Abstract
Dabigatran etexilate is a prodrug of dabigatran, a direct inhibitor of thrombin. Pharmacokinetics of dabigatran etexilate doesn’t have the disadvantages of vitamin K antagonists. It is considered that CES1 enzyme and P-glycoprotein (CES1 and ABCB1 genes accordingly) play important role in pharmacokinetics of dabigatran etexilate. UDP-glucuronosyltransferase enzymes UGT2B15, UGT1A9, UGT2B7 (UGT2B15, UGT1A9, UGT2B7 genes accordingly) take part in the metabolism of active dabigatran. Presence of these gene’s single-nucleotide variants (SNV) can affect effectiveness and safety of dabigatran etexilate usage. The goal of this review is analysis of promising areas of associated researches of SNV of genes CES1 and ABCB1 and search for new candidate genes that reveal effectiveness and safety of dabigatran etexilate usage.
Highlights
1 – Bekhterev National Medical Research Center of Psychiatry and Neurology, St.-Petersburg 2 – FSBEI НЕ Prof
Dabigatran etexilate is a prodrug of dabigatran
Pharmacokinetics of dabigatran etexilate doesn't have the disadvantages of vitamin K antagonists
Summary
Перспективные направления исследования фармакогенетики дабигатрана этексилата Савинова А. 1 – ФГБУ Национальный медицинский исследовательский центр психиатрии и неврологии им. Носительство однонуклеотидных вариантов (ОНВ) этих генов может влиять на эффективность и безопасность применения дабигатрана этексилата. Целью данного обзора является анализ перспективных направлений ассоциативных исследований ОНВ генов CES1 и ABCB1, а также поиск новых генов-кандидатов, отражающих эффективность и безопасность применения дабигатрана. Ключевые слова: дабигатрана этексилат; дабигатран; фармакокинетика; фармакогенетика; эффективность; безопасность; CES1; ABCB1; UGT2B15. Для цитирования: Савинова А.В., Шнайдер Н.А., Петрова М.М., Насырова Р.Ф. Перспективные направления исследования фармакогенетики дабигатрана этексилата // Фармакогенетика и фармакогеномика. Promising areas of research on the pharmacogenetics of dabigatran etexilate Savinova AV1, Shnayder NA1,2, Petrova MM2, Nasyrova RF1,3. 1 – Bekhterev National Medical Research Center of Psychiatry and Neurology, St.-Petersburg 2 – FSBEI НЕ Prof. Voino-Yasenetsky KrasSMU MOH Russia, Russia, Krasnoyarsk 3 – Kazan Federal University, Russia, Kazan
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