Emerging Treatment Option for Hypercholesterolemia

Azelia Brown, Mercer University College of Pharmacy

Elevated blood levels of low density lipoproteins (LDL) are stated to increase risk for atherosclerotic cardiovascular events.  Statins are the reported agent of choice with proven efficacy, though variation in therapeutic response may require the use of additional therapy. [1]

Serine protease proprotein convertase subtilisin–kexin type 9 (PCSK9) is an enzyme that promotes the degradation of LDL receptors which reduces LDL re-uptake and leads to increased LDL levels. [2]  Some PCSK9 agents are monoclonal antibodies that work by sequestering PCSK9 and preventing it from binding to LDL receptors. Inclisiran interferes with ribonucleic acid, reducing the hepatic production PCSK9. [3]

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Evolocumab and Clinical Outcomes in Patients with Cardiovascular Disease

Sandy Liu, Mercer University College of Pharmacy

A 2016 guideline from the American College of Cardiology stated that the inability to achieve a 30%-50% low-density lipoprotein cholesterol (LDL-C) reduction with statins and/or dietary interventions may necessitate the initiation of the following medications: ezetimibe, bile acid sequestrants and proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors.  [1]

Evolocumab is a human monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 by binding to low-density lipoprotein receptors on hepatocyte surfaces to promote LDL-receptor degradation within the liver, thereby lowering LDL-C levels. [2]

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