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Target intelligence / Profile preview
Organic Anion Transporting Polypeptide 1B1 (OATP1B1)
- Target
- OATP1B1
- Molecular classification
- Transporter, Membrane Transport Protein
01
Overview
Organic anion transporting polypeptide 1B1 (OATP1B1) is a membrane-bound transporter protein primarily expressed on the basolateral membrane of human hepatocytes. It mediates the sodium-independent facilitated transport of large amphipathic organic anions into liver cells, playing a crucial role in the hepatic uptake of a wide range of endogenous compounds and xenobiotics, including many clinically important drugs. Genetic polymorphisms in SLCO1B1 can significantly alter transporter activity, impacting drug pharmacokinetics and potentially leading to adverse drug reactions or altered efficacy.
- Other names
- SLCO1B1
02
Mechanism of action
Facilitated transport of organic anions across the hepatocyte membrane; inhibition of transport by competing substrates or inhibitors
03
Biological functions
Hepatic uptake of drugsHepatic uptake of endogenous compoundsDrug clearanceToxin removalHormone regulation
04
Disease associations
Drug-drug interactionsAdverse drug reactionsPharmacogenetic variations in drug response
05
Safety considerations
Statin-induced myopathy (related to SLCO1B1 polymorphisms)Drug-drug interactions leading to altered drug efficacy or toxicity
06
Interacting drugs
Statins (simvastatin acid)
5 more in the full profile.
07
Biomarkers
SLCO1B1 genotype (e.g., c.521T>C)
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