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PRECLINICAL PHARMACOKINETIC ANALYSIS OF (E)-METHYL-4-ARYL-4-OXABUT-2-ENOATE, A NOVEL SER/THR PROTEIN KINASE B INHIBITOR, IN RATS

文献类型： 外文期刊

作者： Zhai, Qian-Qian 1 ; Pang, Jing 1 ; Li, Guo-Qing 1 ; Li, Cong-Ran 1 ; Wang, Yu-Cheng 1 ; Yu, Li-Yan 1 ; Li, Jian 3 ; You, 1 ;

作者机构： 1.Chinese Acad Med Sci, Beijing Key Lab Antiinfect Agents, Inst Med Biotechnol, Beijing 100050, Peoples R China

2.Peking Union Med Coll, Beijing 100050, Peoples R China

3.Chinese Acad Fishery Sci, Yellow Sea Fisheries Res Inst, Key Lab Sustainable Dev Marine Fisheries, Minist Agr, Qingdao 266071, Peoples R China

关键词： (E)-methyl-4-aryl-4-oxabut-2-enoate; phannacokinetics; bioavailability; distribution; excretion; protein binding

期刊名称：ACTA POLONIAE PHARMACEUTICA （ 影响因子：0.33； 五年影响因子：0.667 ）

ISSN： 0001-6837

年卷期： 2017 年 74 卷 1 期

页码：

收录情况： SCI

摘要： (E)-Methyl-l-aryl-4-oxabut-2-enoate. designated YH-8. is a novel Ser/Thr protein kinase B (PknB) inhibitor, which is designed for the treatment of tuberculosis. The aim of this study was to investigate the pharmacokinetics, bioavailability, tissue distribution and excretion characteristics of YH-8 in rats and study its plasma protein binding in rum. The pharmacokinetic properties were examined after intravenously injected YH-8 at 10 and 20 mg/kg and oral administrated YH-8 at 50. 100 and 200 mg/kg to rats. The concentrations of in plasma were determined with LC-MS/MS, with a liquid-liquid extraction. The tissue distribution and urinary, fecal and biliary excretion patterns of YH-8 were investigated following a single oral dosing of 100 mg/kg. The plasma protein binding rates of YH-8 were determined using ultra-filtration method. After intravenous and oral administration. YH-8 showed dose-independent pharmacokinetic characteristics, with T-1/2 of approximately 5.5 h and 7.1 h, respectively. The oral absolute bioavailability of YH-8 was relatively low (about 12%). YH-8 was widely distributed in various tissues and showed substantial deposition in intestine, stomach, liver, lung and kidney. The drug was mainly eliminated via fecal excretion and its binding rate with plasma protein was concentration-dependent. In conclusion, this study as first provided the full pharmacokinetic characteristics of YH-8, which would be helpful for its further development and clinical application.

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