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Lipoprotein(a) lowering and cardiovascular risk reduction by PCSK9 inhibitors
Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibition augments recirculation of the low-density lipoprotein (LDL) receptor to the hepatocyte surface [1], thereby lowering atherogenic particles through accelerated clearance of circulating LDL cholesterol (LDL-C). This observation led to several strategies to inhibit PCSK9, including monoclonal antibodies (evolocumab and alirocumab), small-molecule inhibitors specific to PCSK9, small interfering RNA (siRNA) molecules (inclisiran), antisense oligonucleotides, immunotherapy with a PCSK9 peptide vaccine, and CRISPR/Cas9 editing of PCSK9.
Source: Atherosclerosis - October 21, 2022 Category: Cardiology Authors: Maya S. Safarova, Iftikhar J. Kullo Tags: Editorial Source Type: research

Expanding Biology of PCSK9: Roles in Atherosclerosis and Beyond
Curr Atheroscler Rep. 2022 Jul 29. doi: 10.1007/s11883-022-01057-z. Online ahead of print.ABSTRACTPURPOSE OF REVIEW: Since the discovery of PCSK9 in 2003, this proprotein convertase was shown to target specific receptors for degradation in endosomes/lysosomes, including LDLR and other family members and hence to enhance the levels of circulating LDL-cholesterol (LDLc). Accordingly, inhibitors of PCSK9, including monoclonal antibodies blocking its circulating activity and siRNA silencers of its hepatic expression, are now used in clinics worldwide to treat hypercholesterolemia patients effectively and safely in combination ...
Source: Atherosclerosis - July 29, 2022 Category: Cardiology Authors: Nabil G Seidah Damien Gar çon Source Type: research

PCSK9 inhibitors and LDL reduction: pharmacology, clinical implications and future perspectives.
Authors: Fitzgerald G, Kiernan T Abstract INTRODUCTION: PCSK9 inhibitors are monoclonal antibodies to proprotein convertase-subtilisin/kexin type 9 which significantly reduce LDL cholesterol concentration in vivo by inhibiting degradation of the LDL receptor in hepatocytes. The introduction of PCSK9 inhibitors heralded a new era of intensive LDL-C reduction with LDL-C concentrations lowered below levels ever thought possible with conventional treatments such as statins. With their introduction considerations regarding cost, clinical outcomes and long-term safety are paramount. Areas covered: This review examines th...
Source: Expert Review of Cardiovascular Therapy - July 8, 2018 Category: Cardiology Tags: Expert Rev Cardiovasc Ther Source Type: research