【摘 要】
：
Tolcapone and entacapone, two potent catechol-O-methyltransferase COMT inhibitors, were commonly used as therapeutic drugs for treatment of Parkinsons disease.Tolcapone and entacapone share a common c
【机 构】
：
Laboratory of Pharmaceutical Resource Discovery, Dalian Institute of Chemical Physics, Chinese Acade
【出 处】
：
2015年第一届药代动力学朝阳论坛
论文部分内容阅读
Tolcapone and entacapone, two potent catechol-O-methyltransferase COMT inhibitors, were commonly used as therapeutic drugs for treatment of Parkinsons disease.Tolcapone and entacapone share a common chemical backbone structure, which is the determinant for exerting similar pharmacological activity.However, it has been reported that tolcapone can lead to unconjugated hyperbilirubinemia, jaundice and liver damage in certain susceptible individuals who received tolcapone.UDP-glucuronosyhransferases (UGT)1A1 is the only physiologically relevant UGT isoform involved in the metabolic clearance of endobiotics toxic bilirubin.Inhibition of UGT1A1 by the concomitant use of certain drugs may reduce the glucuronidation of bilirubin, resulting in unconjugated hyperbilirubinemia.In this study, we aimed to investigate and compare the inhibitory effects of tolcapone and entacapone on the catalytic activities of human UGTs, which are very helpful to evaluate the potential risks of drug-drug interactions (DDI).
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