5-HT3R Inhibitors
4 drugsAbout 5-HT3R
The 5-HT3 receptor (5-HT3R), also known as the serotonin receptor subtype 3, is a ligand-gated ion channel crucial in neuronal signaling. It mediates fast synaptic transmission in the central and peripheral nervous systems.
Human genetic studies provide moderate support for 5-HT3R as a therapeutic target, with variants linked to hypermobility syndrome (score 0.38). Higher receptor activity is associated with increased disease risk, suggesting that antagonists may be beneficial.
5-HT3R is targeted by 4 FDA-approved small molecule drugs, including AKYNZEO, SUSTOL, ALOSETRON HYDROCHLORIDE and ONDANSETRON HYDROCHLORIDE. These drugs are utilized across various therapeutic areas categorized as 'other'.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Pancreatic Diseases with only 1 trials.
Human Genetic Evidence Moderate
Genetic evidence offers moderate support, with a maximum score of 0.38 for hypermobility syndrome.
Further investigation into the genetic associations could reveal novel therapeutic opportunities.
Evidence Across Diseases
4 totalGWAS and other genetic studies link HTR3A to 4 diseases.
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
Four companies have approved drugs targeting 5-HT3R, including Hikma and HELSINN HLTHCARE.
The relatively low number of players suggests a moderately concentrated market with potential entry opportunities.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| SUSTOL | HERON THERAPS INC | 2016 | 2 |
Drug Modality Landscape
Modalities
Routes of Administration
5-HT3R is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or biologics could provide a competitive advantage.
Clinical Trials 189 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 41 | 35 | 5 | 1 | 88% |
| Phase 2 | 53 | 39 | 11 | 3 | 78% |
| Phase 3 | 46 | 40 | 4 | 2 | 91% |
| Phase 4 | 49 | 38 | 5 | 6 | 88% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
Drug Approval Timeline (2000 - 2021)
Nausea and vomiting from highly emetogenic chemotherapy
The first drug was approved in 2006 (ONDANSETRON HYDROCHLORIDE), and the most recent in 2016 (SUSTOL).
The approval timeline indicates a potentially maturing market with limited recent innovation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 4 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
- • 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 96 clinical trials targeting 5-HT3R.
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