problendoПроблемы ЭндокринологииProblems of Endocrinology0375-96602308-1430Endocrinology Research Centre10.14341/probl201056552-60problendo-4753Research ArticleСтатьиArticlesРасширение группы препаратов, основанных на действии инкретинов: новый ингибитор ДПП-4 саксаглиптинExtension of the group of incretin-targeted preparations: Saxagliptin – a new dipeptidyl peptidase-4 inhibitorShestakovaM V-SukharevaO Iuolgasukhareva@mail.ru201015102010565ТОМ 56, №5 (2010)5260Copyright © Shestakova M.V., Sukhareva O.I., 20102010Shestakova M.V., Sukhareva O.I.Shestakova M.V., Sukhareva O.I.Данная работа распространяется под лицензией Creative Commons Attribution 4.0.This work is licensed under a Creative Commons Attribution 4.0 License.https://www.probl-endojournals.ru/jour/article/view/4753

В августе 2010 г. в Российской Федерации зарегистрирован новый препарат инкретинового ряда саксаглиптин - селективный ингибитор фермента дипептидилпептидазы-4, инактивирующего глюкагоноподобный пептид-1 (ГПП-1). В результате действия препарата увеличивается концентрация ГПП-1 в плазме, что сопровождается глюкозозависимым увеличением секреции инсулина β-клетками поджелудочной железы и подавлением секреции глюкагона. При пероральном применении препарат быстро всасывается и сохраняет активность в течение 24 ч, что позволяет назначать его однократно в сутки. Результаты клинических исследований показали, что саксаглиптин улучшает гликемический контроль и в качестве монотерапии, и в комбинации с другими сахароснижающими препаратами (метформин, препараты сульфонилмочевины, тиазолидиндионы). Применение саксаглиптина сопровождается снижением уровня глюкозы в плазме крови натощак и после приема пищи, что приводит к клинически значимому снижению уровня гликированного гемоглобина (HbA1c). Низкий риск возникновения гипогликемии при применении саксаглиптина обусловлен глюкозозависимым механизмом его действия. Результаты клинических исследований показали, что саксаглиптин нейтрален в отношении увеличения массы тела и обладает хорошими переносимостью и безопасностью.

A new selective incretin-targeted dipeptidyl peptidase-4 inhibitor was registered in the Russian Federation in August 2010. The enzyme dipeptidyl peptidase-4 inactivates glucagon-like peptide-1 (GLP-1). A rise of GLP-1 concentration in blood plasma is known to result in the glucose-dependent stimulation of insulin secretion by pancreatic beta-cells and suppression of glucagon release. Saxagliptin is readily absorbed in the gastrointestinal tract and remains active within 24 hours after oral intake. It allows the drug to be taken once during 24 hours. Clinical studies have demonstrated that saxagliptin improves glycemic control when used as both monotherapy and in combination with other antidiabetic medicines (metformin, sulfonylureas, and thiazolidinediones). The use of saxagliptin leads to a reduction of fasting and postprandial plasma glucose level and thereby to the clinically significant decrease in glycated hemoglobin (HbA1c) concentration. The low risk of hypoglycemia following saxagliptin intake is due to the glucose-dependent mechanism of its action. The results of clinical investigations indicate that saxagliptin is safe and well tolerated by the patients and has no significant influence on their body weight; its dose does not need to be corrected for the sex and age of the patients or the presence of concomitant hepatic disorders.

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The authors declare that there are no conflicts of interest present.