Small Molecule · BHV-2100
BHV-2100
Potential first-in-class, potent, selective, orally administered TRPM3 (transient receptor potential melastatin 3) channel antagonist in development as a non-opioid, non-sedating treatment for acute migraine and pain. Originated through Biohaven's license and research collaboration with KU Leuven.
Also known as: BHV-2100
- Modality
- Small molecule
- Mechanism
- TRPM3 antagonist
- Highest phase
- Phase 2
- Lead indication
- Migraine
- Developer
- Biohaven Ltd. (BHVN)
- Trials
- 1 tracked · 60 sites
- Next catalyst
- 1H 2025 — Topline data (Migraine)
Mechanism of action
BHV-2100 is a first-in-class, orally bioavailable antagonist of TRPM3, a calcium-permeable cation channel expressed in trigeminal- and dorsal-root-ganglion sensory neurons and implicated in nociceptive/neuroinflammatory pain signaling and CGRP release. It inhibited human, mouse and rat TRPM3 with IC50 values in the 1-10 nM range and inhibited pregnenolone-sulfate-evoked calcium influx in human iPSC-derived sensory neurons with an IC50 of ~10.9 nM, with >1000-fold selectivity over a broad panel of other ion channels and receptors.
| Target | Action | Affinity |
|---|---|---|
| TRPM3primaryTRPM3 | Antagonist | IC50 10.9 nMⓘ |
Formulations
| Formulation | Route | Regimen | Pharmacokinetics |
|---|---|---|---|
| BHV-2100 oral Oral single doses; Phase 2 acute-migraine study evaluates 75 mg and 150 mg single doses. Phase 1 SAD tested single doses up to 500 mg in healthy adults. | Oral | Single dose | t½ 10 h · Tmax 1.75 h |
Development timeline
- UpcomingTopline proof-of-concept efficacy data for BHV-2100 in the acute treatment of migraine (Phase 2, NCT06603623)↗
- NCT06603623 reached primary completion (CT.gov primary completion date 2025-03-24; overall status Completed) with 647 actual participants enrolled. Topline efficacy not yet publicly reported in primary sources as of 2025-05-12.
- Biohaven initiated the pivotal Phase 2 acute migraine trial (NCT06603623); study start date 2024-10-10. Announced 2024-09-30 as ~575 patients across ~60 US sites at 75 mg and 150 mg vs placebo.↗
BHV-2100 for Migraine
Phase 2ActiveMigraine indication →
BHV-2100 is in a pivotal, registration-enabling Phase 2 trial (NCT06603623) for the acute treatment of migraine, evaluating 75 mg and 150 mg oral doses vs placebo with FDA-accepted co-primary endpoints of pain freedom and freedom from most bothersome symptom at 2 hours. The trial reached primary completion on 2025-03-24; topline efficacy had not been publicly reported as of Biohaven's Q1 2025 update (2025-05-12), which guided migraine proof-of-concept data for 1H 2025. Status set to active pending the readout.
Readouts
- 1H 2025AnticipatedTopline dataNCT06603623
Topline proof-of-concept efficacy data for BHV-2100 in the acute treatment of migraine (Phase 2, NCT06603623) ↗
Clinical trials
NCT06603623Phase 2Completedn=647
Phase 2 Double-Blind, Randomized, Placebo Controlled, Efficacy and Safety Trial of BHV-2100 for the Acute Treatment of Migraine
Identifiers
Sources
- BHV-2100, A First-In-Class TRPM3 Antagonist for the Treatment of Pain (AAN 2024 oral presentation) — Biohaven Ltd. / American Academy of Neurology 2024
- Biohaven Initiates Pivotal Trial of Novel Investigational Drug for Treatment of Migraine — Biohaven Ltd. / PR Newswire (2024-09-30)
- Biohaven Reports First Quarter 2025 Financial Results and Recent Business Developments — Biohaven Ltd. / PR Newswire (2025-05-12)
- Efficacy and Safety Trial of BHV-2100 for the Acute Treatment of Migraine (NCT06603623) — ClinicalTrials.gov / U.S. National Library of Medicine