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

[ Vol. 8 , Issue. 16 ]


Carl D. Davis and Cen Xu   Pages 1468 - 1479 ( 12 )


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.


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


Department of Neuroscience, Amgen Inc., One Amgen Center Drive, Mailstop 29-2-B, Thousand Oaks, CA 91320-1799.

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