PMID- 23563279 OWN - NLM STAT- MEDLINE DCOM- 20131212 LR - 20181202 IS - 1879-016X (Electronic) IS - 0163-7258 (Linking) VI - 139 IP - 1 DP - 2013 Jul TI - Ipragliflozin and other sodium-glucose cotransporter-2 (SGLT2) inhibitors in the treatment of type 2 diabetes: preclinical and clinical data. PG - 51-9 LID - S0163-7258(13)00082-X [pii] LID - 10.1016/j.pharmthera.2013.04.003 [doi] AB - Sodium-glucose cotransporter-2 (SGLT2) is expressed in the proximal tubules of the kidneys and plays a key role in renal glucose reabsorption. A novel class of antidiabetic medications, SGLT2-selective inhibitors attempt to improve glycemic control in diabetics by preventing glucose from being reabsorbed through SGLT2 and re-entering circulation. Ipragliflozin is an SGLT2 inhibitor in Phase 3 clinical development for the treatment of type 2 diabetes mellitus (T2DM). In this review, we summarize recent animal and human studies on ipragliflozin and other SGLT2 inhibitors including dapagliflozin, canagliflozin, empagliflozin, tofogliflozin, and luseogliflozin. These agents all show potent and selective SGLT2 inhibition in vitro and reduce blood glucose levels and HbA1c in both diabetic animal models and patients with T2DM. SGLT2 inhibitors offer several advantages over other classes of hypoglycemic agents. Due to their insulin-independent mode of action, SGLT2 inhibitors provide steady glucose control without major risk for hypoglycemia and may also reverse beta-cell dysfunction and insulin resistance. Other favorable effects of SGLT2 inhibitors include a reduction in both body weight and blood pressure. SGLT2 inhibitors are safe and well tolerated and can easily be combined with other classes of antidiabetic medications to achieve tighter glycemic control. The long-term safety and efficacy of these agents are under evaluation. CI - Copyright (c) 2013 Elsevier Inc. All rights reserved. FAU - Kurosaki, Eiji AU - Kurosaki E AD - Astellas Pharma, Inc., Ibaraki, Japan. eiji.kurosaki@astellas.com FAU - Ogasawara, Hideaki AU - Ogasawara H LA - eng PT - Journal Article PT - Review DEP - 20130404 PL - England TA - Pharmacol Ther JT - Pharmacology & therapeutics JID - 7905840 RN - 0 (Glucosides) RN - 0 (Hypoglycemic Agents) RN - 0 (Sodium-Glucose Transporter 2 Inhibitors) RN - 0 (Thiophenes) RN - 3N2N8OOR7X (ipragliflozin) RN - IY9XDZ35W2 (Glucose) SB - IM MH - Animals MH - Diabetes Mellitus, Type 2/*drug therapy/metabolism/physiopathology MH - Glucose/metabolism MH - Glucosides/pharmacology/*therapeutic use MH - Humans MH - Hypoglycemic Agents/pharmacology/*therapeutic use MH - Kidney/metabolism MH - *Sodium-Glucose Transporter 2 Inhibitors MH - Thiophenes/pharmacology/*therapeutic use EDAT- 2013/04/09 06:00 MHDA- 2013/12/18 06:00 CRDT- 2013/04/09 06:00 PHST- 2013/02/28 00:00 [received] PHST- 2013/03/01 00:00 [accepted] PHST- 2013/04/09 06:00 [entrez] PHST- 2013/04/09 06:00 [pubmed] PHST- 2013/12/18 06:00 [medline] AID - S0163-7258(13)00082-X [pii] AID - 10.1016/j.pharmthera.2013.04.003 [doi] PST - ppublish SO - Pharmacol Ther. 2013 Jul;139(1):51-9. doi: 10.1016/j.pharmthera.2013.04.003. Epub 2013 Apr 4.