LAG-3 Inhibitors
1 drugsAbout LAG-3
LAG-3 (Lymphocyte Activation Gene 3) is an immune checkpoint receptor on T cells that inhibits their activation. By acting as a brake on the immune system, LAG-3 prevents excessive immune responses and potential damage to healthy tissues.
Blocking LAG-3 can unleash T cell anti-tumor activity, allowing them to target cancer cells. Human genetic studies provide weak support for LAG-3 as a therapeutic target, with variants linked to Hashimoto's thyroiditis (score 0.27).
LAG-3 is targeted by one FDA-approved antibody drug, OPDUALAG, developed by Bristol-Myers Squibb. This drug has two indications and was first approved in 2022, representing the sole approved therapy in this space.
LAG-3 Genetic Evidence
Genetic evidence provides weak support for LAG-3, with a max score of 0.27 for Hashimoto's thyroiditis.
Low genetic support suggests prioritizing indications with strong clinical rationale or biomarker evidence.
Evidence Across Diseases
7 totalGWAS and other genetic studies link LAG3 to 7 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for LAG3 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 LAG-3 Drugs
Bristol-Myers Squibb is the only company with an approved LAG-3 targeting drug.
High market concentration suggests significant entry barriers, requiring strong differentiation strategies.
LAG-3 Drug Modality Landscape
Modalities
Routes of Administration
Only one approved drug targets LAG-3, using antibody modality.
Explore alternative modalities like small molecules or bispecifics to differentiate from existing therapies.
LAG-3 Clinical Trials 1,443 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on LAG-3. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 584 | 250 | 148 | 178 | 63% |
| Phase 2 | 707 | 251 | 137 | 312 | 65% |
| Phase 3 | 138 | 59 | 16 | 63 | 79% |
| Phase 4 | 14 | 7 | 1 | 6 | 88% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Phase 3 Readout Calendar Pro
8 Phase 3 trials testing approved LAG-3 drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting LAG-3. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
LAG-3 Drug Approval Timeline (2022 - 2022)
The first and only LAG-3 targeting drug was approved in 2022.
Recent approval indicates an emerging market, but also a risk of rapid saturation if new drugs follow.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 1 companies competing
- • Market share by company
Full Drug Portfolio
- • All 1 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 1-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 486 (155 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 LAG-3. A trial counts if an approved drug acting on LAG-3 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.