RARgamma Inhibitors
12 drugsAbout RARgamma
RARgamma (RARG) is a nuclear receptor that regulates gene expression by binding to DNA and modulating transcription. As a ligand-activated transcription factor, it influences various cellular processes.
Genetic evidence weakly supports RARG as a therapeutic target, with associations to cervical carcinoma (score 0.19), intelligence (0.12), and schizophrenia (0.10). There are also 3 strong eQTL/pQTL signals (max H4: 1.00).
Four FDA-approved drugs target RARgamma, including RETIN-A, ALTREN, TWYNEO, and ATRALIN, all of which are small molecules. These drugs are currently categorized within the "Other" therapeutic area.
RARgamma Genetic Evidence
Genetic evidence provides weak support for RARG, with a maximum score of 0.19 for cervical carcinoma.
Further research is needed to validate RARG as a drug target due to the weak genetic support.
Evidence Across Diseases
3 totalGWAS and other genetic studies link RARG to 3 diseases.
🔗 Colocalization Evidence 3 strong
max H4: 1.00eQTL/pQTL signals for RARG 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 RARgamma Drugs
Three companies have approved drugs targeting RARgamma: VALEANT PHARMS NORTH, DOW PHARM, and MAYNE PHARMA.
The market is relatively unconcentrated, suggesting opportunities for new entrants.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| AVAGE | CHARTWELL RX | 2000 | 2 |
| ATRALIN | DOW PHARM | 2007 | 1 |
| FABIOR | MAYNE PHARMA | 2012 | 1 |
| TWYNEO | MAYNE PHARMA | 2021 | 1 |
| AKLIEF | GALDERMA LABS LP | 2019 | 1 |
| SOHONOS | IPSEN | 2023 | 1 |
| ALTRENO | DOW PHARM | 2018 | 1 |
| DUOBRII | BAUSCH | 2019 | 1 |
| ARAZLO | BAUSCH | 2019 | 1 |
RARgamma Drug Modality Landscape
Modalities
Routes of Administration
RARgamma is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or peptides could diversify the therapeutic landscape.
RARgamma Clinical Trials 185 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on RARgamma. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 44 | 41 | 1 | 2 | 98% |
| Phase 2 | 42 | 29 | 7 | 5 | 81% |
| Phase 3 | 46 | 40 | 3 | 3 | 93% |
| Phase 4 | 53 | 43 | 6 | 4 | 88% |
Top Sponsors
By Modality
Top Conditions
Phase 3 Readout Calendar Pro
1 Phase 3 trial testing approved RARgamma drugs across all sponsors.
Coverage: trials whose intervention is an approved drug targeting RARgamma. Pre-approval candidates with development codes (e.g. AZD0901, MK-7240) are not yet linked. Anchored on CT.gov primary completion date.
RARgamma Drug Approval Timeline (1971 - 2023)
The first drug targeting RARgamma was approved in 1971 (RETIN-A), and the most recent in 2021 (TWYNEO).
The 51-year span indicates a sustained interest in targeting RARgamma, but also potential saturation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 7 companies competing
- • Market share by company
Full Drug Portfolio
- • All 12 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 12-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 86 (31 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 RARgamma. A trial counts if an approved drug acting on RARgamma 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.