Nicotinic acid receptor Inhibitors
4 drugsAbout Nicotinic acid receptor
The Nicotinic acid receptor (HCAR2) is a drug target. Its gene symbol is HCAR2 (Ensembl ID: ENSG00000182782).
Human genetic studies provide moderate support for HCAR2 as a therapeutic target, with variants linked to metabolic syndrome (score 0.60), physical activity (score 0.51), and breast cancer (score 0.49). There are also 20 strong eQTL/pQTL signals (max H4: 1.00).
HCAR2 is targeted by 4 FDA-approved small molecule drugs: DIROXIMEL FUMARATE, VUMERITY, TECFIDERA, and BAFIERTAM. These drugs are marketed by Biogen, BANNER LIFE SCIENCES, and ZYDUS, and are indicated for CNS and other therapeutic areas.
Nicotinic acid receptor Genetic Evidence Moderate
Genetic evidence offers moderate support for HCAR2, with a max score of 0.60.
Further research is needed to validate HCAR2 as a target for metabolic syndrome.
Evidence Across Diseases
9 totalGWAS and other genetic studies link HCAR2 to 9 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 1.00eQTL/pQTL signals for HCAR2 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 Nicotinic acid receptor Drugs
Three companies have approved drugs targeting HCAR2.
The market is relatively concentrated, suggesting high barriers to entry.
Nicotinic acid receptor Drug Modality Landscape
Modalities
Routes of Administration
Nicotinic acid receptor is amenable to small molecule drugs, with oral options available for convenient dosing.
Consider exploring alternative modalities to differentiate from existing therapies.
Nicotinic acid receptor Clinical Trials 63 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on Nicotinic acid receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 12 | 9 | 3 | 0 | 75% |
| Phase 2 | 14 | 6 | 3 | 5 | 67% |
| Phase 3 | 19 | 10 | 5 | 4 | 67% |
| Phase 4 | 18 | 11 | 6 | 1 | 65% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Nicotinic acid receptor Drug Approval Timeline (2013 - 2025)
The first drug was approved in 2013, and the most recent in 2025.
The approval timeline indicates continued interest in this target.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 3 companies competing
- • Market share by company
Full Drug Portfolio
- • All 4 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 4-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 28 (7 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 Nicotinic acid receptor. A trial counts if an approved drug acting on Nicotinic acid receptor 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.