Several members of the organic anion transporting polypeptide (OATP/Oatp) family of uptake transporters are expressed in the hepatocyte sinusoidal membrane in humans and preclinical species. The mouse liver specific Oatp is Oatp1b2, and the human homologs most closely related are OATP1B1 and 1B3. The substrate specificity of these transporters is broad, and the widely accepted view is that they...

Genetic polymorphisms in drug-metabolizing enzymes, transporters, receptors, and other drug targets have been linked to interindividual differences in the efficacy and toxicity of many medications. Pharmacogenomic studies are rapidly elucidating the inherited nature of these differences in drug disposition and effects, thereby enhancing drug discovery and providing a stronger scientific basis f...

Various mechanisms can influence the intestinal absorption and oral bioavailability of drugs. The barrier effects of efflux transporters may be one of the critical factors limiting the bioavailability of certain drugs. It has been reported that multidrug resistance-associated protein 2 (Mrp2) is expressed in the mucosal membrane of the epithelium of the small intestine and secretes various drug...

Before a recommendation for antimalarial drug use in pregnancy is made, it is essential that we understand the potential risks involved and have mechanisms in place to monitor risk during treatment. This requires data on drug disposition during pregnancy and potential toxicological liabilities to the developing fetus and mother. In most cases this information is not available. We review the rep...