as Binimetinib in the shared literature.

4 shared diseases4 shared papers
Irinotecan

Studied across 2 of the same disease areas as Binimetinib in the shared literature.

2 shared diseases1 shared paper
Vemurafenib

Studied across 2 of the same disease areas as Binimetinib in the shared literature.

2 shared diseases1 shared paper
References & data sources
  • RxNorm (U.S. National Library of Medicine) — drug identity
  • ChEMBL (EMBL-EBI) & UniProt — pharmacology and targets
  • Europe PMC — research literature
  • ClinicalTrials.gov — clinical trials
  • Regulatory event sources are credited in the Regulatory Timeline above.