| Autor: |
Wu, Shuanzhi, Wang, Tenghua, Li, Jieyun, Zhang, Zhixin, Li, Chen, Xiao, Shuangshuang, He, Jin, Wang, Xuan, Hu, Zhiqin, Wang, Xiaole, Zheng, Sichao, Liang, Xintong, Chen, Guiying, Li, Yongmei, Li, Xianbo, Zhan, Yaoxuan, Zou, Qinwen, Jiang, Hongliang, Zheng, Qingshan, Ban, Li, Liu, Haiyan, Fang, Yi |
| Zdroj: |
Expert Opinion on Investigational Drugs; November 2023, Vol. 32 Issue: 11 p1085-1094, 10p |
| Abstrakt: |
ABSTRACTBackgroundSAR107375E is a direct dual inhibitor of both Factor Xa and Factor IIa and has shown potent anticoagulation activity in vitro and animals. This study evaluated the safety, tolerability, pharmacokinetics, and pharmacodynamics of single ascending intravenous doses of SAR107375E in healthy Chinese adult subjects.MethodsIn this randomized, double-blind, placebo-controlled trial, 60 healthy Chinese adult subjects were administered intravenously single ascending doses (0.5, 1.5, 3.0, 5.0, 7.5, 10.0, 15.0, or 20.0 mg) of SAR107375E (N = 44) or placebo (N = 16). Plasma and urine concentrations of SAR107375E were measured and used to calculate pharmacokinetic parameters. Coagulation functions were measured and compared with baseline values. Treatment-emergent adverse events were recorded to evaluate safety.ResultsIn plasma, from the 0.5 to 20.0 mg dose group, t1/2is 1.51–4.00 h, Cmaxis 59.05–1360 ug/L, and AUC0-tis 25.01–528.45 h*ug/L. And it shows dose proportionality in the 5.0–20.0 mg range. Activated partial thromboplastin time and Ecarin clotting time correlated linearly with drug plasma concentration. No serious adverse events were reported during the study.ConclusionSAR107375E exhibits good safety and tolerability, predictable pharmacokinetics and pharmacodynamics.Clinical trial registrationwww.chinadrugtrials.org.cn, identifier is CTR20211082. |
| Databáze: |
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