The therapeutic potential of PCSK9 inhibition in primary dyslipidemia, the example from SAR236553/REGN727

Abstract

The proprotein convertase subtilisin kexin 9 (PCSK9) is a serine protease that has recently emerged as a potential target for the treatment of hypercholesterolemia. SAR236553/REGN727 is a highly specific monoclonal antibody to PCSK9 that significantly reduced LDL cholesterol levels in healthy volunteers and in subjects with hypercholesterolemia in three Phase-I studies. It was subsequently tested in a recent Phase-II study in patients with primary hypercholesterolemia with impressive results. In this report the trial is discussed along with the significance of the results in guiding further research in PCSK9 inhibition.