SGLT inhibitors: a novel target for diabetes Abhinav Kanwal & Sanjay K Banerjee* Division of Pharmacology, Indian Institute of Chemical Technology, Hyderabad-500607, India *Author for correspondence: Tel.: +91 402 719 1618 Fax: +91 402 719 3189 E-mail: skbanerjee@iict.res.in, banerjees74@ hotmail.com Inhibiting sodium–glucose co-transporters (SGLT1/SGLT2), which have a key role in the absorption of glucose in the kidney and/or GI tract has been proposed as a novel therapeutic strategy for diabetes. Thus, screening and patenting of chemical compounds for SGLT1/SGLT2 gets more importance in the development of new drugs in diabetes. Several companies are developing SGLT inhibitors, some of which are now in various stages of clinical development. Some molecules in the pipeline, including dapaglilozin, canaglilozin, ASP1941, BI10773, LX4211, RG7201 and TS071, are at various stages of drug development. This patent review presents the overall progress carried out in the development of SGLT inhibitors over the last decade with the active participation of various pharmaceutical companies. This class of drug is anticipated to have a large impact on diabetes ield and predicting to attain a blockbuster status. According to the International Diabetes Foundation, 366 million people worldwide are diabetic and this is expected to rise to 552 million by 2030 [1] . As diabetes is of major concern in both the developed and developing world, increasing research is being undertaken in different sectors including research institutions, universities and private companies. Several drugs that affect different targets are approved for the treatment of diabetes. However, the use of current antidiabetic agents, such as metformin, sulphonylureas, thiazolidinedione and incretinmimetics, are often limited by their potential to induce significant adverse effects. Glycaemic control is difficult to attain at the late stage of diabetes, even with a combination of multiple oral agents. Thus, the quest for developing therapeutic agents with novel mecha- nisms of action without any side effects continues. One of the major and upcoming targets of this decade is sodium–glucose co-transporters (SGLTs). Inhibiting SGLTs, which have a key role by reabsorption of glucose in the kidney and absorption of glucose in the GI tract, has been proposed as a novel therapeutic strategy for diabetes [2,3] . Data suggest that the beneficial effects of SGLT2 inhibi- tion might be achieved without exerting significant side effects – an advantage over many current diabetes medications [4] . Thus, the focus of this patent review is to discuss the role of SGLTs in glucose homeostasis and the evidence available so far in regards to the potential SGLTs in- hibitors and their associated patents. Several organizations have already developed and continue developing selective and non-selective SGLT inhibitors since past one decade. This review will also reflect the progress of SGLTs inhibitors that are in the preclinical and clinical phases of drug development. Mechanism of action The kidney plays a key role in regulating glucose levels by mediating reabsorp- tion of glucose back into the blood. The glomeruli of a normal healthy adult fil- ter approximately 180 g of glucose every day. Under normal pathophysiological ISSN 2046-8954 77 Pharm. Pat. Analyst (2013) 2(1), 77–91 10.4155/PPA.12.78 © 2013 Future Science Ltd Patent Review