Induction of Influx and Efflux Transporters and Cytochrome P450 3A4 in Primary Human Hepatocytes by Rifampin, Rifabutin, and Rifapentine

被引：113

作者：

Williamson, Beth ^{[1
]}

Dooley, Kelly E. ^{[2
,3
]}

Zhang, Yuan ^{[1
]}

Back, David J. ^{[1
]}

Owen, Andrew ^{[1
]}

机构：

[1] Univ Liverpool, Dept Mol & Clin Pharmacol, Liverpool L69 3BX, Merseyside, England

[2] Johns Hopkins Univ, Sch Med, Dept Med, Div Clin Pharmacol, Baltimore, MD 21205 USA

[3] Johns Hopkins Univ, Sch Med, Div Infect Dis, Baltimore, MD 21205 USA

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2013年 / 57卷 / 12期

关键词：

MULTIDRUG-RESISTANCE PROTEIN-2; CLINICAL PHARMACOKINETICS; TUBERCULOSIS; CELLS; BINDING;

D O I：

10.1128/AAC.01124-13

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

Rifampin is a potent inducer of cytochrome P450 (CYP) enzymes and transporters. Drug-drug interactions during tuberculosis treatment are common. Induction by rifapentine and rifabutin is understudied. Rifampin and rifabutin significantly induced CYP3A4 (80-fold and 20-fold, respectively) in primary human hepatocytes. The induction was concentration dependent. Rifapentine induced CYP3A4 in hepatocytes from 3 of 6 donors. Data were also generated for ABCB1, ABCC1, ABCC2, organic anion-transporting polypeptide 1B1 (OATP1B1), and OATP1B3. This work serves as a basis for further study of the extent to which rifamycins induce key metabolism and transporter genes.

引用

页码：6366 / 6369

页数：4

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