Evaluating rimegepant for the treatment of migraine

Figures & data

Table 1. Pharmacodynamic and pharmacokinetic parameters of NURTEC ODT (75 mg)

NURTEC ODT (75 mg)
Tmax	1.5 hours
Bioavailability	64%
Plasma protein binding	96%
Volume of distribution	120 L
Partition coefficient (Log P)	2.95
Ki	27 pM

Figure 1. Rimegepant as a continuum for mixed acute and prophylactic treatment in migraine. Rimegepant is situated between pure acute treatments (e.g. ubrogepant) and pure prophylactic treatments (e.g. monoclonal antibodies (mAbs)) in migraine, based on its plasma half-life. This allows clinicians to choose the optimal treatment based on the migraine frequency

Table 2. Drug summary box for rimegepant

Drug summary box
Drug name (generic)	Rimegepant (BMS-927711)
Phase	FDA approved for the acute treatment of migraine
Indication	Migraine
Pharmacology description/mechanism of action	Small-molecule CGRP receptor antagonist
Route of Administration	Oral, swallowed
Chemical structure	C28H28F2N6O3
Pivotal trials	NCT01430442 (phase IIb) [30] NCT03235479 (phase III) [32] NCT03237845 (phase III) [31] NCT03461757 (phase III) [25]

Marcus R, Goadsby PJ, Dodick D, et al. BMS-927711 for the acute treatment of migraine: a double-blind, randomized, placebo controlled, dose-ranging trial. Cephalalgia. 2014 Feb;34(2):114–125. PubMed PMID: 23965396.

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Lipton RB, Conway CM, Stock EG, et al. Efficacy, safety, and tolerability of rimegepant 75 mg, an oral CGRP receptor antagonist, for the acute treatment of migraine: results from a phase 3, double-blind, randomized, placebo-controlled trial, study 301. American Headache Society 60th Annual Scientific Meeting; San Fransisco CA: Biohaven Pharmaceuticals; 2018.

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Lipton RB, Croop R, Stock EG, et al. Rimegepant, an Oral Calcitonin Gene–Related Peptide Receptor Antagonist, for Migraine. N Engl J Med. 2019 Jul 11;381(2):142–149. PubMed PMID: 31291516.

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Croop R, Goadsby PJ, Stock DA, et al. Efficacy, safety, and tolerability of rimegepant orally disintegrating tablet for the acute treatment of migraine: a randomised, phase 3, double-blind, placebo-controlled trial. Lancet. 2019 Aug 31;394(10200):737–745. PubMed PMID: 31311674.

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