OATP1B1 变异体对利福平的转运。
Rifampicin Transport by OATP1B1 Variants.
机构信息
Department of Pharmacy, Radboud Institute for Health Sciences, Radboud University Medical Center, Nijmegen, The Netherlands
Department of Pharmacology and Toxicology, Radboud Institute for Molecular Life Sciences, Radboud University Medical Center, Nijmegen, The Netherlands.
出版信息
Antimicrob Agents Chemother. 2020 Sep 21;64(10). doi: 10.1128/AAC.00955-20.
Abstract
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 rifampicin intrinsic clearance. For OATP1B15 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.
摘要
OATP1B1 转运体中的单核苷酸多态性被认为部分解释了利福平暴露的个体间差异很大。用过表达野生型 (WT) 或 OATP1B1 变体 *1b、*4、*5 和 15 的 HEK293 细胞来确定利福平的内在清除率。与 WT 相比，OATP1B15 和 *15 的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。
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