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Anna Sadurní, Gerald Kehr, Marie Ahlqvist, Johan Wernevik, Helena Peilot Sjögren, Cecilia Kankkonen, Laurent Knerr, Ryan Gilmour
Inhibition of the sodium-glucose co-transporters (SGLT1 and SGLT2) is a validated strategy to address the increasing prevalence of type II diabetes mellitus. However, achieving selective inhibition of human SGLT1 or SGLT2 remains challenging. Orally available small molecule drugs based on the d-glucose core of the natural product Gliflozin have proven to be clinically effective in this regard, effectively impeding glucose reabsorption. Herein, we disclose the influence of molecular editing with fluorine at the C2 position of the pyranose ring of Phlorizin analogues Remogliflozin Etabonate and Dapagliflozin (Farxiga® ) to concurrently direct β-selective glycosylation, as is required for biological efficacy, and enhance aspects of the physicochemical profile...
February 26, 2018: Chemistry: a European Journal
Rhona Johnston, Olalekan Uthman, Ewen Cummins, Christine Clar, Pamela Royle, Jill Colquitt, Bee Kang Tan, Andrew Clegg, Saran Shantikumar, Rachel Court, J Paul O'Hare, David McGrane, Tim Holt, Norman Waugh
BACKGROUND: Most people with type 2 diabetes are overweight, so initial treatment is aimed at reducing weight and increasing physical activity. Even modest weight loss can improve control of blood glucose. If drug treatment is necessary, the drug of first choice is metformin. However, some people cannot tolerate metformin, which causes diarrhoea in about 10%, and it cannot be used in people with renal impairment. This review appraises three of the newest class of drugs for monotherapy when metformin cannot be used, the sodium-glucose co-transporter 2 (SGLT2) inhibitors...
January 2017: Health Technology Assessment: HTA
Ann Shastay
No abstract text is available yet for this article.
October 2016: Home Healthcare Now
Clinton K Pong, George E Maxted
No abstract text is available yet for this article.
June 15, 2015: American Family Physician
Eva M Vivian
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...
March 1, 2015: American Journal of Health-system Pharmacy: AJHP
Qin C Ji, Xiaohui Xu, Eric Ma, Jane Liu, Shenita Basdeo, Guowen Liu, William Mylott, David W Boulton, Jim X Shen, Bruce Stouffer, Anne-Françoise Aubry, Mark E Arnold
Dapagliflozin (Farxiga), alone, or in the fixed dose combination with metformin (Xigduo), is an orally active, highly selective, reversible inhibitor of sodium-glucose cotransporter type 2 (SGLT2) that is marketed in United States, Europe, and many other countries for the treatment of type 2 diabetes mellitus. Here we report a liquid chromatography-tandem mass spectrometry (LC-MS/MS) bioanalytical assay of dapagliflozin in human plasma. A lower limit of quantitation (LLOQ) at 0.2 ng/mL with 50 μL of plasma was obtained, which reflects a 5-fold improvement of the overall assay sensitivity in comparison to the previous most sensitive assay using the same mass spectrometry instrumentation...
March 17, 2015: Analytical Chemistry
Portia N Davis, Uche Anadu Ndefo, Ashley Oliver
OBJECTIVE: To review clinical evidence for the efficacy, safety, and tolerability of dapagliflozin (Farxiga-AstraZeneca), a sodium glucose cotransporter 2 inhibitor, as monotherapy or in combination with other hypoglycemic agents for the treatment of type 2 diabetes. DATA SOURCES: Literature was identified through a systematic MEDLINE search of clinical trial results for dapagliflozin. DATA SYNTHESIS: Multiple controlled clinical trials have established the efficacy, safety, and tolerability of dapagliflozin as monotherapy or in combination with other therapies for type 2 diabetes...
April 2016: Journal of Pharmacy Practice
Marianna Maranghi, Anna Carnovale, Cosimo Durante, Giovanna Tarquini, Giusy Tiseo, Sebastiano Filetti
INTRODUCTION: Dapagliflozin (DAPA) (Farxiga or Forxiga) is a sodium glucose cotransporter 2 (SGLT2) inhibitor approved for type 2 diabetes mellitus(T2DM) treatment. AREAS COVERED: The review focuses on the pharmacokinetics (PK), pharmacodynamics(PD) and clinical studies published on DAPA. The authors searched PubMed database for English language studies describing DAPA characteristics and use in T2DM subjects published through June 2014. EXPERT OPINION: DAPA exhibits favorable PK and PD properties and is effective in reducing glycemic levels...
January 2015: Expert Opinion on Drug Metabolism & Toxicology
Greg L Plosker
Dapagliflozin (Forxiga(®), Farxiga(®)) is an orally administered sodium-glucose co-transporter-2 (SGLT2) inhibitor used in the management of patients with type 2 diabetes. Dapagliflozin reduces renal glucose reabsorption by inhibiting the transporter protein SGLT2 in the renal proximal tubule, thereby increasing urinary glucose excretion and reducing blood glucose levels. Its mechanism of action is independent of insulin secretion or action; therefore, dapagliflozin provides complementary therapy when used in combination with other antihyperglycaemic drugs...
December 2014: Drugs
Andrew Aylsworth, Zachary Dean, Cody VanNorman, Arinze Nkemdirim Okere
OBJECTIVE: To review the pharmacology, pharmacokinetics, clinical trials, and adverse effects of dapagliflozin, a sodium glucose co-transporter 2 (SGLT-2) inhibitor. DATA SOURCES: Data were gathered from articles indexed in PubMed, International Pharmaceutical from (2006 to April 2014) was performed using the following terms "dapagliflozin," "SGLT-2 inhibitor," and "Farxiga." Abstracts and manufacturer's package insert were also used as an additional reference. STUDY SELECTION AND DATA EXTRACTION: All English language prospective randomized, double-blinded trials evaluating the efficacy of dapagliflozin for the treatment of type 2 diabetes were identified...
September 2014: Annals of Pharmacotherapy
Marvin M Goldenberg
Dapaglifozin (Farxiga) for improved glycemic control in type-2 diabetes, and trametinib (Mekinist) in combination with dabrafenib (Tafinlar) for the treatment of advanced, unresectable melanoma.
March 2014: P & T: a Peer-reviewed Journal for Formulary Management
(no author information available yet)
No abstract text is available yet for this article.
February 17, 2014: Medical Letter on Drugs and Therapeutics
(no author information available yet)
No abstract text is available yet for this article.
February 17, 2014: Medical Letter on Drugs and Therapeutics
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