Xenobiotica ( IF 1.3 ) Pub Date : 2020-12-17 Yuqing Zhao, Lijun Xie, Ning Ou, Jie Wu, Hongwen Zhang, Sufeng Zhou, Yun Liu, Juan Chen, Lu Wang, Li-bin Wang, Jingjing Wang, Feng Shao
Abstract
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SHR0534 is being developed for type 2 diabetes mellitus. Herein the tolerability, safety, pharmacokinetics and pharmacodynamics of SHR0534 in healthy Chinese subjects were assessed in a phase I, randomized, double-blind, placebo-controlled, single- and multiple-ascending dose study.
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Forty subjects were randomized 4:1 to receive SHR0534 at the dose of 10, 25, 50 or 100 mg, or placebo, and another eleven subjects were allocated to either the 5 mg group or the placebo group at an 8:3 ratio. All subjects received a single dose on day 1, followed by a 9-day washout and once-daily administrations for 14 consecutive days. Serial samples were collected, and vital signs, electrocardiograms, laboratory tests, urinalysis and adverse events (AEs) were recorded.
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All doses of SHR0534 were safe and well tolerated with infrequent, generally mild-to-moderate AEs and no serious AEs in the study. SHR0534 was absorbed with a Tmax of approximately 4 hours, and systemic exposure increased with dose. Accumulation was minimal (2-3 folds) and steady state was reached after seven days of dosing. For pharmacodynamics, no significant hypoglycemic effects were seen in healthy adults.
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Good pharmacokinetics and safety were demonstrated but no obvious effect was found.