ABT-072 (potassium trihydrate) 是一种具有口服活性的强效非核苷 HCV NS5B 聚合酶抑制剂 (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM)。
ABT-072 (potassium trihydrate) is an orally active and potent non-nucleoside HCV NS5B polymerase inhibitor (HCV GT1a EC50=1 nM; HCV GT1b EC50=0.3 nM)[1][2][3].
ABT-072 (potassium trihydrate) is a non-nucleoside NS5B polymerase inhibitor with nanomolar potency in vitro against genotype 1a and 1b hepatitis C virus polymerases[1].
ABT-072 (5 and/or 30 mg/kg; i.v. or p.o.) (potassium trihydrate) shows good PK properties[3].ABT-072 (2.5 and/or 30 mg/kg; i.v. or p.o.) (potassium trihydrate) shows low plasma clearance and high oral bioavailability[3].
[1]. Lawitz E, et al. A phase 2a trial of 12-week interferon-free therapy with two direct-acting antivirals (ABT-450/r, ABT-072) and ribavirin in IL28B C/C patients with chronic hepatitis C genotype 1. J Hepatol. 2013;59(1):18-23.
[2]. Shi Y, et al. Assessing Supersaturation and Its Impact on In Vivo Bioavailability of a Low-Solubility Compound ABT-072 With a Dual pH, Two-Phase Dissolution Method. J Pharm Sci. 2016;105(9):2886-2895.
[3]. Randolph JT, et al. Synthesis and Biological Characterization of Aryl Uracil Inhibitors of Hepatitis C Virus NS5B Polymerase: Discovery of ABT-072, a trans-Stilbene Analog with Good Oral Bioavailability. J Med Chem. 2018;61(3):1153-1163.
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