Summary
Binimetinib has reached the approved stage (maximum clinical phase 4) for at least one indication, so its use in Colorectal Cancer would be drug repurposing rather than first-in-human development. This does not mean it is approved for Colorectal Cancer. ClinicalTrials.gov lists 8 registered trials linking Binimetinib to Colorectal Cancer: 3 are currently recruiting; 3 have completed; 2 are terminated, withdrawn, suspended or of unknown status. The most advanced is Phase 2 (NCT06207656). The largest enrolment is 336 participants (NCT03947385). Registration activity spans 2009 to 2024. The literature layer holds 11 publications for this pair: 2 Cochrane reviews, 1 systematic review, 3 randomised controlled trial publications and 5 clinical trial publications. Publication years run from 2021 to 2026. Because at least one synthesis-level source exists (systematic review, meta-analysis or Cochrane review), this pair has been assessed beyond single studies, although the synthesis may concern a different indication.
The RepurpOS disease-intelligence file for Colorectal Cancer ranks 1212 candidate therapeutics from Open Targets, ChEMBL, DGIdb and PubMed; only a minority carry direct clinical evidence, and this page covers one of those. Spontaneous remission context recorded for the condition: Essentially zero; 5-year survival stage I: ~90% (resectable); stage IV: ~15% overall, ~20-30% with modern therapy and liver metastasis resection.
Evidence table
| Evidence tier | A · Strong |
|---|---|
| Evidence score | 71.5 (trials 21.5, literature 30.0, tier 15, approved bonus 5.0) |
| Registered trials | 8 total: 3 recruiting, 0 active / not yet recruiting, 3 completed, 2 other |
| Linked publications | 11 (5 clinical trial publications, 3 randomised controlled trial publications, 2 Cochrane reviews, 1 systematic review) |
| Agent type | Drug (Small molecule) |
| Development stage (any indication) | Approved |
| Mechanism / class | Not recorded |
| Data sources | DGIdb |
| Linked via biomarker / target | APC |
How the evidence score is calculated
- Each registered trial scores by status (recruiting / active / enrolling 3, completed 2.5, not yet recruiting 2, unknown 1, terminated / withdrawn / suspended 0.5) plus a phase bonus (phase 3-4 +2, phase 2 +1, phase 1 +0.5). The trial component is capped at 30.
- Each literature item scores by design (Cochrane review 5, meta-analysis 4, systematic review 3, RCT 3, clinical trial publication 2, curated reference 1.5, other PubMed record 1). The literature component is capped at 30.
- The existing evidence tier adds 15 (A / Strong), 10 (B / Moderate), 5 (C / Preliminary) or 0 (D / Anecdotal).
- Agents approved for any indication (max clinical phase 4) add 5, because an approved agent has an established safety profile that lowers the barrier to repurposing trials.
- The score ranks what has been studied, not what works. It does not read effect sizes or directions of effect.
Registered clinical trials
| NCT ID | Title | Status | Phase | Enrolment |
|---|---|---|---|---|
| NCT06207656 | Study to Evaluate the Efficacy and Safety of Cetuximab in Combination with Encorafenib Plus Binimetinib As Induction Treatment in BRAF V600E Mutated MSS Initially Resectable or Potentially Resectable Advanced Colorectal Cancer 2024 | recruiting | Phase 2 | 70 |
| NCT06229340 | Leflunomide or Combination of MEK Inhibitor and Hydroxychloroquine for Refractory Patients With RAS Mutations 2023 | recruiting | Phase 2 | 20 |
| NCT03374254 | Safety and Efficacy of Pembrolizumab (MK-3475) Plus Binimetinib Alone or Pembrolizumab Plus Chemotherapy With or Without Binimetinib in Metastatic Colorectal Cancer (mCRC) Participants (MK-3475-651/KEYNOTE-651) 2018 | completed | Phase 1 | 116 |
| NCT00959127 | A Study of ARRY-438162 (MEK162) in Patients With Advanced Cancer 2009 | completed | Phase 1 | 93 |
| NCT02613650 | A Trial of mFOLFIRI With MEK162 in Patients With Advanced RAS (HRAS, NRAS, or KRAS) Positive Metastatic Colorectal Cancers 2016 | completed | Phase 1 | 25 |
| NCT04870034 | Binimetinib and Palbociclib Before Surgery for the Treatment of Operable KRAS-Positive Lung, Colorectal, or Pancreatic Cancer 2024 | withdrawn | Early Phase 1 | — |
| NCT03947385 | Study of IDE196 in Patients With Solid Tumors Harboring GNAQ/11 Mutations or PRKC Fusions 2019 | recruiting | PHASE1, PHASE2 | 336 |
| NCT01562899 | A Study of MEK162 and AMG 479 in Patients With Selected Solid Tumors 2012 | terminated | PHASE1, PHASE2 | 77 |
Published literature
- Clinical trial publication Safety and efficacy of lapatinib, binimetinib, and vinorelbine for RAS mutant metastatic colorectal cancer: results of the RASTRIC Phase I/II trialHuismans MA, Gort EH, van der Heijden LT et al. · British journal of cancer · 2026 · PMID 41946829
- Cochrane review Safety and Efficacy of Triple Therapy Containing Encorafenib, Cetuximab, and Binimetinib for BRAF V600E-Mutated Colorectal Cancer: a Systematic Review and Meta-AnalysisAnsab M, Ramzan NUH, Ishaque G et al. · Journal of gastrointestinal cancer · 2026 · PMID 41677963
- Clinical trial publication A Phase Ia/b study of MEK1/2 inhibitor binimetinib with MET inhibitor crizotinib in patients with RAS mutant advanced colorectal cancer (MErCuRIC)Aroldi F, Elez E, André T et al. · BMC cancer · 2025 · PMID 40211189
- Cochrane review The efficacy of targeted therapy and/or immunotherapy with or without chemotherapy in patients with colorectal cancer: A network meta-analysisGuo H, Miao L, Yu C · European journal of pharmacology · 2025 · PMID 39716565
- Clinical trial publication Molecular profiling of BRAF-V600E-mutant metastatic colorectal cancer in the phase 3 BEACON CRC trialKopetz S, Murphy DA, Pu J et al. · Nature medicine · 2024 · PMID 39313594
- Clinical trial publication A Phase II Study of Potentiation of Pembrolizumab with Binimetinib and Bevacizumab in Refractory Microsatellite-Stable Colorectal CancerLentz RW, Friedrich TJ, Blatchford PJ et al. · Clinical cancer research : an official journal of the American Association for Cancer Research · 2024 · PMID 38869830
- Clinical trial publication Pembrolizumab Plus Binimetinib With or Without Chemotherapy for MSS/pMMR Metastatic Colorectal Cancer: Outcomes From KEYNOTE-651 Cohorts A, C, and EChen EX, Kavan P, Tehfe M et al. · Clinical colorectal cancer · 2024 · PMID 38653648
- Randomized controlled trial Binimetinib in combination with nivolumab or nivolumab and ipilimumab in patients with previously treated microsatellite-stable metastatic colorectal cancer with RAS mutations in an open-label phase 1b/2 studyElez E, Cubillo A, Alfonso PG et al. · BMC cancer · 2024 · PMID 38600471
- Randomized controlled trial Quality of life with encorafenib plus cetuximab with or without binimetinib treatment in patients with BRAF V600E-mutant metastatic colorectal cancer: patient-reported outcomes from BEACON CRCKopetz S, Grothey A, Van Cutsem E et al. · ESMO open · 2022 · PMID 35653981
- Systematic review Systematic review of randomised clinical trials and observational studies for patients with RAS wild-type or BRAF(V600E)-mutant metastatic and/or unresectable colorectal cancerGarcía-Alfonso P, Lièvre A, Loupakis F et al. · Critical reviews in oncology/hematology · 2022 · PMID 35344913
- Randomized controlled trial Encorafenib Plus Cetuximab as a New Standard of Care for Previously Treated BRAF V600E-Mutant Metastatic Colorectal Cancer: Updated Survival Results and Subgroup Analyses from the BEACON StudyTabernero J, Grothey A, Van Cutsem E et al. · Journal of clinical oncology : official journal of the American Society of Clinical Oncology · 2021 · PMID 33503393
Mechanism and notes
No mechanism of action is recorded for this pair in the source databases.
OSMF's existing evidence tier for this pair is A (Strong), derived from the strength of the disease association recorded in DGIdb, in this case via the biomarker or target APC. The tier describes how well the drug-disease link is documented, not how well the drug works.
Frequently asked questions
Is Binimetinib approved for Colorectal Cancer?
Binimetinib has reached the approved stage (maximum clinical phase 4) for at least one indication, so its use in Colorectal Cancer would be drug repurposing rather than first-in-human development. This does not mean it is approved for Colorectal Cancer. Approval status for the specific indication should always be confirmed with the relevant regulator and prescribing information.
Is Binimetinib in clinical trials for Colorectal Cancer?
ClinicalTrials.gov lists 8 registered trials linking Binimetinib to Colorectal Cancer: 3 are currently recruiting; 3 have completed; 2 are terminated, withdrawn, suspended or of unknown status. The most advanced is Phase 2 (NCT06207656). The largest enrolment is 336 participants (NCT03947385). Registration activity spans 2009 to 2024.
What does the evidence show for Binimetinib in Colorectal Cancer?
Binimetinib has both completed registered trials and synthesis-level publications linked to Colorectal Cancer. That is the strongest profile in this database, but the summaries here do not extract effect sizes, so read the linked reviews for direction and magnitude of benefit. OSMF's existing evidence tier for this pair is A (Strong), derived from the strength of the disease association recorded in DGIdb, in this case via the biomarker or target APC. The tier describes how well the drug-disease link is documented, not how well the drug works.
Cite this page
Data: ClinicalTrials.gov, PubMed, Open Targets, ChEMBL, DGIdb and the OSMF therapeutic agent database. Last updated 2026-07-05. Page built 2026-10-07.