HMG-CoA reductase inhibitors - a review of the recent patent literature.
Statins are very potent inhibitors of HMG-CoA reductase, the rate-limiting enzyme in cholesterol biosynthesis at the mevalonate level. Today there is an increasing tendency to treat hypercholesterolemia aggressively, hence, the greater use of statins worldwide. The pleiotropic effect of statins is well documented. Examination of the patent literature reveals that in the past year pharmaceutical companies continued to be very active in this area. Accumulated knowledge of the actions of statins shows that they may be involved in many more processes than originally anticipated. Hence, in addition to 'old' indications (hypercholesterolemia, hyperlipidemia and atherosclerosis) many patent applications published in 2001 attempted to cover combination therapies, widening indications for statins to almost all known diseases. Many of the 'new' claims are not well substantiated and biological data are absent. Based on the magnitude of cardiovascular disease and aging population globally this area of drug discovery will continue to be an important area of research for all pharmaceutical companies.
Bagi
Cedo M
CM
Pfizer Inc, Eastern Point Road 8274-1312, Groton, CT 06340, USA. cedo_bagi@groton.pfizer.com