5-HT3 receptor Inhibitors
6 drugsAbout 5-HT3 receptor
The 5-HT3 receptor (serotonin receptor subtype 3) is a ligand-gated ion channel crucial for neuronal signaling in the nervous system. As a key player, it mediates fast synaptic transmission and modulates neurotransmitter release.
Human genetic studies provide moderate support for HTR3A as a therapeutic target, with variants linked to hypermobility syndrome (score 0.38). This suggests that modulating 5-HT3 receptor activity could impact disease risk.
The 5-HT3 receptor is targeted by 6 FDA-approved small molecule drugs, including ONDANSETRON HYDROCHLORIDE and LOTRONEX. These drugs span therapeutic areas such as CNS disorders and other conditions.
5-HT3 receptor Genetic Evidence Moderate
Genetic evidence offers moderate support, with a max score of 0.38 linking HTR3A to hypermobility syndrome.
Further research into high scoring indications 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 5-HT3 receptor Drugs
Six companies have approved drugs targeting the 5-HT3 receptor, including VIWIT PHARM and PF PRISM CV.
The relatively unconcentrated market suggests opportunities for new entrants with differentiated therapies.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| VARENICLINE TARTRATE | ZYDUS | 2021 | 1 |
| CHANTIX | PF PRISM CV | 2006 | 1 |
| TRINTELLIX | Takeda | 2013 | 1 |
5-HT3 receptor Drug Modality Landscape
Modalities
Routes of Administration
5-HT3 receptor 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.
5-HT3 receptor Clinical Trials 392 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on 5-HT3 receptor. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 55 | 45 | 8 | 2 | 85% |
| Phase 2 | 115 | 86 | 19 | 10 | 82% |
| Phase 3 | 88 | 70 | 11 | 7 | 86% |
| Phase 4 | 134 | 106 | 15 | 13 | 88% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
5-HT3 receptor Drug Approval Timeline (2000 - 2021)
The first drug was approved in 2000, with the most recent approval in 2021, spanning 22 years.
The continued approval of new drugs indicates sustained interest and potential for further innovation.
Pro Intelligence Preview
Deep insights for drug target analysis
Competitive Landscape
- • 6 companies competing
- • Market share by company
Full Drug Portfolio
- • All 6 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 6-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 203 (35 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 5-HT3 receptor. A trial counts if an approved drug acting on 5-HT3 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.