In the early 1970s we isolated the first statin, mevastatin (formerly called compactin or ML-236B), from Penicillium citrinum, as a potent inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the rate-controlling enzyme in cholesterol synthetic pathway. By the end of the 1970s we had demonstrated that mevastatin was highly effective in lowering serum total and low-density lipoprotein (LDL) cholesterol in both experimental animals and patients with primary hypercholesterolemia. The discovery of mevastatin paved the way for the worldwide development of its analogues (statins), and since then several statins-lovastatin, simvastatin, pravastatin, fluvastatin and atorvastatin-have been approved in many countries and are currently used by millions of patients. (C) 2004 Elsevier B.V. All rights reserved.