Organic anion transporting polypeptide 1B1 (SLCO1B1)
Also known as: OATP1B1, SLCO1B1, OATP-C
Hepatic uptake transporter (SLCO1B1) that mediates drug entry into hepatocytes, including most statins (simvastatin, atorvastatin, rosuvastatin, pravastatin).
OATP1B1 inhibition (e.g. ciclosporin, clarithromycin) reduces hepatic uptake of statins and raises systemic concentrations, with risk of myopathy and rhabdomyolysis.
Substrates: simvastatin, atorvastatin, rosuvastatin, pravastatin, repaglinide, methotrexate, rifampicin.
Inhibitors: ciclosporin, clarithromycin, gemfibrozil, ritonavir, rifampicin (single dose).
Inducers: not applicable (uptake transport, not metabolism).
The SLCO1B1 polymorphism and inhibition by ciclosporin/clarithromycin explain statin myopathy risk in transplant patients.
DailyMed/FDA (NIH/NLM) — approved labels (simvastatin, rosuvastatin); PubMed (NIH/NLM)
