First-in-class therapeutic for migraine treatment promises to improve QOL of sufferers | Multidisciplinary

A new migraine medication is now available. Rimegepant, a calcitonin gene-related peptide (CGRP) receptor antagonist, is indicated for the acute treatment and prophylaxis of migraine, a condition recognized as a leading cause of disability globally. [J Headache Pain 2020;21(1):137]

Deborah Seifert, MISP Cluster Lead for Emerging Markets Asia at Pfizer, emphasized the company's recognition of the significant impact of migraine on patients’ daily lives, including their health, work, education, leisure, and social engagement. The introduction of rimegepant as an additional therapeutic option aims to empower those afflicted by migraines.

Speaking at the launch, Dr Julia Shahnaz Merican, a consultant neurologist, said the International Headache Society’s classification of migraine without aura is that of a recurrent headache disorder with episodes lasting from 4 to 72 hours. Characteristic symptoms include unilateral location, pulsating in nature, moderate to severe intensity, worsening with routine physical activity, and often accompanied by nausea and/or sensitivity to light and sound (photophobia and phonophobia). [Cephalalgia 2018;38(1):1–211]

Julia noted that migraines may manifest with or without aura, the former being characterized by visual disturbances like dots, sparks, or zigzags preceding a migraine attack. Independent of type, migraines significantly impair the quality of life (QOL), typically resulting in patients seeking relief in dark, quiet environments until symptoms abate. She also noted the treatment of migraine is different from person to person, and the clinician should help their patient to identify stressors and triggers to help them manage their migraine.

Migraine exhibits a gender disparity, being notably more prevalent in women, with occurrences three to four times higher than in men. The precise etiology of migraines remains elusive; however, over the past 3 decades, both clinical and preclinical studies have explored the involvement of a neuropeptide known as CGRP in the pathogenesis of migraines. [Physiol Rev 2014;94(4):1099–1142] CGRP is thought to be the key driver of migraine via the dilation of cerebral and dural blood vessels, release of inflammatory mediators from mast cells, and transmission of nociceptive information from intracranial blood vessels to the nervous system. Evidence for the role of CGRP in migraine genesis comes from findings alluding to elevation of serum CGRP concentrations during migraine attacks and other neurological headache types. Additionally, the use of triptans to relieve migraine coincides with the normalization of CGRP serum concentrations. [Headache 2006;46(Suppl 1):S3–S8]

About rimegepant
Rimegepant is a reversible CGRP receptor antagonist. By blocking the CGRP receptors, pain signaling and neurogenic inflammation is inhibited and reduced. The medication is approved for treating acute migraine episodes, with a maximum frequency of once daily, and in prophylaxis to decrease the frequency of subsequent attacks where it is taken every other day.

A meta-analysis looking into the safety and efficacy of rimegepant found that there was no significant difference between rimegepant and placebo in terms of safety (4.4 percent vs 3.7 percent). It was also noted that rimegepant demonstrated more of an advantage in terms of safety compared to other CGRP blockers or triptans. In terms of side effects, the adverse events of rimegepant 75 mg treatment for migraine were similar to those of the placebo, with no significant difference in adverse events between rimegepant and placebo. [Front Pharmacol 2020;10:1577]