Targeting the Proprotein Convertase Subtilisin/Kexin Type 9 for the Treatment of Dyslipidemia and Atherosclerosis

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Targeting the proprotein convertase subtilisin/kexin type 9 for the treatment of dyslipidemia and atherosclerosis.

Hypercholesterolemia is a major risk factor for cardiovascular diseases, increasing the incidence of myocardial infarction and death. Statin-induced lowering of low-density lipoprotein cholesterol (LDL-C) reduces cardiovascular morbidity and mortality. However, many individuals treated with statins do not achieve their target levels of LDL-C, and thus, LDL-associated residual risk remains. Gain...

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Proprotein convertase subtilisin/kexin type 9 enzyme inhibitors: An emerging new therapeutic option for the treatment of dyslipidemia

The treatment of hypercholesterolemia entered in a new phase of development with the introduction of proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitors in the market. The Food and Drug Administration and European Medicines Agency recently approved the alirocumab and evolocumab, subcutaneously injectable monoclonal antibody every 2 or 4 weeks against PCSK9, for the treatment of hyp...

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Gene inactivation of proprotein convertase subtilisin/kexin type 9 reduces atherosclerosis in mice.

BACKGROUND The proprotein convertase subtilisin/kexin type 9 (PCSK9) promotes independently of its enzymatic activity the degradation of the low-density lipoprotein (LDL) receptor. PCSK9 gain of function in humans leads to autosomal dominant hypercholesterolemia, whereas the absence of functional PCSK9 results in ≈7-fold lower levels of LDL cholesterol. This suggests that lowering PCSK9 may pro...

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Inhibition of proprotein convertase subtilisin/kexin type 9 in the treatment of hypercholesterolemia.

Según datos de la Organización Mundial de la Salud, la enfermedad cardiovascular de origen isquémico o arterioscleroso (ECVA) es la primera causa de muerte en el mundo y especialmente en los países desarrollados. La aterosclerosis es una enfermedad arterial multifactorial, en la que el depósito en el espacio subendotelial de las lipoproteínas que transportan apolipoproteína B y colesterol, prin...

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ژورنال

عنوان ژورنال: Journal of the American College of Cardiology

سال: 2013

ISSN: 0735-1097

DOI: 10.1016/j.jacc.2013.07.056