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
收藏
页码：6366 / 6369
页数：4
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