PCSK9 INHIBITORS

Course overview

FAMILIAL HYPERCHOLESTEROLEMIA IS CHARACTERIZED BY EXTREMELY HIGH TOTAL AND LDL CHOLESTEROL LEVELS, PREMATURE VASCULAR DISEASE, AND TENDON XANTHOMAS. IN MOST CASES, THIS IS DUE TO A GENETIC MUTATION OF THE LDL RECEPTOR, RARELY MUTATIONS OF THE APOPROTEIN B100 OR PCSK9 GENES. THERE ARE THREE PHARMACEUTICAL PRODUCTS AVAILABLE IN THE UNITED STATES THAT REDUCE PCSK9 ACTIVITY: ALIROCUMAB, EVOLOCUMAB, AND INCLISIRAN. ALIROCUMAB AND EVOLOCUMAB ARE FULLY-HUMANIZED MONOCLONAL ANTIBODIES. INCLISIRAN IS A SMALL INTERFERING MRNA THAT INHIBITS THE INTRACELLULAR SYNTHESIS OF PCSK9. THIS ACTIVITY OUTLINES THE INDICATIONS, MECHANISM OF ACTION, ADMINISTRATION METHODS, SIGNIFICANT ADVERSE EFFECTS, CONTRAINDICATIONS, MONITORING, AND TOXICITY OF PCSK9 INHIBITORS SO PROVIDERS CAN DIRECT PATIENT THERAPY TO OPTIMAL OUTCOMES IN SERUM LIPID MANAGEMENT WITH THESE AGENTS AND OBTAIN IMPROVED CARDIOVASCULAR OUTCOMES.