MT2 Inhibitors
5 drugsAbout MT2
MT2 (Melatonin Receptor Type 2) is a G protein-coupled receptor. It is a valuable target for pharmaceutical intervention due to its role in regulating circadian rhythms and sleep.
Human genetic studies provide strong validation for MT2 as a therapeutic target, with variants linked to type 2 diabetes (score 0.89) and diabetes mellitus (score 0.87). Gain-of-function variants are protective, suggesting activation-based therapies may be beneficial.
MT2 is targeted by 3 FDA-approved small molecule drugs, including HETLIOZ and TASIMELTEON. These drugs are used to treat conditions classified in the 'Other' therapeutic area.
MT2 Genetic Evidence Strong
MT2 has strong genetic support with a max score of 0.89 linking it to 28 diseases.
Strong genetic support suggests a higher likelihood of clinical success for MT2-targeting drugs.
💡 Why activation?
- • Gain-of-function variants reduce disease risk — enhancing activity may help
- • 100% directional consistency across 1 traits
- • Strong signal in endocrine system disease, nutritional or metabolic disease, phenotype pathways
Cross-Disease Effects
Trade-off: LowDirection of Effect
100% alignedEvidence Across Diseases
20 totalGWAS and other genetic studies link MTNR1B to 28 diseases.
Activating this target may be therapeutic
🔗 Colocalization Evidence 2 strong
max H4: 0.98eQTL/pQTL signals for MTNR1B 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 MT2 Drugs
The competitive landscape includes 2 companies with approved drugs: Apotex and VANDA PHARMS INC.
The limited number of players suggests relatively low barriers to entry in the MT2 drug market.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| TASIMELTEON | Teva | 2022 | 1 |
| HETLIOZ LQ | VANDA PHARMS INC | 2020 | 1 |
MT2 Drug Modality Landscape
Modalities
Routes of Administration
MT2 is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like biologics could provide a competitive advantage in the MT2 space.
MT2 Clinical Trials 49 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on MT2. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 13 | 13 | 0 | 0 | 100% |
| Phase 2 | 7 | 6 | 1 | 0 | 86% |
| Phase 3 | 13 | 5 | 5 | 3 | 50% |
| Phase 4 | 16 | 10 | 4 | 2 | 71% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Phase 3 Readout Calendar Pro
1 Phase 3 trial testing approved MT2 drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting MT2. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
MT2 Drug Approval Timeline (2005 - 2022)
The first MT2-targeting drug was approved in 2014, with the most recent approval in 2022.
The recent approval suggests continued interest and potential for further development in this area.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 4 companies competing
- • Market share by company
Full Drug Portfolio
- • All 5 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 5-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 23 (4 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 MT2. A trial counts if an approved drug acting on MT2 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.