RARgamma Inhibitors
11 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.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Acute Promyelocytic Leukemia With t(15;17)(q24.1;q21.2); PML-RARA with only 1 trials.
Human 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 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 Modality Landscape
Modalities
Routes of Administration
RARgamma is druggable by small molecules, though no oral formulations are currently approved.
Exploring alternative modalities like antibodies or peptides could diversify the therapeutic landscape.
Clinical Trials 187 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 53 | 41 | 5 | 7 | 89% |
| Phase 2 | 42 | 25 | 3 | 11 | 89% |
| Phase 3 | 39 | 30 | 3 | 6 | 91% |
| Phase 4 | 53 | 45 | 6 | 2 | 88% |
Top Sponsors
By Modality
Drug Approval Timeline (1971 - 2021)
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.
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Deep insights for drug target analysis
Competitive Landscape
- • 7 companies competing
- • Market share by company
Full Drug Portfolio
- • All 11 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 11-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Competition: High (15 sponsors)
- • White space: 10 underexplored indications
- • 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 85 clinical trials targeting RARgamma.
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