Novel Oral CGRP Inhibitor Formulation Approved by FDA

March 4, 2020

A new orally disintegrating tablet formulation of CGRP inhibitor rimegepant may restore normal function within 1 hour in adults with migraine, according to the manufacturer.

FDA approval of the first orally disintegrating calcitonin gene-related peptide (CGRP) receptor antagonist for the acute treatment of migraine in adults was announced by Biohaven Pharmaceuticals in a company statement on February 27.

According to the company, a single dose of rimegapant orally disintegrating tablet (Nurtec ODT) can return patients to normal function within 1 hour and efficacy is sustained for up to 48 hours for many patients. 

Nearly 40 million people in the US experience migraine and the World Health Organization classifies migraine as one of the 10 most disabling medical illnesses. There is a significant unmet need for new acute treatments as more than 90% of migraine sufferers are unable to work or function normally during an attack. Moreover, as Biohaven CEO Vlad Coric, MD, notes in the company's press release, "Millions of people [with] migraine are often not satisfied with their current acute treatment, at times having to make significant tradeoffs because of troublesome side effects and reduced ability to function.”

"Millions of people [with] migraine are often not satisfied with their
current acute treatment, at times having to make significant tradeoffs
because of troublesome side effects and reduced ability to function.”

Rimegepant ODT was granted FDA approval based on results from a phase 3 clinical trial, Study 303, and a long-term, open-label safety study, Study 201. Study 201 assessed the safety and tolerability of rimegepant with multiple doses taken over up to 1 year.

The study evaluated 1798 patients who used rimegepant 75 mg as needed to treat migraine attacks, up to 1 dose per day. Of these, 1131 were exposed to rimegepant for at least 6 months and 863 were exposed for at least 1 year. All treated an average of 2 migraine episodes per month. (The safety of treating more than 15 migraines in a 30-day period has not been established, according to the Biohaven statement.)

In the phase 3 clinical trial, compared to placebo, rimegepant ODT achieved statistical significance on the regulatory co-primary endpoints of pain freedom and freedom from most bothersome symptom (MBS) at 2 hours post-dose. Rimegepant ODT also was statistically superior to placebo at 1 hour for pain relief (reduction of moderate or severe pain to no pain or mild pain) and return to normal function.

Of patients treated with a single dose of remegepant ODT in the clinical trial, 86% did not require rescue medication within 24 hours. For many patients, the benefits of pain freedom, pain relief, return to normal function, and freedom from MBS were sustained up to 48 hours after one dose.

“I see many patients in my practice whose lives are disrupted by migraine, afraid to go about everyday life in case of a migraine attack,” said Peter Goadsby, MD, PhD, professor of neurology and director of the King’s Clinical Research Facility, King’s College Hospital, in a statement. “Many feel unsure if their acute treatment will work and if they can manage the side effects."

In the phase 3 clinical trial, rimegepant ODT was generally well tolerated; the most common adverse reaction was nausea (2%) in rimegepant ODT patients vs 0.4% of patients who received placebo.

Rimegepant ODT will be available in pharmacies in early March 2020.

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