Prakt. Lékáren. 2017; 13(3e) [Klin Farmakol Farm. 2016;30(4):11-13]

Monoclonal antibodies in treating high cholesterol levels

Rostislav Večeřa
Ústav farmakologie, Lékařská fakulta Univerzity Palackého, Olomouc

Proprotein convertase subtilisin-kexin type 9 (PCSK9) is mainly responsible for the recycling receptors for LDL particles. This results in an increasein LDL levels, which then drastically contributes to the development of atherosclerotic changes in vessel wall. This increases cardiovascularmorbidity and mortality. New drugs based on monoclonal antibodies as alirocumab or evolocumab belongs among PCSK9 inhibitors. Theiradministration leads to a dramatic reduction in LDL particles up to 50–60 %. Given that the Czech Republic ranks among the countries withhigh cardiovascular mortality, is introduction of these new drugs in clinical practice one of the key milestones in the treatment of high bloodlipid levels and improve this negative situation.

Keywords: alirocumab, evolocumab, hypercholesterolemia, PCSK9, cholesterol

Received: April 17, 2018; Accepted: July 24, 2018; Prepublished online: July 24, 2018; Published: October 1, 2017  Show citation

ACS AIP APA ASA Harvard Chicago Chicago Notes IEEE ISO690 MLA NLM Turabian Vancouver
Večeřa R. Monoclonal antibodies in treating high cholesterol levels. Praktické lékárenství. 2017;13(E-verze 3/17):.
Download citation

References

  1. Albiero M, Avogaro A, Fadini GP. A perspective on sirtuins in the metabolic syndrome. Metab Syndr Relat Disord. 2015; 13(4): 161-164. Go to original source... Go to PubMed...
  2. Rizzo M, Rizvi AA, Rini GB, Berneis K. The therapeutic modulation of atherogenic dyslipidemia and inflammatory markers in the metabolic syndrome: what is the clinical relevance? Acta Diabetol. 2009; 46(1): 1-11. Go to original source... Go to PubMed...
  3. Cífková R, Bruthans J, Adámková V, et al. Prevalence základních kardiovaskulárních rizikových faktorů v české populaci v letech 2006-2009. Studie Czech post-Monica. Cor Vasa 2011; 53: 220-229. Go to original source...
  4. Bláha V. Léčba hypercholesterolemie inhibitory PCSK9. Interní Med. 2014; 16(5): 179-183.
  5. Bultas J. Význam proproteinových konvertáz subtilisin/kexinového typu (PCSK) nejen v regulaci metabolismu lipidů. Remedia 2016; 2: 117-122.
  6. Turpeinen H, Ortutay Z, Pesu M. Genetics of the first seven proprotein convertase enzymes in health and disease. Curr Genomics 2013; 14: 453-467. Go to original source... Go to PubMed...
  7. Chen S, Cao P, Dong N, et al. PCSK6-mediated corin activation is essential for normal blood pressure. Nat Med 2015; 21: 1048-1053. Go to original source... Go to PubMed...
  8. Sun H, Samarghandi A, Zhang N, et al. Proprotein Convertase Subtilisin/Kexin Type 9 interact with apolipoprotein B and prevents its intracellular degradation, irrespective of the low-density lipoprotein receptor. Arterioscler Thromb Vasc Biol 2012; 32: 1585-1595. Go to original source... Go to PubMed...
  9. Le May C, Kourimate S, Langhi C, Chétiveaux M, et al. Proprotein convertase subtilisin kexin type 9 null mice are protected from postprandial triglyceridemia. Arterioscler Thromb Vasc Biol. 2009; 29: 684-690. Go to original source... Go to PubMed...
  10. Levy E, Ben Djoudi Ouadda A, Spahis S, Sane AT, et al. PCSK9 plays a significant role in cholesterol homeostasis and lipid transport in intestinal epithelial cells. Atherosclerosis. 2013; 227: 297-306. Go to original source... Go to PubMed...
  11. Vráblík M. Evolocumab: snížení hodnot LDL cholesterolu i kardiovaskulárního rizika. Remedia 2015; 6: 403-406.
  12. SPC přípravku Praluent 150 mg: http://www.ema.europa.eu/docs/cs_CZ/document_library/EPAR_-_Product_Information/human/003882/WC500194521.pdf
  13. Stroes E, Guyton JR, Lepor N, Civeira F, et al. Efficacy and Safety of Alirocumab 150 mg Every 4 Weeks in Patients With Hypercholesterolemia Not on Statin Therapy: The ODYSSEY CHOICE II Study. J Am Heart Assoc. 2016; 13: 5(9), pii: e003421. doi: 10.1161/JAHA.116.003421.https://www.ncbi.nlm.nih.gov/pubmed/?term=ODYSSEY%20CHOICE%20II%20Investigators%5BCorporate%20Author%5D Go to original source... Go to PubMed...
  14. Raal FJ, Honarpour N, Blom DJ, Hovingh GK, et al. Inhibition of PCSK9 with evolocumab in homozygous familial hypercholesterolaemia (TESLA Part B): a randomised, double-blind, placebo-controlled trial. Lancet. 2015; 24: 385(9965): 341-350. Go to original source... Go to PubMed...
  15. SPC přípravku Repatha 140 mg: http://www.ema.europa.eu/docs/cs_CZ/document_library/EPAR_-_Product_Information/human/003766/WC500191398.pdf




Pharmacy for Practice

Madam, Sir,
please be aware that the website on which you intend to enter, not the general public because it contains technical information about medicines, including advertisements relating to medicinal products. This information and communication professionals are solely under §2 of the Act n.40/1995 Coll. Is active persons authorized to prescribe or supply (hereinafter expert).
Take note that if you are not an expert, you run the risk of danger to their health or the health of other persons, if you the obtained information improperly understood or interpreted, and especially advertising which may be part of this site, or whether you used it for self-diagnosis or medical treatment, whether in relation to each other in person or in relation to others.

I declare:

  1. that I have met the above instruction
  2. I'm an expert within the meaning of the Act n.40/1995 Coll. the regulation of advertising, as amended, and I am aware of the risks that would be a person other than the expert input to these sites exhibited


No

Yes

If your statement is not true, please be aware
that brings the risk of danger to their health or the health of others.