Open AccessRifampicin Transport by OATP1B1 Variants
Author(s) -
Carlijn H. C. Litjens,
Jeroen J. M. W. van den Heuvel,
Frans G. M. Rüssel,
Rob E. Aarnoutse,
Lindsey H M Te Brake,
Jan B. Koenderink
Publication year - 2020
Publication title -
antimicrobial agents and chemotherapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.07
H-Index - 259
eISSN - 1070-6283
pISSN - 0066-4804
DOI - 10.1128/aac.00955-20
Subject(s) - rifampicin , in vitro , transporter , single nucleotide polymorphism , biology , wild type , pharmacology , genetics , chemistry , genotype , gene , antibiotics , mutant
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.