The novel sodium glucose transporter 2 inhibitor dapagliflozin sustains pancreatic function and preserves islet morphology in obese, diabetic rats

Abstract

Sustained glucose lowering with dapagliflozin in this model of type 2 diabetes prevented the continued decline in functional adaptation of pancreatic β-cells.

SHR3824, a novel selective inhibitor of renal sodium glucose cotransporter 2, exhibits antidiabetic efficacy in rodent models

“…Chronic treatment with SHR3824 increased insulin staining in the islet cells of db/db mice, suggesting that β-cell function was improved. This result is similar to several other SGLT2 inhibitor studies reported previously [14,22] , and might be due to the correction of chronic hyperglycemia by enhancing urinary glucose excretion. Thus, SGLT2 inhibitors may contribute to the protection of β-cell function by suppressing glucose toxicity.…”

“…Chronic phlorizin administration restored insulin secretion and normalized β-cell volume and gene expression [18][19][20] . Long-term studies of canagliflozin and dapagliflozin treatment yielded similar results [21,22] . These data indicate that long-term treatment with SGLT2 inhibitors in animal models of T2DM can protect β-cell function.…”

Bioequivalence of Canagliflozin/Metformin Immediate Release Fixed- Dose Combination Tablets Compared with Concomitant Administration of Single Components of Canagliflozin and Metformin in Healthy Fed Participants

“…Canagliflozin (Invokana ® ; Janssen Pharmaceuticals, Inc.) belongs to a novel class of orally active inhibitors of renal sodium glucose cotransporter 2 (SGLT2) that decrease extent of glucose reabsorption from the proximal tubules of the kidney, thereby increasing urinary glucose excretion (UGE) and decreasing plasma glucose levels in patients with hyperglycemia [10][11][12][13][14][15][16][17][18][19][20]. Canagliflozin is approved as an adjunct to diet and exercise to improve glycemic control in adults with T2DM in numerous countries worldwide.…”

Досвід Використання Дапагліфлозину У Хворих На Цукровий Діабет 2-Го Типу

“…Вследствие осмотического диурети-ческого эффекта развивается и прогрессирует по-лиурия, что способствует гипотензивному эффекту. Кроме того, за счет потери избытка глюкозы идет потеря калорий с дозозависимым снижением мас-сы тела пациента [8,12].…”

“…В результате 12-24-недельного применения дапаглифлозина в Рисунок 1. Механизм действия дапаглифлозина виде монотерапии или в качестве комбинирован-ной сахароснижающей терапии (с инсулином или без него) отмечалось снижение уровня НbAlc у больных СД 2-го типа на 0,54-0,89 %, а снижение массы тела -на 2-3 кг по сравнению с плацебо [8,12]. Также наблюдалось снижение артериаль-ного давления (АД) (систолического -на 2-5 мм рт.ст., диастолического -на 1,5-3,0 мм рт.ст.…”