Valopicitabine (NM283) 是一种核苷类似物，是强效抗 HCV 剂的 2’-C-甲基胞苷 (NM107) 的口服生物利用前药。NM107 竞争性抑制 NS5B 聚合酶，导致链终止。
Valopicitabine (NM283) is a nucleoside analog and the orally bioavailable prodrug of the potent anti-HCV agent 2’-C-methylcytidine (NM107). NM107competitively inhibits NS5B polymerase, causing chain termination[1][2].
Valopicitabine (NM283) (100 mg/kg; oral administration; Sprague-Dawley Rats) shows the Cmax, AUC, t1/2, and tmax were 3.624 μg/mL, 8.95 μg h/mL, 0.64 hours and 1 hour, respectively[2].
[1]. Pierra C, et al. Nm 283, an efficient prodrug of the potent anti-HCV agent 2’-C-methylcytidine. Nucleosides Nucleotides Nucleic Acids. 2005;24(5-7):767-70.
[2]. Pierra C, et al. Synthesis and pharmacokinetics of valopicitabine (NM283), an efficient prodrug of the potent anti-HCV agent 2’-C-methylcytidine. J Med Chem. 2006 Nov 2;49(22):6614-20.
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