Rifampicin Transport by OATP1B1 Variants.

Carlijn H C LitjensJeroen J M W van den HeuvelFrans G M RusselRob E AarnoutseLindsey H M Te BrakeJan B Koenderink

Published in: Antimicrobial agents and chemotherapy (2020)

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.

Keyphrases

mycobacterium tuberculosis
wild type
pulmonary tuberculosis
copy number
induced apoptosis
cell cycle arrest
gene expression
signaling pathway
endoplasmic reticulum stress