A Brief Review of Gepants

Curr Pain Headache Rep. 2023 Sep;27(9):479-488. doi: 10.1007/s11916-023-01142-1. Epub 2023 Aug 2.

Abstract

Purpose of review: Gepants are small molecules that antagonize calcitonin gene-related peptide (CGRP) receptors. Due to their favorable side effect profile and versatility in treating headaches acutely and preventively, gepants are preferred over triptans. We will cover the indications for the four FDA-approved gepants in adults: rimegepant, atogepant, ubrogepant, and zavegepant. This review will illustrate how gepants will continue to revolutionize the acute and preventive treatment of headaches.

Recent findings: Gepants are now available in oral tablet, dissolving tablet, and intra-nasal spray formulations. Recent studies have shown promising utility in treating the pre-headache or prodromal phase. They have favorable tolerability, no evidence for association with medication overuse, and remain a safer alternative in those who have cerebrovascular risk factors. Additional research is needed to explore occurrence of Raynaud's phenomenon in participants treated with gepants, as it has been associated with CGRP monoclonal antibodies, but are not extensively studied in gepants. Gepants are expected to play a significant role in the next generation of migraine treatments.

Keywords: Atogepant; CGRP; Gepant; Rimegepant; Ubrogepant; Zavegepant.

Publication types

  • Review

MeSH terms

  • Calcitonin Gene-Related Peptide Receptor Antagonists* / administration & dosage
  • Calcitonin Gene-Related Peptide Receptor Antagonists* / adverse effects
  • Calcitonin Gene-Related Peptide Receptor Antagonists* / therapeutic use
  • Humans
  • Migraine Disorders* / drug therapy
  • Pyridines* / administration & dosage
  • Pyridines* / adverse effects
  • Pyridines* / therapeutic use
  • Pyrroles* / administration & dosage
  • Pyrroles* / adverse effects
  • Pyrroles* / therapeutic use
  • Raynaud Disease / chemically induced

Substances

  • Calcitonin Gene-Related Peptide Receptor Antagonists
  • rimegepant sulfate
  • atogepant
  • ubrogepant
  • Pyridines
  • Pyrroles