Rimegepant is a small molecule inhibitor of the calcitonin gene-related peptide (CGRP) receptor that blocks the action of CGRP, a potent vasodilator believed to play a role in migraine headaches. Rimegepant is approved for treatment of acute migraine attacks. In clinical trials, rimegepant was generally well tolerated with only rare instances of transient serum aminotransferase elevations during therapy and with no reported instances of clinically apparent liver injury.

Rimegepant is an oral antagonist of the CGRP receptor developed by Biohaven Pharmaceuticals. It received FDA approval on February 27, 2020 for the acute treatment migraine headache. While several parenteral antagonists of CGRP and its receptor have been approved for migraine therapy (e.g. [erenumab], [fremanezumab], [galcanezumab]), rimegepant and [ubrogepant] are the only members of the “gepants” family of medications remaining in development, and the only CGRP antagonists that possess oral bioavailability. The current standard of migraine therapy involves abortive treatment with “triptans”, such as [sumatriptan], but these medications are contraindicated in patients with pre-existing cerebrovascular and cardiovascular disease due to their vasoconstrictive properties. Antagonism of the CGRP pathway has become an attractive target for migraine therapy as, unlike the triptans, oral CGRP antagonists have no observed vasoconstrictive properties and are therefore safer for use in patients with contraindications to standard therapy.

Rimegepant is a Calcitonin Gene-related Peptide Receptor Antagonist. The mechanism of action of rimegepant is as a Calcitonin Gene-related Peptide Receptor Antagonist.

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