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.
Strategic Insights
ℹ️ How we calculate- phase2 represents biological uncertainty with 59% completion.
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 |
|---|---|---|---|
| MEKTOVI | ARRAY BIOPHARMA INC | 2018 | 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 496 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 223 | 107 | 52 | 61 | 67% |
| Phase 2 | 234 | 77 | 48 | 109 | 62% |
| Phase 3 | 32 | 13 | 4 | 15 | 76% |
| Phase 4 | 7 | 0 | 1 | 6 | 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
- • Competition: High (15 sponsors)
- • Success rates by condition
Full summary • All drugs • Genetic evidence • Trials • Timeline
How We Calculate These Metrics
Target Attractiveness Score
A 0-100 score based on trial activity, sponsor diversity, and completion rates. Calculated from 372 clinical trials targeting MAP2K1.
Completion rate: Percentage of trials that reached their planned endpoint. Trials terminated early, withdrawn, or suspended are not counted—these often indicate safety issues, lack of efficacy, or strategic pivots.
- Highly Attractive (80+): High trial activity, many sponsors, strong completion rates
- Attractive (60-79): Good trial activity and validation
- Moderate (40-59): Moderate interest from sponsors
- Low (under 40): Limited trial activity or validation concerns
Strategic Insights
Auto-generated insights based on trial analytics including competition intensity, white space opportunities, modality shifts, and failure patterns. We analyze trial sponsors, phases, indications, and outcomes.
Risk Signals
- High Competition: Many sponsors competing for this target (may reduce market opportunity)
- High Failure Risk: Low trial completion rates suggest development challenges
- Low Validation: Limited trial activity or poor outcomes indicate uncertain viability
- White Space Available: Underexplored indications present opportunities