Dapagliflozin(BMS-512148) is a potent sodium-glucose transport proteins inhibitor with IC50 of 1.1 nM and 1.4 μM for SGLT2 and SGLT1, respectively. Dapagliflozin (BMS-512148) inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. Symptoms of hypoglycaemia occurred in similar proportions of patients in the dapagliflozin (2~4%) and placebo groups (3%). Signs, symptoms, and other reports suggestive of genital infections were more frequent in the dapagliflozin groups (2•5 mg, [8%]; 5 mg, [13%]; 10 mg, [9%]) than in the placebo group ( [5%]). [1][2]
参考文献
Effect of dapagliflozin in patients with type 2 diabetes who have inadequate glycaemic control with metformin:a randomised, double-blind, placebo-controlled trial Cliff ord J Bailey, Jorge L Gross, et al. Lancet 2010;375: 2223–2233
In Vitro Characterization and Pharmacokinetics of Dapagliflozin (BMS-512148), a Potent Sodium-Glucose Cotransporter Type II Inhibitor, in Animals and Humans M. Obermeier, M. Yao,et al. DMD 2010;38:405–414
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