Rimegepant Orally Disintegrating Tablet for Acute Migraine Treatment: A Review

Ann Pharmacother. 2021 May;55(5):650-657. doi: 10.1177/1060028020954800. Epub 2020 Sep 10.

Abstract

Objective: To review the pharmacology, pharmacokinetics, efficacy, safety, and place in therapy of rimegepant for treatment of migraine.

Data sources: A comprehensive PubMed and Cochrane search (1985 to May 2020) was performed utilizing the keywords rimegepant, Nurtec, orally disintegrating tablet, migraine, migraine headache, migraine disorder, calcitonin gene-related peptide, and calcitonin gene-related peptide antagonist. Additional data were obtained from the references of identified articles, manufacturer's product labeling and website, ClinicalTrials.gov, and governmental sources.

Study selection and data extraction: All English-language trials evaluating oral rimegepant were included for this review.

Data synthesis: Rimegepant orally disintegrating tablet (ODT) is Food and Drug Administration approved for the treatment of migraine. According to data from 3 phase 3 randomized controlled trials, rimegepant has been shown to significantly improve freedom from pain at 2 hours after the dose and freedom from the most bothersome symptom 2 hours postdose. Additional outcomes improved include freedom from photophobia and phonophobia at 2 hours postdose and pain relief 2 hours after the dose. Adverse effects of rimegepant include nausea, urinary tract infection, and dizziness.

Relevance to patient care and clinical practice: Orally disintegrating rimegepant provides a novel mechanism of action for the treatment of acute migraine. When patients experience inadequate relief from other therapies, have contraindications to triptans, or are unable to tolerate the adverse effects of triptans, rimegepant is a promising therapeutic option.

Conclusion: Rimegepant ODT is an efficacious migraine treatment option with a novel mechanism of action, convenient dosage form, and limited adverse effect profile.

Keywords: Nurtec; calcitonin gene-related peptide; calcitonin gene-related peptide antagonist; migraine; migraine disorder; migraine headache; orally disintegrating tablet; rimegepant.

MeSH terms

  • Acute Disease
  • Administration, Oral
  • Calcitonin Gene-Related Peptide / antagonists & inhibitors
  • Calcitonin Gene-Related Peptide Receptor Antagonists / pharmacokinetics
  • Calcitonin Gene-Related Peptide Receptor Antagonists / therapeutic use
  • Clinical Trials as Topic / methods
  • Humans
  • Migraine Disorders / diagnosis
  • Migraine Disorders / drug therapy*
  • Migraine Disorders / metabolism*
  • Nausea / chemically induced
  • Pain / drug therapy
  • Pain / metabolism
  • Pain Management / methods*
  • Piperidines / administration & dosage*
  • Piperidines / pharmacokinetics*
  • Pyridines / administration & dosage*
  • Pyridines / pharmacokinetics*
  • Solubility
  • Tablets
  • Treatment Outcome

Substances

  • Calcitonin Gene-Related Peptide Receptor Antagonists
  • Piperidines
  • Pyridines
  • Tablets
  • rimegepant sulfate
  • Calcitonin Gene-Related Peptide