PCSK9 Inhibition for Patients with Hypercholesterolemia

Proprotein convertase subtilisin kexin type 9 (PCSK9) is a serine protease that plays an important role in modulating low density lipoprotein cholesterol (LDL-C) levels by targeting LDL-C receptors for lysosomal degradation. Genetic association studies have demonstrated that loss-of-function mutations in PCSK9 are associated with low plasma LDL-C levels and a reduction in the incidence of adverse cardiovascular events. Monoclonal antibodies directed against PCSK9 have been developed and have been shown in phase 1, 2, and 3 trials to dramatically reduce LDL-C regardless of background lipid lowering therapy, including in clinically challenging populations such as patients intolerant of statin therapy and those with familial hypercholesterolemia.

Source: Trends in Cardiovascular Medicine - February 10, 2015 Category: Cardiology Authors: Nihar R. Desai, Marc S. Sabatine Source Type: research