5-HT1B Inhibitors
16 drugsAbout 5-HT1B
The 5-HT1B receptor is a G protein-coupled receptor that binds serotonin, regulating neuronal activity and vascular function in the brain. As a serotonin receptor subtype, it modulates neurotransmission and plays a role in CNS processes.
Human genetic studies provide strong support for 5-HT1B as a therapeutic target, with variants linked to mathematical ability (score 0.76) and smoking initiation (score 0.69). This genetic evidence, combined with clinical efficacy, validates the receptor's significance.
Nine FDA-approved drugs target 5-HT1B, including SUMATRIPTAN and FROVATRIPTAN, all of which are small molecules. These drugs, developed by 8 companies like GSK and Lannett Co. Inc., are used to treat CNS conditions.
5-HT1B Genetic Evidence Strong
HTR1B has strong genetic support with a max score of 0.76 linked to mathematical ability.
The strong genetic support suggests a higher likelihood of success in clinical trials for novel 5-HT1B-targeting drugs.
Evidence Across Diseases
20 totalGWAS and other genetic studies link HTR1B to 21 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-HT1B Drugs
Eight companies have approved drugs targeting 5-HT1B, with Lannett Co Inc and GSK among the top players.
The presence of multiple players indicates a competitive market, requiring a differentiated strategy for new entrants.
| Drug | Company | Approved | Indications |
|---|---|---|---|
| FROVATRIPTAN SUCCINATE | PHARMOBEDIENT | 2014 | 2 |
| SUMATRIPTAN | PERRIGO UK FINCO | 2016 | 2 |
| ZOLMITRIPTAN | Apotex | 2013 | 1 |
| RIZATRIPTAN BENZOATE | Apotex | 2012 | 1 |
| SYMBRAVO | AXSOME | 2025 | 1 |
| MAXALT-MLT | Merck | 1998 | 1 |
| RELPAX | UPJOHN | 2002 | 1 |
| ALMOTRIPTAN MALATE | Viatris | 2015 | 1 |
| TOSYMRA | TONIX MEDS | 2019 | 1 |
| MAXALT | Merck | 1998 | 1 |
| TRUDHESA | IMPEL PHARMS | 2021 | 1 |
| ONZETRA XSAIL | AZURITY | 2016 | 1 |
| ATZUMI | SATSUMA PHARMS | 2025 | 1 |
5-HT1B Drug Modality Landscape
Modalities
Routes of Administration
5-HT1B is amenable to small molecule drugs, with oral options available for convenient dosing.
Exploring alternative modalities like antibodies or peptides could provide a competitive advantage in this space.
5-HT1B Clinical Trials 238 trials
Phase 1-4 trials started in 2008 or later that test an FDA-approved drug acting on 5-HT1B. Source: ClinicalTrials.gov. How we count
Completion by Phase
| Phase | Total | Completed | Stopped | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 66 | 59 | 5 | 2 | 92% |
| Phase 2 | 54 | 44 | 9 | 1 | 83% |
| Phase 3 | 58 | 49 | 8 | 1 | 86% |
| Phase 4 | 60 | 43 | 8 | 9 | 84% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
5-HT1B Drug Approval Timeline (1998 - 2025)
The first 5-HT1B-targeting drug was approved in 1992, with the most recent approval in 2019.
The approval timeline suggests a mature market, potentially indicating limited whitespace for new targets within the same indication.
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Competitive Landscape
- • 14 companies competing
- • Market share by company
Full Drug Portfolio
- • All 16 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 16-drug timeline
- • First-of-modality markers
Clinical Trials Analysis
- • Sponsors: 131 (61 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-HT1B. A trial counts if an approved drug acting on 5-HT1B 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.