Transporters Involved In Pharmacokinetics Hepatic Transporters

HMG-CoA REDUCTASE INHIBITORS

Statins are cholesterol-lowering agents that reversibly inhibit HMG-CoA reductase, which catalyzes a rate-limiting step in cholesterol biosynthesis (see Chapter 35). Most of the statins in the acid form are substrates of uptake transporters that mediate hepatic uptake and enterohepatic circulation (Figures 2—5 and 2-6). In this process, hepatic uptake transporters such as OATP1B1 and efflux transporters such as MRP2 cooperate to produce vectorial transcellular transport of bisubstrates in the liver. The efficient first-pass hepatic uptake of statins by OATP1B1 helps them to exert their pharmacological effect and also minimizes the systemic drug distribution, thereby minimizing adverse effects in smooth muscle. Recently, two common SNPs in SLCO1B1 (OATP1B1) have been associated with elevated plasma levels of pravastatin.

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