Calcitonin gene-related peptide receptor antagonists for migraine.

Abstract

IMPORTANCE OF THE FIELD:

Migraine is a highly prevalent disabling condition, and the current treatment options are not satisfactory. The role of calcitonin gene-related peptide (CGRP) in migraine pathophysiology is well established. CGRP receptor antagonists address this new target and have the potential to improve therapy for both responders and non-responders to previous options.

AREAS COVERED IN THIS REVIEW:

This review describes CGRP, its receptors and their role in the pathophysiology of migraine. CGRP receptor antagonists are a recent development; all reported antagonists are reported in chronological order. The experimental evidence, as well as all clinical trials since the first proof-of-concept study in 2004, is discussed.

WHAT THE READER WILL GAIN:

An overview of the CGRP system and why it provides an attractive drug target for headache. The main focus is on the currently presented CGRP receptor antagonists and clinical evidence for this new therapeutic option.

TAKE HOME MESSAGE:

CGRP receptor antagonists will provide an additional and valuable therapeutic option for the treatment of headaches.

• Authors: Michael J M Fischer
• Journal: Expert opinion on investigational drugs (Expert Opin Investig Drugs) Vol. 19 Issue 7 Pg. 815-23 (Jul 2010) ISSN: 1744-7658 [Electronic] England
• PMID: 20482328 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't, Review)

Chemical References

• 4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5-yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxamide
• Azepines
• Calcitonin Gene-Related Peptide Receptor Antagonists
• Dipeptides
• Imidazoles
• Indazoles
• Piperazines
• Quinazolines
• Quinazolinones
• telcagepant
• Calcitonin Gene-Related Peptide
• olcegepant

Topics

• Animals
• Azepines (adverse effects, pharmacology, therapeutic use)
• Calcitonin Gene-Related Peptide (metabolism)
• Calcitonin Gene-Related Peptide Receptor Antagonists
• Clinical Trials as Topic
• Dipeptides (adverse effects, pharmacology, therapeutic use)
• Humans
• Imidazoles (adverse effects, pharmacology, therapeutic use)
• Indazoles (adverse effects, pharmacology, therapeutic use)
• Migraine Disorders (drug therapy, metabolism)
• Piperazines
• Quinazolines (adverse effects, pharmacology, therapeutic use)
• Quinazolinones (adverse effects, pharmacology, therapeutic use)
• Treatment Outcome
• Trigeminal Nerve (metabolism)