Calcitonin gene-related peptide (CGRP), a 37 amino acid neuropeptide, has been implicated in the pathogenesis of migraine. Clinical studies with the intravenously-administered olcegepant and the orally-administered telcagepant have validated the effectiveness of CGRP receptor antagonists in the acute treatment of migraine. Our research program focused on developing orally bioavailable CGRP receptor antagonists. The optimization of a weakly potent benzodiazepine HTS lead into novel, highly potent CGRP receptor antagonists will be discussed.

Highly potent CGRP receptor antagonists as novel migraine therapeutics

248th National Meeting (2014)

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