CGRP antagonists: unravelling the role of CGRP in migraine.

Abstract

Migraine is a complex, debilitating neurovascular disorder. Although knowledge on the main molecular players is still incomplete, recent preclinical and clinical findings indicate that there is a clear correlation between migraine-associated headache and the release of the neuropeptide calcitonin gene-related peptide (CGRP). BIBN4096 was the first CGRP antagonist to be tested in clinical trials for the treatment of migraine. The proven efficacy of this agent, and also the CGRP antagonist MK-0974, to alleviate acute migraine headache provided significant support for the hypothesis that CGRP has an important role in migraine pathophysiology. Moreover, the recently published results from Phase II trials are encouraging and suggest that this new type of drug might offer advantages over existing therapies for patients suffering from migraine and related headaches.

• Authors: Henri Doods, Kirsten Arndt, Klaus Rudolf, Stefan Just
• Journal: Trends in pharmacological sciences (Trends Pharmacol Sci) Vol. 28 Issue 11 Pg. 580-7 (Nov 2007) ISSN: 0165-6147 [Print] England
• PMID: 17963849 (Publication Type: Journal Article, Review)

Chemical References

• 1-(N(2)-(3,4-dibromo-N-((4-(3,4-dihydro-2(1H)-oxoquinazolin-3-yl)-1-piperidinyl)carbonyl)tyrosyl)lysyl)-4-(4-pyridinyl)piperazine
• Azepines
• Dipeptides
• Imidazoles
• Quinazolines
• telcagepant
• Calcitonin Gene-Related Peptide

Topics

• Animals
• Azepines (chemistry, pharmacology, therapeutic use)
• Calcitonin Gene-Related Peptide (antagonists & inhibitors, physiology)
• Clinical Trials as Topic
• Dipeptides (chemistry, pharmacology, therapeutic use)
• Humans
• Imidazoles (chemistry, pharmacology, therapeutic use)
• Migraine Disorders (drug therapy, physiopathology)
• Models, Biological
• Molecular Structure
• Quinazolines (chemistry, pharmacology, therapeutic use)