Slide 1: First-in-Human Study of First-in-Class TRPM3 Antagonist BHV-2100 for Migraine and Pain
First-in-Human Study Evaluating the Safety, Tolerability, and Pharmacokinetics of the First-in-Class TRPM3 Antagonist BHV-2100 in Development for Migraine and Pain Volkan Granit, MD, MSc1; Richard Bertz, PhD1; Andrew Lucas, PharmD, MS, MS2; Eric Ashbrenner, MS1; Mary Donohue, MS1, Patricia Mydlow, B
Slide 2: Rationale for TRPM3 Antagonism as a Treatment for Migraine
Rationale for TRPM3 Antagonism as a Treatment for Migraine • Strong mechanistic evidence supports the role of TRPM3 in neurogenic inflammation and sensitization of the trigeminovascular system, which underlie migraine pathogenesis1 • TRPM3 receptors sensitize and activate the nociceptors of the trig
Slide 3: BHV-2100: A First-in-Class Orally Administered TRPM3 Antagonist
BHV-2100: A First-in-Class Orally Administered TRPM3 Antagonist in Clinical Development for Migraine and Pain BHV-2100 is being developed with an improved profile compared to existing pain medications and other TRP antagonists TRPV1 Effects on thermal sensation and thermoregulation hampered clinical
Slide 4: BHV-2100 Phase 1 First-in-Human SAD/MAD Study
BHV-2100 Phase 1 First-in-Human SAD/MAD Study Objectives Population: • Healthy adult males and females aged 18-55 years Evaluate safety and tolerability of single and multiple dose oral administration of BHV-2100 Study Design: • Phase 1, randomized, placebo controlled, sequential SAD/MAD study Evalu
Slide 5: BHV-2100 Demonstrates Rapid Absorption and Sustained Concentrations
BHV-2100 Demonstrates Rapid Absorption and Sustained Concentrations Mean Concentration vs. Time Profiles of Single Oral Doses of BHV-2100 • Tmax 1.5 to 2 hours • T1/2 ranges from 8 to 12 hours • The PK of BHV-2100 was approximately dose-proportional at doses up to 150 mg • At the lowest dose of 25 m
Slide 6: BHV-2100 PK Not Significantly Impacted by Food or Acid-Reducing Agent
BHV-2100 PK Not Significantly Impacted by Food or Acid-Reducing Agent Mean Concentration vs. Time Profiles of Single Oral Doses of Mean Concentration vs. Time Profile of Single Oral Doses of 150 mg BHV-2100 With and Without Food 150 mg BHV-2100 With and Without Famotidine High-fat meal delayed Tmax
Slide 7: BHV-2100: Safe and Well-Tolerated to Date in Healthy Adults
BHV-2100: Safe and Well-Tolerated to Date in Healthy Adults SAFETY AND TOLERABILITY • No dose limiting toxicities • No SAEs Placebo BHV-2100 • No severe TEAEs; 1 moderate TEAE not SAD Cohorts (pooled) (N=9) (N=30) related to study drug; all other TEAEs mild TEAE’s in ≥ 2 subjects n (%) n (%) • No cl
Slide 8: BHV-2100: A Clinical-Stage TRPM3 Antagonist for Migraine and Pain
BHV-2100: A Clinical-Stage TRPM3 Antagonist for Migraine and Pain TRPM3 represents a novel target for the treatment of migraine and pain BHV-2100 is a first-in-class, orally administered, peripherally-restricted and selective TRPM3 antagonist BHV-2100 demonstrated rapid absorption and sustained conc
Slide 9: Thank you!
Thank you!