5-HT 1F Inhibitors
4 drugsAbout 5-HT 1F
The 5-HT1F receptor is a serotonin receptor subtype expressed in the central nervous system. It is implicated in neuronal signaling and has been explored as a drug target for CNS conditions.
Human genetic studies provide moderate support for 5-HT1F as a therapeutic target, with variants linked to prostate carcinoma (score 0.55) and intestinal disease (score 0.53). Colocalization analysis reveals 20 strong eQTL/pQTL signals.
5-HT1F is targeted by 3 FDA-approved small molecule drugs, including ELETRIPTAN HYDROBROMIDE (Relpax) and ALMOTRIPTAN MALATE, all indicated for CNS conditions. Chartwell RX, Upjohn, and Ajanta Pharma Ltd. are key players in this space.
5-HT 1F Genetic Evidence Moderate
Genetic evidence offers moderate support, with a maximum score of 0.55 linking HTR1F to prostate carcinoma.
Further investigation of the top genetic associations could reveal novel therapeutic opportunities.
Evidence Across Diseases
20 totalGWAS and other genetic studies link HTR1F to 26 diseases.
🔗 Colocalization Evidence 20 strong
max H4: 0.99eQTL/pQTL signals for HTR1F 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 5-HT 1F Drugs
Chartwell RX, Upjohn, and Ajanta Pharma Ltd. are the companies with approved 5-HT1F targeting drugs.
The relatively unconcentrated market suggests opportunities for new entrants with differentiated products.
5-HT 1F Drug Modality Landscape
Modalities
Routes of Administration
5-HT 1F 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-HT 1F Clinical Trials 31 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on 5-HT 1F. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 21 | 21 | 0 | 0 | 100% |
| Phase 2 | 3 | 3 | 0 | 0 | 100% |
| Phase 3 | 7 | 5 | 2 | 0 | 71% |
Top Sponsors
By Modality
5-HT 1F Drug Approval Timeline (2002 - 2017)
The first drug was approved in 2002 (Relpax), and the most recent in 2017 (ELETRIPTAN HYDROBROMIDE).
The approval timeline indicates a potentially maturing market, requiring innovative strategies for future success.
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
- • Sponsors: 3 (3 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-HT 1F. A trial counts if an approved drug acting on 5-HT 1F 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.