Rimegepant (BMS-927711) is a highly potent, oral calcitonin gene-related peptide (CGRP) receptor antagonist with a K_i of 0.027 nM and an IC₅₀ of 0.14 nM for hCGRP receptor^[1]. IC50 & Target: Ki: 0.027 nM (CGRP receptor)^[1]
IC50: 0.14 nM (CGRP receptor)^[1] In Vitro: Rimegepant (BMS-927711) is a full, competitive CGRP receptor antagonist with IC₅₀ of 0.14±0.01 nM^[1]. In Vivo: Rimegepant (BMS-927711) has good oral bioavailability in rat and cynomolgus monkey, attractive overall preclinical properties, and shows dose-dependent activity in a primate model of CGRP-induced facial blood flow^[1]. The ratios of the mean AUC (0-24 h) values for Rimegepant (BMS-927711) (60, 100, and 300 mg/kg) in the DBS matrix, compare with plasma, are 0.5-0.6 across all doses in rats. Results from this study suggest a strong correlation of Rimegepant concentrations between rat plasma and rat blood (DBS)^[2].