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P-糖蛋白与药代动力学

P-glycoprotein and pharmacokinetics.

作者信息

Levêque D, Jehl F

机构信息

Institut de Bactériologie de la Faculté de Médecine, Université Louis-Pasteur, Strasbourg, France.

出版信息

Anticancer Res. 1995 Mar-Apr;15(2):331-6.

PMID:7763002
Abstract

P-glycoprotein (P-gp) is a transmembrane protein associated with a phenotype of cross resistance to certain anticancer agents. P-gp is thought to act as an energy dependent pump that expels the anticancer drug out of the tumoral cell, reducing its accumulation and hence its activity. P-gp has been detected in vivo and in vitro in numerous tumor cell types but also in normal tissues and particularly in organs involved in the pharmacokinetic behaviour of xenobiotics. The physiologic functions of P-gp remain unclear but a growing amount of information suggests that it can play an important role at the different steps of pharmacokinetics (i.e., absorption, distribution, elimination). This review gives an update on what is known about the impact of P-gp on the disposition of drugs.

摘要

P-糖蛋白(P-gp)是一种跨膜蛋白,与对某些抗癌药物的交叉耐药表型相关。P-gp被认为是一种能量依赖性泵,可将抗癌药物排出肿瘤细胞,减少其蓄积,从而降低其活性。P-gp已在体内和体外的多种肿瘤细胞类型中被检测到,也存在于正常组织中,尤其是参与外源性物质药代动力学行为的器官中。P-gp的生理功能尚不清楚,但越来越多的信息表明,它在药代动力学的不同阶段(即吸收、分布、消除)可能发挥重要作用。本文综述了关于P-gp对药物处置影响的已知信息。

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