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Evolocumab (AMG 145) is a human monoclonal antibody that inhibits PCSK9. Evolocumab is used in the study of hypercholesterolemia and atherosclerotic cardiovascular disease. Evolocumab binds to circulating PCSK9 protein and inhibits its binding to LDLR. Evolocumab has antioxidant and cytoprotective activities against H2O2-induced oxidative damage to endothelial cells. Evolocumab may also negatively regulate activation of the TLR-4/NF-κB signaling pathway to prevent inflammation[1][2][3]. | [Clinical Use]
IgG2 monoclonal antibody:Treatment of hypercholesterolaemia, mixed
dyslipidaemia and homozygous familial
hypercholesterolaemia | [Drug interactions]
Potentially hazardous interactions with other drugs
Antipsychotics: avoid with clozapine - increased risk
of agranulocytosis.
Vaccines: avoid concomitant use with live vaccines. | [Metabolism]
Evolocumab is composed of amino acids and
carbohydrates as native immunoglobulin and is unlikely
to be eliminated via hepatic metabolic mechanisms.
Its metabolism and elimination are expected to follow
the immunoglobulin clearance pathways, resulting in
degradation to small peptides and individual amino acids. | [References]
[1] Fala L, et, al. Repatha (Evolocumab): Second PCSK9 Inhibitor Approved by the FDA for Patients with Familial Hypercholesterolemia. Am Health Drug Benefits. 2016 Mar;9(Spec Feature):136-9. PMID:27668060
[2] Zhou Q, et al. Protective effect of evolocumab on Müller cells in the rat retina under hyperglycaemic and hypoxic conditions. J Diabetes Complications. 2023 Oct;37(10):108593. DOI:10.1016/j.jdiacomp.2023.108593
[3] Safaeian L, et al. Evolocumab, a PCSK9 inhibitor, protects human endothelial cells against H2O2-induced oxidative stress. Arch Physiol Biochem. 2022 Dec;128(6):1681-1686. DOI:10.1080/13813455.2020.1788605 |
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