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Ann M Carracher, Payal H Marathe, Kelly L Close
Ann M. Carracher, Payal H. Marathe, and Kelly L. Close are of Close Concerns (, a healthcare information company focused exclusively on diabetes and obesity care. Close Concerns publishes Closer Look, a periodical that brings together news and insights in these areas. Each month, the Journal of Diabetes includes this News feature, in which Carracher, Marathe, and Close review the latest developments relevant to researchers and clinicians.
April 2018: Journal of Diabetes
Aml A Emam
Canagliflozin is a newly approved drug for type II diabetes mellitus. A full stability study of canagliflozin was performed following international conference on harmonization strategies. The drug was stable against all conditions except oxidation where only one degradation product was separated and structurally elucidated using mass spectrometry and infrared spectroscopy. A green high-performance thin-layer chromatographic densitometric determination was developed and validated for the accurate quantification of canagliflozin and its main oxidative degradation product...
February 2018: Journal of Separation Science
Emma D Deeks, André J Scheen
Canagliflozin (Invokana®) is a sodium-glucose co-transporter-2 (SGLT2) inhibitor indicated in various countries worldwide for the once-daily oral treatment of type 2 diabetes (T2D). Canagliflozin lowers blood glucose levels independently of insulin, with the inhibition of SGLT2 reducing renal reabsorption of glucose and increasing excretion of glucose in the urine. In well-designed clinical trials, canagliflozin (as first-line monotherapy or add-on therapy to other antihyperglycaemic agents) improved glycaemic control in adults with T2D, including those of older age and/or at high cardiovascular (CV) risk, and also had beneficial effects on their bodyweight and blood pressure (BP)...
September 2017: Drugs
Ronghui Lin, David C Hoerr, Larry E Weaner, Rhys Salter
Canagliflozin (Invokana, JNJ-28431754) is an orally bioavailable and selective SGLT2 (subtype 2 sodium-glucose transport protein) inhibitor approved for the treatment of type 2 diabetes. Herein, we report the synthesis of (13) C and (14) C-labeled canagliflozin. Stable isotope-labeled [(13) C6 ]canagliflozin was synthesized in 4 steps starting from [(13) C6 ]-labeled glucose. The [(14) C]-Labeled canagliflozin was synthesized by incorporation of [(14) C] into the benzylic position between the thiophene and benzene rings of the compound...
August 18, 2017: Journal of Labelled Compounds & Radiopharmaceuticals
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
Alehegn Gelaye, Abdallah Haidar, Christina Kassab, Syed Kazmi, Prabhat Sinha
Canagliflozin (Invokana) is a selective sodium glucose cotransporter-2 (SGLT-2) inhibitor that was first introduced in 2013 for the treatment of type 2 diabetes mellitus (DM). Though not FDA approved yet, its use in type 1 DM has been justified by the fact that its mechanism of action is independent of insulin secretion or action. However, some serious side effects, including severe anion gap metabolic acidosis and euglycemic diabetic ketoacidosis (DKA), have been reported. Prompt identification of the causal association and initiation of appropriate therapy should be instituted for this life threatening condition...
2016: Case Reports in Critical Care
Danielle Fortuna, Laura J McCloskey, Douglas F Stickle
BACKGROUND: Renal reabsorption of 1,5-anhydroglucitol (AG) is competitively inhibited by elevated glucose and leads to depleted plasma AG in diabetes. Plasma AG recovery in diabetes normally correlates with improved glycemic control. However, use of sodium-glucose co-transporter 2 (SGLT2) inhibitors (e.g., canagliflozin) to treat diabetes by inhibition of renal glucose reabsorption can negate this correlation, via an indirect effect (increase of renal filtrate glucose concentration) to inhibit AG reabsorption by sodium-glucose co-transporter 4 (SGLT4)...
January 15, 2016: Clinica Chimica Acta; International Journal of Clinical Chemistry
Narat Srivali, Charat Thongprayoon, Wisit Cheungpasitporn, Patompong Ungprasert
Canagliflozin (Invokana) is an innovative treatment for type 2 diabetes mellitus (DM) approved in a new class acknowledged as sodium-glucose co-transporter 2 inhibitors. Acute pancreatitis is a very rare side effect with an incidence <1%. a 50-year-old white male with DM type 2 presented to the emergency department with acute onset of abdominal pain after 4 days treatment with canagliflozin. He was successfully diagnosed with diabetic ketoacidosis induced by acute pancreatitis. Canagliflozin was discontinued...
June 2015: Journal of Basic and Clinical Pharmacy
(no author information available yet)
Currently, metformin is the only oral hypoglycaemic drug with reasonably well-established efficacy in preventing the complications of type 2 diabetes. Canagliflozin is the second renal sodium-glucose cotransporter 2 (SGLT2) inhibitor to be authorised in the European Union, after dapagliflozin. Initial evaluation of canagliflozin included no controlled clinical trials designed to determine its efficacy in preventing the clinical complications of diabetes. The eight available placebo-controlled trials show a moderate hypoglycaemic effect (mean HbA1c decline: -0...
February 2015: Prescrire International
A J Scheen
Canagliflozin is an inhibitor of sodium-glucose cotransporters type 2 (SGLT2) that are present in renal tubules. This specific insulin-independent mechanism promotes glucosuria, which results in a reduction in fasting and postprandial glycaemia and a decrease of glycated haemoglobin (HbA(1c)). Furthermore, canagliflozin promotes weight loss and lowers arterial (mainly systolic) blood pressure. Its efficacy is decreased in patients with renal insufficiency and the treatment should be stopped if estimated glomerular filtration rate is below 45 ml/min/1...
December 2014: Revue Médicale de Liège
Manoj Khurana, Jayabharathi Vaidyanathan, Anshu Marathe, Nitin Mehrotra, Chandrahas G Sahajwalla, Issam Zineh, Lokesh Jain
Canagliflozin (INVOKANA™) is approved as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus (T2DM). Canagliflozin inhibits renal sodium-glucose co-transporter 2 (SGLT2), thereby, reducing reabsorption of filtered glucose and increasing urinary glucose excretion. Given the mechanism of action of SGLT2 inhibitors, we assessed the interplay between renal function, efficacy (HbA1c reduction), and safety (renal adverse reactions). The focus of this article is to highlight the FDA's quantitative clinical pharmacology analyses that were conducted to support the regulatory decision on dosing in patients with renal impairment (RI)...
June 2015: Journal of Clinical Pharmacology
Marek Rosiak, Susanna Grzeszczak, Dariusz A Kosior, Marek Postuła
Type 2 diabetes mellitus (T2DM) is a prevalent metabolic disorder, which affects more than 300 million people globally. The common effect of uncontrolled diabetes is the state of hyperglycemia, which results from beta-cell dysfunction as well as insulin resistance, which is accompanied with microvascular and macrovascular complications. As hyperglycemia defines diabetes, glycemic control is fundamental to the management of diabetes. Sodium glucose co-transporter 2 inhibitors (SGLT2) are a new group of oral antidiabetic medications that act by blocking the reabsorption of glucose, causing it to be excreted in the urine...
2014: Therapeutics and Clinical Risk Management
Greg L Plosker
Canagliflozin (Invokana™) is an orally administered sodium-glucose co-transporter-2 (SGLT2) inhibitor used in the treatment of patients with type 2 diabetes. By inhibiting the transporter protein SGLT2 in the kidneys, canagliflozin reduces renal glucose reabsorption, thereby increasing urinary glucose excretion and reducing blood glucose levels. Several randomized placebo- or active comparator-controlled trials of 26-52 weeks' duration (plus extension phases) have shown that canagliflozin improves glycaemic control when used as monotherapy or as add-on therapy to metformin and/or other antihyperglycaemic agents, including insulin, in patients with type 2 diabetes...
May 2014: Drugs
Sheila Sarnoski-Brocavich, Olga Hilas
No abstract text is available yet for this article.
November 2013: P & T: a Peer-reviewed Journal for Formulary Management
Marvin M Goldenberg
Canagliflozin (Invokana) for type-2 diabetes; denosumab (Xgeva) for giant-cell tumor of bone; and paroxetine mesylate (Brisdelle) for vasomotor symptoms in menopause.
August 2013: P & T: a Peer-reviewed Journal for Formulary Management
Nida Akhtar
Diabetes Mellitus is a chronic metabolic disease affecting wide range of people across the globe. In India the rate of subjects being suffered from diabetes is continuously increasing. So, the development of drugs for its effective treatment is essential. Thereby, various attempts have been made to discover newer drugs, to reduce the rate of anti diabetic occurrence. Anti-diabetic drugs were found to treat diabetes mellitus by lowering glucose levels in the blood. Both the use antidiabetic drugs as well as the changes in lifestyle and proper diet can significantly affect the severity of diabetes mellitus and also reduces the symptoms and occurrence of the disease...
November 2013: Current Diabetes Reviews
Syed M D Rizvi, Shahnawaz Shakil, Deboshree Biswas, Shazi Shakil, Sibhghatulla Shaikh, Paramdeep Bagga, Mohammad A Kamal
Acetylcholinesterase (AChE) is a primary target for Alzheimer's therapy while recently sodium glucose cotransporter 2 (SGLT2) has gained importance as a potential target for Type 2 Diabetes Mellitus (T2DM) therapy. The present study emphasizes the molecular interactions between a new Food and Drug Administration (FDA) approved antidiabetic drug 'Invokana' (chemically known as Canagliflozin) with AChE and SGLT2 to establish a link between the treatment of T2DM and Alzheimer's Disease (AD). Docking study was performed using 'Autodock4...
April 2014: CNS & Neurological Disorders Drug Targets
Shelley Elkinson, Lesley J Scott
Canagliflozin (Invokana™), an oral selective sodium-glucose co-transporter 2 (SGLT2) inhibitor, is under global development with Mitsubishi Tanabe Pharma and Janssen Pharmaceuticals, a subsidiary of Johnson and Johnson, for the treatment of type 2 diabetes mellitus. SGLT2 are mainly located in the proximal tubule of the kidney and are involved in the reabsorption of filtered glucose from the glomeruli into the body. Inhibition of SGLT2 lowers blood glucose in an insulin independent manner as a consequence of blocking reabsorption of filtered glucose in the glomeruli, thereby increasing urinary excretion of glucose and, in turn, potentially reducing bodyweight...
June 2013: Drugs
(no author information available yet)
No abstract text is available yet for this article.
May 13, 2013: Medical Letter on Drugs and Therapeutics
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