Eva M Vivian1. 1. Eva M. Vivian, Pharm.D., M.S., BC-ADM, CDE, is Associate Professor, School of Pharmacy, University of Wisconsin, Madison (emvivian@pharmacy.wisc.edu).
Abstract
PURPOSE: The pharmacologic properties and clinical efficacy of dapagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes, are reviewed. SUMMARY: Dapagliflozin (Farxiga, AstraZeneca) is a selective SGLT2 inhibitor approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. Dapagliflozin lowers blood glucose independent of insulin secretion and action by inhibiting renal reabsorption of glucose, thus promoting increased urinary excretion of glucose. Dapagliflozin has been shown to improve glycemic parameters in patients with type 2 diabetes when used as monotherapy or in combination with metformin, glimepiride, pioglitazone, sitagliptin, or insulin. Dapagliflozin treatment is associated with weight reduction, it has a low intrinsic propensity to cause hypoglycemia, and it may offer the advantage of a complementary mechanism of action when added to other therapies. During Phase III clinical trials, dapagliflozin was generally well tolerated, with an overall frequency of adverse events similar to that reported with placebo use. However, increased rates of genital and, in some trials, urinary tract infections have been reported in dapagliflozin-treated groups relative to placebo groups. Pooled data from clinical trials indicated an imbalance in bladder cancer cases between dapagliflozin-treated and placebo groups; however, most cases were diagnosed within one year of exposure. Ongoing research is expected to further delineate the effects of dapagliflozin on bladder cancer risk and cardiovascular safety measures. CONCLUSION: Dapagliflozin, an SGLT2 inhibitor, offers a novel treatment option for type 2 diabetes that is independent of insulin secretion or action.
PURPOSE: The pharmacologic properties and clinical efficacy of dapagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes, are reviewed. SUMMARY:Dapagliflozin (Farxiga, AstraZeneca) is a selective SGLT2 inhibitor approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes. Dapagliflozin lowers blood glucose independent of insulin secretion and action by inhibiting renal reabsorption of glucose, thus promoting increased urinary excretion of glucose. Dapagliflozin has been shown to improve glycemic parameters in patients with type 2 diabetes when used as monotherapy or in combination with metformin, glimepiride, pioglitazone, sitagliptin, or insulin. Dapagliflozin treatment is associated with weight reduction, it has a low intrinsic propensity to cause hypoglycemia, and it may offer the advantage of a complementary mechanism of action when added to other therapies. During Phase III clinical trials, dapagliflozin was generally well tolerated, with an overall frequency of adverse events similar to that reported with placebo use. However, increased rates of genital and, in some trials, urinary tract infections have been reported in dapagliflozin-treated groups relative to placebo groups. Pooled data from clinical trials indicated an imbalance in bladder cancer cases between dapagliflozin-treated and placebo groups; however, most cases were diagnosed within one year of exposure. Ongoing research is expected to further delineate the effects of dapagliflozin on bladder cancer risk and cardiovascular safety measures. CONCLUSION:Dapagliflozin, an SGLT2 inhibitor, offers a novel treatment option for type 2 diabetes that is independent of insulin secretion or action.