Dapagliflozin - CAS 461432-26-8
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Not Intended for Therapeutic Use. For research use only.
Dapagliflozin(BMS512148) is a selective, orally active inhibitor of the renal sodium-glucose co-transporter type 2 (SGLT2) is in development for the treatment of type 2 diabetes mellitus (T2DM).
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Dapagliflozin; trade name Farxiga in the US and Forxiga in the EU.
1.Sodium-glucose cotransporter-2 inhibitor combination therapy to optimize glycemic control and tolerability in patients with type 2 diabetes: focus on dapagliflozin-metformin.
Schwartz SS1, Katz A2. Diabetes Metab Syndr Obes. 2016 Mar 15;9:71-82. doi: 10.2147/DMSO.S65588. eCollection 2016.
In type 2 diabetes (T2D), early combination therapy using agents that target a number of the underlying pathophysiologic defects contributing to hyperglycemia may improve patient outcomes. For many patients, the combination of metformin with a sodium-glucose cotransporter-2 (SGLT-2) inhibitor may be a good option because these agents have complementary mechanisms of action, neutral-to-positive effects on body weight, and a low risk of hypoglycemia. This review focuses on the combination of metformin with dapagliflozin, a member of the SGLT-2 inhibitor class of antidiabetes agents. In clinical trials, the combination of dapagliflozin with metformin produced significant and sustained reductions in glycated hemoglobin and body weight in a broad range of adult patients with T2D, including those initiating pharmacotherapy and those with more advanced disease. These reductions were accompanied by modest decreases in blood pressure. Dapagliflozin as add-on therapy to metformin was well tolerated and associated with low rates of hypoglycemia.
2.Sodium-Glucose Cotransporter-2 Inhibitors and Genital and Urinary Tract Infections in Type 2 Diabetes.
Arakaki RF1. Postgrad Med. 2016 Mar 16. [Epub ahead of print]
Coincident with the high and increasing worldwide prevalence of type 2 diabetes (T2D), a growing armamentarium of antidiabetes medications has been introduced to target different organ systems that play a role in the pathophysiology of T2D. Among these, the sodium-glucose cotransporter-2 (SGLT-2) inhibitors were introduced in the United States in 2013 as a new treatment option to address the hyperglycemia associated with T2D. SGLT-2 inhibitors decrease renal glucose reabsorption, resulting in glucosuria, alleviation of hyperglycemia, and modest weight loss and are associated with a low risk of hypoglycemia. The SGLT-2 inhibitors have been linked to an increased incidence of genital mycotic infections and, to a lesser extent, urinary tract infections, which may limit their utility in some patients. This review examines the prevalence, recurrence rates, treatment options, and responses to treatment of genital and urinary tract infections in patients with T2D receiving SGLT-2 inhibitors, with the aim of guiding clinicians in the most effective use of these agents for the treatment of hyperglycemia.
3.Dapagliflozin in the Treatment of Patients With Type 2 Diabetes Presenting With High Baseline A1C.
Skolnik N1, Bonnes H1, Yeh H2, Katz A2. Postgrad Med. 2016 Apr 4. [Epub ahead of print]
OBJECTIVES: To evaluate the efficacy and safety of dapagliflozin 5 and 10 mg/d versus placebo in patients with type 2 diabetes and high baseline A1C defined as A1C ≥9% or ≥10%.
4.Long-term maintenance of efficacy of dapagliflozin in patients with type 2 diabetes mellitus and cardiovascular disease.
Leiter LA1, Cefalu WT2, de Bruin TW3, Xu J4, Parikh S5, Johnsson E6, Gause-Nilsson I6. Diabetes Obes Metab. 2016 Mar 24. doi: 10.1111/dom.12666. [Epub ahead of print]
AIM: To evaluate the long-term efficacy, safety and tolerability of dapagliflozin versus placebo added to usual care in patients with type 2 diabetes mellitus (T2DM) and cardiovascular disease (CVD).
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