Atherosclerosis I: LDL Cholesterol Lowering

Abstract

Lowering LDL cholesterol in patients has been directly linked to lowering the incidence of cardiovascular disease and represents one of the most successful avenues of medicinal chemistry. This chapter discusses current drugs on the market and in development that effectively lower this key biomarker of heart disease. Mechanistic pathways presented are HMG-CoA reductase inhibition, cholesterol absorption inhibition (NPC1L1 inhibition), and the use of bile acid sequestrants. New therapeutic targets, such as PCSK9, antisense apoB 100 and MTP inhibition, as well as combination therapy are also presented. Keywords: bile acid sequestrants; ezetimibe; LDL cholesterol; lipid lowering agents; statins