Targeting pro-protein convertase subtilisin kexin-9 as a novel therapy of hypercholesterolemia
Abstract: Reducing low density
lipoprotein (LDL) cholesterol level is an established primary and secondary
prevention strategy for coronary heart disease. However, not all patients are
able to achieve their LDL targets as recommended by the guidelines. Over the
last 10 years, high plasma LDL level is known to be associated with a higher
level of pro-protein convertase subtilisin kexin-9 (PCSK-9). Loss-of-function
mutations in the PCSK-9 gene is associated with lower plasma LDL level and
cardiovascular risk. Since its discovery in 2003, PCSK-9 has triggered many
researchers to design a PCSK-9 inhibitor to reduce LDL cholesterol through
competitive inhibition of this molecule. Some phase III clinical trials have
showed promising results of PCSK-9 inhibitor efficacy in lowering LDL level and
improving clinical outcome. This article aims to discuss the role of PCSK-9 in
LDL metabolism and the efficacy of PCSK-9 inhibitor in reducing plasma LDL
level.
Keywords: low density
lipoprotein; PCSK-9 inhibitor; pro-protein convertase subtilisin kexin-9
Author: Bambang Dwiputra,
Anwar Santoso, Kian K. Poh
Journal Code: jpkedokterangg170189