Pleiotropy (drugs) Pleiotropy (drugs) In pharmacology, pleiotropy includes all of a drug's actions other than those for which the agent was specifically developed. It may include adverse effects which are detrimental ones, but is often used to denote additional beneficial effects. For example, statins are HMG-CoA reductase inhibitors that primarily act by decreasing cholesterol synthesis, but which are believed to have other beneficial effects, including acting as antioxidants and stabilizing atherosclerotic plaques. Steroid drugs, such as prednisone and prednisolone, have pleiotropic effects, including systemic ones, for the same reason that endogenous steroid hormones do too: cells throughout the body have receptors that
Discovery and development of statins is needed for normal cell function and inhibition in non-hepatic cells could possibly be harmful. The essential structural components of all statins are a dihydroxyheptanoic acid unit and a ring system with different substituents. The statin pharmacophore is modified hydroxyglutaric acid component, which is structurally similar to the endogenous substrate HMG CoA and the mevaldyl CoA transition state intermediate (Figure 1). The statin pharmacophore binds to the same active site as the substrate HMG-CoA and inhibits the HMGR enzyme. It has also been shown that the HMGR is stereoselective and as a result all statins need to have the required