Target intelligence / Profile preview

Hepatocyte Organic Anion Transporting Polypeptide 1B1 (OATP1B1)

Target
OATP1B1
Molecular classification
Transporter, Solute Carrier, OATP family member
01

Overview

OATP1B1 is a membrane transporter protein primarily expressed on the basolateral (sinusoidal) membrane of human hepatocytes. It belongs to the solute carrier organic anion transporting polypeptide (OATP) family and plays a crucial role in mediating the hepatic uptake of a wide range of endogenous compounds and xenobiotics, including many clinically important drugs. Polymorphisms in SLCO1B1 can markedly affect OATP1B1 function, leading to altered drug pharmacokinetics and increased risk for adverse effects.

Other names
SLCO1B1
02

Mechanism of action

Facilitates Na(+)-independent transport of large amphipathic organic anions across the hepatocyte membrane.

03

Biological functions

Hepatic uptakeDrug transportAnion transportHepatic clearance
04

Disease associations

Drug response variabilityDrug-induced toxicityPharmacokinetics variations
05

Safety considerations

Statin-induced myopathyDrug-drug interactionsMethotrexate toxicity
06

Interacting drugs

Statins (e.g., simvastatin)

5 more in the full profile.

07

Biomarkers

SLCO1B1 c.521T>C (rs4149056)

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