207 KB15 KB200520252022Štrukelj, Borutštevilka:2letnik:73str. 137-140ISSN:0014-8229COBISSID_HOST:108483075URN:URN:NBN:SI:doc-X2ZJ2JJ9slSlovensko farmacevtsko društvoFarmacevtski vestnikHolesterolinklisiranLDL-holesterolmonoklonska protitelesazaviralci PCSK-9Novosti pri zdravljenju povišanega holesterola| Novel treatment approaches against elevated levels of cholesterol|Low-density lipoprotein cholesterol (LDL-cholesterol) is one of the most important causal factors associated with cardiovascular diseases. Among established therapies with statins and ezetimib, the last decade has been focused in the development and use of PCSK-9 inhibitors. The PCSK-9 protein binds to an LDL receptor and accelerates its degradation and increases levels of LDL-cholesterol. Two human monoclonal antibodies, evolocumab and alirocumab, are used as PCSK-9 inhibitors, while an even more revolutionary approach has been reached by a small two-stranded interfering RNA (siRNA), known as inclisiran. Inclisiran binds to mRNA for PCSK-9 and triggers its degradation, which results in increased uptake and metabolism of LDL-cholesterol in hepatocytes, and a decrease of LDL-cholesterol plasma levelsholesterol v lipoproteinih majhne gostote (LDL-holesterol) je eden od najpomembnejših vzročnih dejavnikov nastanka srčno-žilnih bolezni. Poleg že uveljavljenega zdravljenja s statini in ezetimibom je zadnje desetletje namenjeno razvoju in uporabi zaviralcev proteina PCSK-9, ki z vezavo na receptor LDL pospeši njegovo razgradnjo in s tem viša vrednosti LDL-holesterola. V ta namen uporabljamo dve humani monoklonski protitelesi evolokumab in alirokumab, še večjo revolucijo v zdravljenju pa predstavlja majhna dvovijačna interferenčna RNA (siRNA), imenovana inklisiran. Delovanje inklisirana je povezano z vezavo in razgradnjo mRNA za PCSK-9, kar vodi do večjega privzema in metabolizma LDL-holesterola v hepatocitih in posledično njegovega zmanjšanja v plazmiTEXTznanstveno časopisjejournalsSlovenian National E-content AggregatorNational and University Library of SloveniaSlovensko farmacevtsko društvo