Rifampicin Transport by OATP1B1 Variants

被引：8

作者：

Litjens, Carlijn H. C. ^{[1
,2
]}

van den Heuvel, Jeroen J. M. W. ^{[2
]}

Russel, Frans G. M. ^{[2
]}

Aarnoutse, Rob E. ^{[1
]}

te Brake, Lindsey H. M. ^{[1
]}

Koenderink, Jan B. ^{[2
]}

机构：

[1] Radboud Univ Nijmegen, Radboud Inst Hlth Sci, Dept Pharm, Med Ctr, Nijmegen, Netherlands

[2] Radboud Univ Nijmegen, Radboud Inst Mol Life Sci, Dept Pharmacol & Toxicol, Med Ctr, Nijmegen, Netherlands

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2020年 / 64卷 / 10期

关键词：

OATP1B1; SNP; drug transport; rifampicin; DRUG DISPOSITION; POLYPEPTIDE; 1B1; HEPATIC-UPTAKE; POLYMORPHISMS; PHARMACOKINETICS; TUBERCULOSIS; SLCO1B1-ASTERISK-15; ROSUVASTATIN; VARIABILITY; EXPRESSION;

D O I：

10.1128/AAC.00955-20

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

Single nucleotide polymorphisms in the OATP1B1 transporter have been suggested to partially explain the large interindividual variation in rifampicin exposure. HEK293 cells overexpressing wild-type (WT) or OATP1B1 variants *1b, *4, *5, and *15 were used to determine the in vitro rifampicin intrinsic clearance. For OATP1B1*5 and *15, a 36% and 42% reduction in intrinsic clearance, respectively, compared to WT was found. We consider that these differences in intrinsic clearance most likely have minor clinical implications.

引用

页数：6

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