Rifampicin Transport by OATP1B1 Variants

Antimicrob Agents Chemother. 2020 Sep 21;64(10):e00955-20. doi: 10.1128/AAC.00955-20. Print 2020 Sep 21.

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 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.

Keywords: OATP1B1; SNP; drug transport; rifampicin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Biological Transport
  • HEK293 Cells
  • Humans
  • Liver / metabolism
  • Liver-Specific Organic Anion Transporter 1
  • Organic Anion Transporters* / genetics
  • Organic Anion Transporters* / metabolism
  • Polymorphism, Single Nucleotide
  • Rifampin* / metabolism
  • Rifampin* / pharmacology

Substances

  • Liver-Specific Organic Anion Transporter 1
  • Organic Anion Transporters
  • SLCO1B1 protein, human
  • Rifampin