Response to in vitro and physiologically-based pharmacokinetic assessment of the drug-drug interaction potential of canagliflozin.
作者信息
Miners John O, Pattanawongsa Attarat, Rowland Andrew
机构信息
Department of Clinical Pharmacology, Flinders University College of Medicine and Public Health, Adelaide, Australia.
出版信息
Br J Clin Pharmacol. 2018 Feb;84(2):392-393. doi: 10.1111/bcp.13443. Epub 2017 Nov 3.
Abstract
摘要
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Inhibition of human UDP-glucuronosyltransferase enzymes by lapatinib, pazopanib, regorafenib and sorafenib: Implications for hyperbilirubinemia.拉帕替尼、帕唑帕尼、瑞戈非尼和索拉非尼对人尿苷二磷酸葡萄糖醛酸转移酶的抑制作用：与高胆红素血症的关系。
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In vitro and physiologically-based pharmacokinetic based assessment of drug-drug interaction potential of canagliflozin.基于体外和生理药代动力学的卡格列净药物相互作用潜力评估。
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The prediction of drug-glucuronidation parameters in humans: UDP-glucuronosyltransferase enzyme-selective substrate and inhibitor probes for reaction phenotyping and in vitro-in vivo extrapolation of drug clearance and drug-drug interaction potential.预测人体药物葡萄糖醛酸化参数：用于反应表型分析的 UDP-葡萄糖醛酸基转移酶酶选择性底物和抑制剂探针，以及用于预测药物清除率和药物相互作用潜力的体外-体内外推。
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The "albumin effect" and drug glucuronidation: bovine serum albumin and fatty acid-free human serum albumin enhance the glucuronidation of UDP-glucuronosyltransferase (UGT) 1A9 substrates but not UGT1A1 and UGT1A6 activities.“白蛋白效应”与药物葡糖醛酸化：牛血清白蛋白和无脂肪酸人血清白蛋白增强尿苷二磷酸葡糖醛酸基转移酶（UGT）1A9底物的葡糖醛酸化作用，但不影响UGT1A1和UGT1A6的活性。
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