Antagonists of the CGRP (calcitonin gene-related peptide) receptor, a Class B GPCR (G-protein coupled receptor), have been shown to be clinically effective in the acute treatment of migraine headaches.  Four compounds have already achieved Proof-of-Concept in human migraine trials.  In this seminar, the discovery of a series of CGRP receptor antagonists will be presented.  Specifically, the discovery of an intranasally bioavailable, picomolar potent CGRP receptor antagonist (BMS-742413) and an orally bioavailable picomolar CGRP receptor antagonist (BMS-927711) will be detailed.  A complete characterization of both compounds will be presented, and clinical results for BMS-927711 will also be presented.

Discovery and development of both intranasally and orally administered CGRP (calcitonin gene-related peptide) receptor antagonists for the treatment of migraine

245th National Meeting (2013)

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