HIV protease inhibitors are substrates for OATP1A2, OATP1B1 and OATP1B3 and lopinavir plasma concentrations are influenced by SLCO1B1 polymorphisms by Hartkoorn Ruben C, Kwan Wai San, Shallcross Victoria, Chaikan Ammara, Liptrott Neill, Egan Deirdre, Sora Enrique Salcedo, James Chloƫ E, Gibbons Sara, Bray Pat G, Back David J, Khoo Saye H, Owen Andrew in Pharmacogenetics and genomics (2010). PubMed

Abstract

OATP1B1 and OATP1B3 are major hepatic drug transporters whilst OATP1A2 is mainly located in the brain but is also located in liver and several other organs. These transporters affect the distribution and clearance of many endobiotics and xenobiotics and have been reported to have functional single nucleotide polymorphisms (SNPs). We have assessed the substrate specificities of these transporters for a panel of antiretrovirals and investigated the effects of SNPs within these transporters on the pharmacokinetics of lopinavir.

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