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BMT-052 is a potent and selective Pan-genotypic HCV NS5B Polymerase Inhibitor (EC50 = 7 nM). The key challenge of poor metabolic stability was overcome by strategic incorporation of deuterium at potential metabolic soft spots. BMT-052 is structurally close to BMS-986139. BMT-052 expressed potent, pan-genotype HCV inhibition, a PK profile predictive of QD dosing in humans and improved physiochemical properties compared to BMS-986139. Empirically, in this context we have shown the ability of deuterium to reduced metabolic rates in LMs as evident by the longer recorded half-lives. |
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