Elevated levels of calcitonin gene-related peptide (CGRP) have been shown to be an early critical part of migraine pathophysiology.  A number of CGRP receptor antagonists have been effective in clinical trials as novel anti-migraine agents, and there has been a decade long effort to discover orally available CGRP receptor antagonists.  Overall, it has been a tremendously difficult challenge to incorporate all the required structural features in one molecule that can qualify for clinical development. Presently, the only oral CGRP receptor antagonist in clinical trials is BMS-927711.  In this presentation, we will present the discovery of BMS-927711 and some initial human pharmacokinetics.

Discovery and development of BMS-927711, a potent oral CGRP antagonist for migraine

243rd National Meeting (2012)

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