Международный эндокринологический журнал Том 19, №3, 2023
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Бемпедоєва кислота: механізм дії та застосування при атеросклеротичних серцево-судинних захворюваннях і цукровому діабеті
Авторы: Сергієнко В.О., Сергієнко О.О.
Львівський національний медичний університет імені Данила Галицького, м. Львів, Україна
Рубрики: Эндокринология
Разделы: Справочник специалиста
Версия для печати
Бемпедоєва кислота — новий лікарський засіб (ЛЗ) для зниження рівня холестерину, який нещодавно отримав схвалення Управління з контролю за продуктами й ліками США та Європейського агентства з лікарських засобів. Цей ЛЗ націлений на метаболізм ліпідів і глюкози, а також на запалення шляхом зниження регуляції аденозинтрифосфатцитратліази та підвищення регуляції аденозинмонофосфат-активованої протеїнкінази (AMPK). Основним ефектом є зниження синтезу холестерину в печінці, і його використання, як правило, не пов’язане з небажаними м’язовими розладами. Бемпедоєва кислота може зменшувати процеси глюконеогенезу, що призводить до покращення чутливості до інсуліну, метаболізму глюкози й особливостей перебігу метаболічного синдрому. Протизапальна дія бемпедоєвої кислоти переважно досягається шляхом активації шляху AMPK в імунних клітинах, що сприяє зниженню рівня С-реактивного білка в плазмі. Вплив бемпедоєвої кислоти на перебіг атеросклеротичних серцево-судинних захворювань, цукрового діабету 2-го типу і хронічних захворювань печінки оцінювали в рандомізованих клінічних дослідженнях, які потребують проведення подальших випробувань. Клінічні дослідження безпеки у фазі III показують, що бемпедоєва кислота загалом добре переноситься в комбінації зі статинами, езетимібом або інгібіторами пропротеїнової конвертази субтилізин/кексин типу 9 для досягнення цільових показників холестерину ліпопротеїнів низької щільності. Метою цього огляду є аналіз основних механізмів дії, потенційних клінічних цілей бемпедоєвої кислоти та опис існуючих доказів клінічних випробувань. Пошук проводився в Scopus, Science Direct (від Elsevier) і PubMed, включно з базами даних Medline. Використані ключові слова «бемпедоєва кислота», «холестерин ліпопротеїнів низької щільності», «атеросклеротичні серцево-судинні захворювання», «цукровий діабет». Для виявлення результатів дослідження, які не вдалося знайти під час онлайн-пошуку, використовувався ручний пошук бібліографії публікацій.
Bempedoic acid is a new cholesterol-lowering drug that recently received approval from the US Food and Drug Administration and the European Medicines Agency. This drug targets lipid and glucose metabolism as well as inflammation by downregulating the ATP citrate lyase and upregulating of AMP-activated protein kinase (AMPK). The main effect is to reduce cholesterol synthesis in the liver, and its use is generally not associated with undesirable muscle disorders. Bempedoic acid can reduce the processes of gluconeogenesis, which leads to an improvement in insulin sensitivity, glucose metabolism and features of the metabolic syndrome. The anti-inflammatory effect of bempedoic acid is mainly achieved by activating the AMPK pathway in immune cells, which helps reduce the level of C-reactive protein in plasma. The effects of bempedoic acid on the course of atherosclerotic cardiovascular disease, type 2 diabetes and chronic liver disease have been evaluated in randomized clinical trials that require further research. Phase III clinical safety trial show that bempedoic acid is generally well tolerated in combination with statins, ezetimibe, or proprotein convertase subtilisin/kexin type 9 inhibitors in achieving target levels of low-density lipoprotein cholesterol. The aim of this review is to analyze the main mechanisms of action, potential clinical targets of bempedoic acid and describe the existing evidence from clinical trials. The search was done in the Scopus, Science Direct (from Elsevier), and PubMed databases, including the Medline. The following keywords were used: bempedoic acid, low-density lipoprotein cholesterol, atherosclerotic cardiovascular diseases, diabetes. In order to identify research results that could not be found during the online search, a manual search of the bibliography of publications was used.
бемпедоєва кислота; холестерин ліпопротеїнів низької щільності; атеросклеротичні серцево-судинні захворювання; цукровий діабет 2-го типу; огляд
bempedoic acid; low-density lipoprotein cholesterol; atherosclerotic cardiovascular diseases; type 2 diabetes; review
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