Calcitonin gene-related peptide antagonists and therapeutic antibodies

Roxana Maria Rujan, Christopher A. Reynolds

Research output: Chapter in Book/Report/Conference proceedingChapterpeer-review

4 Citations (Scopus)


The calcitonin gene-related peptide (CGRP) receptor is composed of the calcitonin receptor-like receptor (CLR, a class B GPCR) and a single-pass membrane protein known as receptor activity modifying protein type 1 (RAMP1). The levels of the CGRP peptide increase during a migraine attack and infusion of CGRP can provoke a migraine attack. Consequently, there is much interest in inhibiting the actions of CGRP as a way to control migraine. Here we describe the development of small molecule antagonists designed to bind to the CGRP receptor to block its action by preventing binding of the CGRP peptide. We also describe the development of antibody drugs, designed to bind either to the CGRP receptor to block its action, or to bind directly to the CGRP peptide. The field has been very active, with one antibody drug approved and three antibody drugs in phase III clinical trial. Initial programs on the development CGRP antagonists were frustrated by liver toxicity but the current outlook is very promising with five small molecule antagonists in various stages of clinical trial.

Original languageEnglish
Title of host publicationHandbook of Experimental Pharmacology
EditorsS. Brain, P. Geppetti
PublisherSpringer New York LLC
Number of pages24
ISBN (Electronic)978-3-030-21454-8
ISBN (Print)978-3-030-21453-1
Publication statusPublished - 1 Jan 2019
Externally publishedYes

Publication series

NameHandbook of Experimental Pharmacology
ISSN (Print)0171-2004
ISSN (Electronic)1865-0325


  • Antibody drugs
  • Calcitonin-receptor-like receptor
  • CGRP antagonist
  • CGRP peptide
  • Migraine

ASJC Scopus subject areas

  • Biochemistry
  • Pharmacology, Toxicology and Pharmaceutics(all)


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