The Tortuous Road to an Ideal CGRP Function Blocker for the Treatment of Migraine

Title: The Tortuous Road to an Ideal CGRP Function Blocker for the Treatment of Migraine

Volume: 8 Issue: 16

Author(s): Carl D. Davis and Cen Xu

Affiliation:

Keywords: Migraine, CGRP receptor, BIBN4096BS, Merck-0974, CGRP scavenger, antibody, bioavailability, protein-binding

Abstract: The critical role of Calcitonin Gene-Related Peptide (CGRP) in migraine has been validated, with two small molecule CGRP antagonists BIBN4096BS and MK-0974 demonstrating efficacy in the reversal of acute migraine attack [1,2]. Multiple approaches have been taken to find the ideal agent that most effectively inhibits CGRPs function. Here, we have summarized the progress made in recent years, including the identification and optimization of an orally bioavailable small molecule CGRP receptor antagonist. We also describe other interventions such as scavenging of CGRP itself. The advantages and disadvantages of these distinct approaches are discussed.

Cite this article as:

Davis D. Carl and Xu Cen, The Tortuous Road to an Ideal CGRP Function Blocker for the Treatment of Migraine, Current Topics in Medicinal Chemistry 2008; 8 (16) . https://dx.doi.org/10.2174/156802608786264218