Hepatic OATP and OCT uptake transporters: their role for drug-drug interactions and pharmacogenetic aspects.
Uptake transporters in the basolateral membrane of hepatocytes are important for the hepatobiliary elimination of drugs. Further, since drug-metabolizing enzymes are located intracellularly, uptake into hepatocytes is a prerequisite for their subsequent metabolism. Therefore, alteration of uptake transporter function (e.g., by concomitantly administered drugs or due to functional consequences of genetic variations, leading to reduced transport function) may result in a change in drug pharmacokinetics. In this review, we focus on the hepatocellularly expressed members of the OATP and OCT family, their impact on transport-mediated drug-drug interactions, and on the functional consequences of variations in genes encoding these transporters.
Fahrmayr
Christina
C
Department of Clinical Pharmacology and Clinical Toxicology, Institute of Experimental and Clinical Pharmacology and Toxicology, Friedrich-Alexander-University Erlangen-Nuremberg, Germany.
Fromm
Martin F
MF
König
Jörg
J
D000818:Animals; D004347:Drug Interactions; D006801:Humans; D008099:Liver / Q000378:metabolism*; D027381:Liver-Specific Organic Anion Transporter 1; D050811:Octamer Transcription Factor-1 / Q000235:genetics / Q000378:metabolism; D050810:Octamer Transcription Factors / Q000235:genetics / Q000378:metabolism*; D027361:Organic Anion Transporters / Q000235:genetics / Q000378:metabolism*; D029362:Organic Anion Transporters, Sodium-Independent / Q000235:genetics / Q000378:metabolism; D004364:Pharmaceutical Preparations / Q000378:metabolism; D010597:Pharmacogenetics; D000074542:Solute Carrier Organic Anion Transporter Family Member 1B3
D027381:Liver-Specific Organic Anion Transporter 1; D050811:Octamer Transcription Factor-1; D050810:Octamer Transcription Factors; D027361:Organic Anion Transporters; D029362:Organic Anion Transporters, Sodium-Independent; D004364:Pharmaceutical Preparations; C503999:SLCO1B1 protein, human; C421209:SLCO1B3 protein, human; C450859:SLCO2B1 protein, human; D000074542:Solute Carrier Organic Anion Transporter Family Member 1B3