5-HT1B Inhibitors
9 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.
Strategic Insights
ℹ️ How we calculate- White space opportunity in Untreated Follicular Lymphoma with only 1 trials.
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 |
|---|---|---|---|
| FROVA | ENDO OPERATIONS | 2001 | 2 |
| IMITREX STATDOSE | GSK | 1992 | 2 |
| RIZATRIPTAN BENZOATE | Novartis | 2012 | 1 |
| ZEMBRACE SYMTOUCH | TONIX MEDS | 2016 | 1 |
| TOSYMRA | TONIX MEDS | 2019 | 1 |
| ONZETRA XSAIL | CURRAX | 2016 | 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 180 trials
Completion by Phase
| Phase | Total | Completed | Failed | Active | Completion |
|---|---|---|---|---|---|
| Phase 1 | 50 | 44 | 5 | 1 | 90% |
| Phase 2 | 45 | 36 | 8 | 1 | 82% |
| Phase 3 | 38 | 33 | 5 | 0 | 87% |
| Phase 4 | 47 | 38 | 5 | 4 | 88% |
Top Sponsors
By Modality
Top Conditions
Top Drugs
5-HT1B Drug Approval Timeline (1992 - 2019)
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
- • 8 companies competing
- • Market share by company
Full Drug Portfolio
- • All 9 approved drugs
- • Approval dates & indications
Genetic Validation
- • Full genetic evidence table
- • Effect sizes & directions
Approval Timeline
- • Full 9-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 98 clinical trials targeting 5-HT1B.
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