Canagliflozin, a new sodium–glucose cotransporter 2 inhibitor, in the treatment of diabetes
Open Access
- 15 February 2013
- journal article
- research article
- Published by Oxford University Press (OUP) in American Journal of Health-System Pharmacy
- Vol. 70 (4), 311-319
- https://doi.org/10.2146/ajhp110514
Abstract
Purpose The published evidence on the pharmacology, pharmacodynamics, pharmacokinetics, safety, and efficacy of a promising investigational agent for managing type 2 diabetes is evaluated. Summary Canagliflozin belongs to a class of agents—the sodium–glucose co-transporter 2 (SGLT2) inhibitors—whose novel mechanism of action offers potential advantages over other antihyperglycemic agents, including a relatively low hypoglycemia risk and weight loss-promoting effects. Canagliflozin has dose-dependent pharmacokinetics, and research in laboratory animals demonstrated high oral bioavailability (85%) and rapid effects in lowering glycosylated hemoglobin (HbA1c) values. In four early-stage clinical trials involving a total of over 500 patients, the use of canagliflozin for varying periods was associated with significant mean reductions in HbA1c (absolute reductions of 0.45–0.92%) and fasting plasma glucose (decreases ranged from 16.2% to 42.4%) and weight loss ranging from 0.7 to 3.5 kg. More than a dozen Phase II or III clinical trials of canagliflozin in adults are ongoing or were recently completed, but the final results of most of those studies have not been published. Adverse effects reported in clinical trials of canagliflozin include urinary tract and genital infections, occurring in about 10% of patients. Additional and larger Phase III clinical trials to delineate the potential role of canagliflozin and other SGLT2 inhibitors in the management of diabetes (including studies involving the elderly, children, and patients with renal or hepatic dysfunction) are planned or currently underway. Conclusion Canagliflozin and other investigational SGLT2 inhibitors have a novel mechanism of action that may offer a future alternative treatment pathway for managing type 2 diabetes. Am J Health-Syst Pharm. 2013; 70:311–9Keywords
This publication has 19 references indexed in Scilit:
- Oral Pharmacologic Treatment of Type 2 Diabetes Mellitus: A Clinical Practice Guideline From the American College of PhysiciansAnnals of Internal Medicine, 2012
- Canagliflozin improves glycaemic control over 28 days in subjects with type 2 diabetes not optimally controlled on insulinDiabetes, Obesity and Metabolism, 2012
- Diagnosis and Classification of Diabetes MellitusDiabetes Care, 2011
- Empagliflozin, a novel selective sodium glucose cotransporter‐2 (SGLT‐2) inhibitor: characterisation and comparison with other SGLT‐2 inhibitorsDiabetes, Obesity and Metabolism, 2011
- Sodium-Glucose Co-Transport InhibitorsDrugs, 2010
- Statement by an American Association of Clinical Endocrinologists/ American College of Endocrinology Consensus Panel on Type 2 Diabetes Mellitus: An Algorithm for Glycemic ControlEndocrine Practice, 2009
- Medical Management of Hyperglycemia in Type 2 Diabetes: A Consensus Algorithm for the Initiation and Adjustment of TherapyDiabetes Care, 2009
- Sodium–glucose co‐transporter‐2 inhibitors: an emerging new class of oral antidiabetic drugDiabetes, Obesity and Metabolism, 2008
- Phlorizin: a reviewDiabetes/Metabolism Research and Reviews, 2004
- Combining sulfonylureas and other oral agentsThe American Journal of Medicine, 2000