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Rifampicin Transport by OATP1B1 Variants.
Antimicrobial Agents and Chemotherapy ( IF 4.9 ) Pub Date : 2020-09-21 , DOI: 10.1128/aac.00955-20
Carlijn H C Litjens 1, 2 , Jeroen J M W van den Heuvel 2 , Frans G M Russel 2 , Rob E Aarnoutse 3 , Lindsey H M Te Brake 3 , Jan B Koenderink 2
Affiliation  

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.

中文翻译:

OATP1B1 变体的利福平转运。

有人提出 OATP1B1 转运蛋白中的单核苷酸多态性部分解释了利福平暴露的巨大个体间差异。过表达野生型 (WT) 或 OATP1B1 变体 *1b、*4、*5 和 *15 的 HEK293 细胞用于确定体外利福平内在清除率。对于 OATP1B1*5 和 *15,发现与 WT 相比,内在清除率分别降低了 36% 和 42%。我们认为这些内在清除率的差异很可能具有较小的临床意义。
更新日期:2020-09-21
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