Characteristics and effectiveness of evolocumab in hyperlipidemia treatment

• Konovalov G.A.

Abstract

Despite proven effectiveness of statin therapy, under pressure of statin therapy target values of low density lipoproteins (LDL) cholesterol concentration are often not achieved (especially in high-risk patients). Moreover, significant number of patients cannot tolerate statins at all or in maximum doses. This applies in particular to patients suffering from familial hypercholesterolemia, because of decreasing the number of receptors on liver cells. Thus, there remains a need for additional effective agents for reducing LDL cholesterol concentration. Evolocumab (AMG145) is a monoclonal antibody that inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9), which binding to LDL receptors in the liver and contribute to their destruction. In phase I, II and III studies it was shown that evolocumab in case of subcutaneously injection when used alone or in combination with statins, provides significant dose-dependent LDL cholesterol concentration reduction by 54–80%, apolipoprotein B100 – by 31–61%, and lipoprotein (a) – by 12–36%. Low frequency of side effects was registered, that were limited mainly by nasopharyngitis, injection pain, arthralgia and back pain. Evolocumab is an innovative powerful lipid-lowering medication with additive effect in case of combination with statins and/or ezetimibe. It has wide therapeutic range that provides low incidence of adverse events, mainly mild intensity. If already obtained data will be confirmed in hard endpoints evaluation long-term studies than evolocumab will become an indispensable drug for therapy in a wide range of high-risk patients, in particular suffering from familial hypercholesterolemia (in case of effective doses of statins intolerance), as well as for patients with a very high risk of cardiovasculare pathology, who are not capable of reaching target values of LDL cholesterol concentration on the background of currently available lipid-lowering therapy.

Keywords:hypercholesterolemia, lipidlowering agents, proprotein convertase subtilisin/kexin type 9 (PCSK9), evolocumab (AMG145)

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