Pleiotropic Effects of PCSK-9 Inhibitors
| Autor: | Michał Kosowski, Mateusz Maligłówka, Łukasz Bułdak, Marcin Cyrnek, Grzegorz Machnik, Marcin Basiak, Bogusław Okopień |
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| Rok vydání: | 2021 |
| Předmět: |
Review
Familial hypercholesterolemia 030204 cardiovascular system & hematology Pharmacology Bococizumab lcsh:Chemistry 0302 clinical medicine vaccine hyperlipidemia 030212 general & internal medicine lcsh:QH301-705.5 Spectroscopy Anticholesteremic Agents PCSK9 Inhibitors General Medicine Plaque Atherosclerotic Anti-Bacterial Agents Computer Science Applications new lipid lowering-drugs anti-atherosclerotic effect medicine.symptom medicine.drug Statin anti-aggregation effect medicine.drug_class Antineoplastic Agents pleiotropic effects antineoplastic effect Protein Aggregation Pathological Catalysis Inorganic Chemistry 03 medical and health sciences Ezetimibe medicine Animals Humans Protease Inhibitors Physical and Theoretical Chemistry Blood Coagulation Molecular Biology Alirocumab business.industry Organic Chemistry Anticoagulants anticoagulant effect medicine.disease PCSK-9 Evolocumab lcsh:Biology (General) lcsh:QD1-999 bacterial infections Mechanism of action Humanized mouse business |
| Zdroj: | International Journal of Molecular Sciences International Journal of Molecular Sciences, Vol 22, Iss 3144, p 3144 (2021) |
| ISSN: | 1422-0067 |
| Popis: | Proprotein convertase subtilisin/kexin type 9 (PCSK-9) inhibitors are a group of drugs whose main mechanism of action is binding to the PCSK-9 molecule, which reduces the degradation of the low-density lipoprotein receptor (LDL-R) and, hence, increases the uptake of low-density lipoprotein cholesterol (LDLc) from the bloodstream as well as reducing its concentration. The effectiveness of three monoclonal antibodies, namely, alirocumab (human IgG1/κ monoclonal antibody, genetically engineered in Chinese hamster ovary cells), evolocumab (the first fully human monoclonal antibody), and bococizumab (humanized mouse antibody), in inhibiting the action of PCSK-9 and reducing LDLc levels has been confirmed. The first two, after clinical trials, were approved by the Food and Drug Administration (FDA) and are used primarily in the treatment of autosomal familial hypercholesterolemia and in cases of statin intolerance. They are currently used both as monotherapy and in combination with statins and ezetimibe to intensify therapy and achieve therapeutic goals following the American Heart Association (AHA) and European Society of Cardiology (ESC) guidelines. However, the lipid-lowering effect is not the only effect of action described by researchers that PCSK-9 inhibitors have. This paper is a review of the literature describing the pleiotropic effects of PCSK-9 inhibitors, which belong to a group of drugs that are being increasingly used, especially when standard lipid-lowering therapy fails. The article focuses on activities other than lipid-lowering, such as the anti-atherosclerotic effect and stabilization of atherosclerotic plaque, the anti-aggregation effect, the anticoagulant effect, the antineoplastic effect, and the ability to influence the course of bacterial infections. In this publication, we try to systematically review the current scientific data, both from our own scientific work and knowledge from international publications. |
| Databáze: | OpenAIRE |
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