Drug Metabolism & Transporters

OATP1B1

Also known as:OATP-C · LST-1 · Organic anion-transporting polypeptide 1B1

An organic anion-transporting polypeptide, encoded by the SLCO1B1 gene, that mediates uptake of many drugs and endogenous compounds from blood into hepatocytes across the sinusoidal (basolateral) membrane.

In depth

OATP1B1 is expressed almost exclusively in the liver and is often the rate-determining step in the hepatic clearance of statins (notably simvastatin acid, atorvastatin, rosuvastatin and pravastatin), repaglinide, several sartans, methotrexate and endogenous substrates such as bilirubin and coproporphyrin I. Hepatic uptake also delivers statins to their site of action.

The reduced-function SLCO1B1 variant c.521T>C (rs4149056, found in the *5 and *15 haplotypes) increases plasma simvastatin acid exposure and myopathy risk and underpins CPIC statin guidance. Clinically important OATP1B inhibitors include ciclosporin and single-dose rifampicin (both strong) and gemfibrozil.

Clinical pearl

Ciclosporin and gemfibrozil markedly increase exposure to several statins through OATP1B1 inhibition (gemfibrozil also inhibits CYP2C8), raising the risk of myopathy; statin labels restrict or contraindicate many of these combinations.

Example drugs

Simvastatin Rosuvastatin Atorvastatin Repaglinide Methotrexate
TRIn Turkish

OATP1B1

SLCO1B1 geni tarafından kodlanan ve birçok ilacın ve endojen bileşiğin sinüzoidal (bazolateral) membran üzerinden kandan hepatositlere alımını sağlayan bir organik anyon taşıyıcı polipeptittir.

OATP1B1 hemen yalnızca karaciğerde eksprese edilir ve statinlerin (özellikle simvastatin asit, atorvastatin, rosuvastatin ve pravastatin), repaglinidin, bazı sartanların, metotreksatın ve bilirubin ile koproporfirin I gibi endojen substratların hepatik klirensinde çoğu zaman hızı belirleyen basamaktır. Hepatik alım statinleri etki yerlerine de ulaştırır.

İşlevi azalmış SLCO1B1 c.521T>C varyantı (rs4149056; *5 ve *15 haplotiplerinde bulunur) plazma simvastatin asit maruziyetini ve miyopati riskini artırır ve CPIC'in statin önerilerinin temelini oluşturur. Klinik açıdan önemli OATP1B inhibitörleri arasında siklosporin ve tek doz rifampisin (her ikisi de güçlü) ile gemfibrozil yer alır.

Siklosporin ve gemfibrozil OATP1B1 inhibisyonu yoluyla (gemfibrozil ayrıca CYP2C8'i inhibe eder) birçok statine maruziyeti belirgin şekilde artırarak miyopati riskini yükseltir; statinlerin KÜB'leri bu kombinasyonların çoğunu kısıtlar veya kontrendike sayar.

Diğer adları:Organik anyon taşıyıcı polipeptit 1B1
Updated 24.09.2026 0 views Educational reference — verify against current sources before clinical use.

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Drug Transporterİlaç Taşıyıcısı

A membrane protein that moves drugs across cell membranes, either into cells (uptake) or out of them (efflux), and thereby influences absorption, distribution and elimination.

 Hepatic ClearanceHepatik Klirens

The component of total clearance due to hepatic metabolism and biliary excretion; the volume of blood cleared of drug by the liver per unit time.

 PharmacogenomicsFarmakogenomik

The study of how inherited genetic variation affects an individual's response to drugs, used clinically to guide drug and dose selection.

 Genetic PolymorphismGenetik Polimorfizm

A DNA sequence variation, such as a single-nucleotide change or a copy-number variant, present in more than about 1% of a population.

 CPIC GuidelineCPIC Kılavuzu

A peer-reviewed, evidence-based prescribing recommendation issued by the Clinical Pharmacogenetics Implementation Consortium for a specific gene–drug pair.

 Pharmacokinetic InteractionFarmakokinetik Etkileşim

An interaction in which one drug alters the absorption, distribution, metabolism or excretion of another, so that the concentrations of the affected drug change rather than its concentration–effect relationship.