The Journal of Headache and Pain (Sep 2023)

Mode and site of action of therapies targeting CGRP signaling

  • Alejandro Labastida-Ramírez,
  • Edoardo Caronna,
  • Cédric Gollion,
  • Emily Stanyer,
  • Austeja Dapkute,
  • Diana Braniste,
  • Hoda Naghshineh,
  • Liga Meksa,
  • Nino Chkhitunidze,
  • Tamari Gudadze,
  • Patricia Pozo-Rosich,
  • Rami Burstein,
  • Jan Hoffmann

DOI
https://doi.org/10.1186/s10194-023-01644-8
Journal volume & issue
Vol. 24, no. 1
pp. 1 – 14

Abstract

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Abstract Targeting CGRP has proved to be efficacious, tolerable, and safe to treat migraine; however, many patients with migraine do not benefit from drugs that antagonize the CGRPergic system. Therefore, this review focuses on summarizing the general pharmacology of the different types of treatments currently available, which target directly or indirectly the CGRP receptor or its ligand. Moreover, the latest evidence regarding the selectivity and site of action of CGRP small molecule antagonists (gepants) and monoclonal antibodies is critically discussed. Finally, the reasons behind non-responders to anti-CGRP drugs and rationale for combining and/or switching between these therapies are addressed.

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