MAP2K1 Inhibitors
6 drugsAbout MAP2K1
MAP2K1, also known as MEK, MEK1, or MEK-1, is a protein kinase in the MAPK/ERK signaling pathway, regulating cell growth, proliferation, and survival. As such, MAP2K1 has become an important drug target, particularly in oncology.
Human genetic studies provide strong validation for MAP2K1 as a therapeutic target, with variants linked to rasopathy (score 0.94) and cardiofaciocutaneous syndrome 3 (score 0.91). Strong eQTL/pQTL signals further support MAP2K1's role in disease.
Six FDA-approved drugs target MAP2K1, including MEKINIST, COTELLIC, and MEKTOVI, all of which are small molecules. Four drugs are approved for oncology, while the remaining two target other therapeutic areas.
MAP2K1 Genetic Evidence Strong
MAP2K1 has strong genetic support with a max score of 0.94 linking it to rasopathy.
Strong genetic support suggests a higher likelihood of clinical success for MAP2K1-targeting drugs.
Evidence Across Diseases
13 totalGWAS and other genetic studies link MAP2K1 to 13 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for MAP2K1 colocalize with these GWAS traits, providing causal evidence that gene expression changes drive disease risk.
Understanding these scores
Association Score (0-1): Combines all evidence types (genetic, literature, drugs, animal models). Higher = more evidence linking target to disease. This is a ranking heuristic, not a confidence score.
L2G Score: Open Targets uses a machine learning model (Locus-to-Gene) to predict which gene is causal at each GWAS locus. L2G=0.5 means ~50% probability of being the causal gene. Only associations with L2G > 0.05 are included.
Odds Ratio (OR): From gene burden studies (UK Biobank, AstraZeneca PheWAS). Measures how loss-of-function variants affect disease risk. OR<1 = protective (inhibiting target may help), OR>1 = risk (losing function causes disease).
Beta (β): Effect size for continuous traits. β<0 = protective, β>0 = risk.
Clinical Translation (~1.8x): Based on Nelson et al. 2015: drug targets with genetic evidence have ~2x higher success rates in clinical trials. We estimate: Strong support (score ≥0.7) → ~1.8x, Moderate (0.3-0.7) → ~1.3x, Weak → baseline.
Colocalization (H4): Tests whether a GWAS signal and an eQTL/pQTL signal share the same causal variant. H4 is the posterior probability that both traits are associated AND share a causal variant. H4 > 0.8 = strong evidence that gene expression/protein levels drive disease risk. This links genetic variation → gene expression → disease, supporting the target-disease connection.
Top MAP2K1 Drugs
Six companies have approved drugs targeting MAP2K1, including Novartis, Roche, and SPRINGWORKS.
The presence of multiple players indicates a competitive market, requiring differentiated strategies for new entrants.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| COTELLIC | Roche | 2015 | 2 |
| GOMEKLI | SPRINGWORKS | 2025 | 1 |
| AVMAPKI FAKZYNJA CO-PACK (COPACKAGED) | VERASTEM INC | 2025 | 1 |
MAP2K1 Drug Modality Landscape
Modalities
Routes of Administration
MAP2K1 is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or PROTACs could provide a competitive advantage.
MAP2K1 Clinical Trials 465 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on MAP2K1. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 209 | 100 | 51 | 56 | 66% |
| Phase 2 | 217 | 73 | 43 | 101 | 63% |
| Phase 3 | 33 | 13 | 4 | 16 | 76% |
| Phase 4 | 6 | 0 | 1 | 5 | 0% |
Top Sponsors
By Modality
Top Conditions
Phase 3 Readout Calendar Pro
1 Phase 3 trial testing approved MAP2K1 drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting MAP2K1. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
MAP2K1 Drug Approval Timeline (2013 - 2025)
The first MAP2K1-targeting drug was approved in 2013, with the most recent in 2025.
The continued approval of new drugs suggests ongoing interest and potential in targeting MAP2K1.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 6 companies competing
- • Market share by company
Full Drug Portfolio
- • All 6 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 6-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 163 (34 companies)
- • Completion rates by condition
Full summary • All drugs • Genetic evidence • Trials • Timeline
How We Count Trials
- Trials: phase 1-4 interventional trials on ClinicalTrials.gov that started in 2008 or later and test an FDA-approved drug acting on MAP2K1. A trial counts if an approved drug acting on MAP2K1 is in any arm, including as a comparator, and a trial that tests two such drugs counts once. Trials that test only unapproved drugs are not counted. A trial listed as phase 1/2 counts as phase 1, and phase 2/3 as phase 2.
- Active: recruiting, not yet recruiting, enrolling by invitation, or active and no longer recruiting.
- Completion rate: of the trials that have ended, the share marked Completed rather than Terminated or Withdrawn. Completed means the trial ended as planned; it does not mean the drug worked. Suspended trials are not counted as ended.
- Stopped: terminated or withdrawn. Trials stop for many reasons, including slow enrolment and business decisions, not only safety or efficacy.
- Sponsors: the lead sponsor of each trial. Companies are the sponsors ClinicalTrials.gov classes as industry; the rest are universities, hospitals, cooperative groups, government bodies and individuals.