Drug development report (6): Pravastatin: A hydrophilic inhibitor of cholesterol synthesis

The development of the 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA)-reductase inhibitors has resulted in a more rational and effective approach to the treatment of hypercholesterolaemia. Pravastatin is a member of this group of drugs which is characterised by its hydrophilic property. The development of pravastatin is reviewed and its physical properties compared to those of other HMG-CoA reductase inhibitors. In addition, the clinical efficacy and safety-in-use of the drug are discussed. It is concluded that the hydrophilic nature of the drug results in selective cellular uptake and inhibition of cholesterol synthesis. Pravastatin is selectively taken up by hepatocytes with minimal uptake into peripheral cells.