Rimegepant (BHV-3000) – for acute treatment of Migraine
Rimegepant, the lead product candidate, is an orally available, selective and potent small molecule CGRP receptor antagonist. Based on the data from its Phase 2b clinical trial, we believe rimegepant has the potential to be a best-in-class CGRP receptor antagonist for the acute treatment of migraine with the ability to address important unmet needs, such as durable efficacy across all four traditional migraine symptoms and reduced incidence of headache recurrence, without contraindications or warnings in patients with cardiovascular disease or hypertension, since its CGRP-based mechanism of action does not involve active vasoconstriction (the constriction of blood vessels), in contrast to the triptans which are contraindicated in patients with cardiovascular disease and hypertension.
In a Phase 2b, double-blind, randomized, placebo-controlled, dose-ranging clinical trial of 812 patients completed by BMS rimegepant dosed at 75 mg was observed to have statistically significant improvement as compared to placebo on all four key migraine symptoms—pain, nausea, photophobia and phonophobia—the four traditional endpoints identified by the U.S. Food and Drug Administration, or FDA, for drug approval for treatment of migraine. To our knowledge based on publicly available information, rimegepant is the only small molecule CGRP receptor antagonist currently in development that has achieved statistically significant improvement on all four of the traditional endpoints within a single study. Rimegepant also was observed to have statistically significant effects on two-to-24 hour and two-to-48 hour pain freedom (head pain intensity level reported as “no pain”) and two-to-24 hour pain relief (no pain or mild pain), as compared to placebo. In these measurements, benefits were present at two hours after dosing and persisted through 24 hours after dosing and, with respect to pain freedom, persisted through 48 hours after dosing. This durable improvement is significant because other common migraine medications, such as triptans, have been linked to the headache recurrence.
As of December 31, 2016, approximately 687 subjects have received single or multiple doses of rimegepant, and no treatment-related serious adverse events have been observed and adverse events have generally been mild and transient in nature. In the second half of 2017, we plan to commence two Phase 3 clinical trials of rimegepant for the acute treatment of migraine, with topline results expected in the first half of 2018.