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Dec 17, 2019

NDA 211-765 (ubrogepant, AGN-241688)

Summary of selected (key) nonclinical findings

The primary pharmacology studies conducted characterize ubrogepant as an antagonist at the mouse, rat, rabbit, rhesus monkey, and human CGRP receptors, with greater in vitro binding affinity and more potent in vivo functional (capsaicin-induced vasodilation) effects in human and rhesus monkey compared to mouse (binding data only), rat, and New Zealand White rabbit. (The mouse and rat strains used for the in vitro binding assays were not specified; Sprague-Dawley rat was used in the functional assay.) Ubrogepant exhibited selectivity for the CGRP receptor, as evidenced by substantially lower potency at the human adrenomedullin (AM) 1 and 2, calcitonin, and amylin (AMY) 1 and 3 receptors, and the lack of notable off-target binding (except for the dopamine transporter) in a comprehensive panel of in vitro binding assays.

By Freed LM

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