SGLT2 inhibitors for the treatment of diabetes: a patent review (2013-2018)

ABSTRACT

Introduction: The sodium-glucose co-transporter 2 (SGLT2) is ascribed to target renal tubular glucose re-absorption, and its inhibition has been proved to induce glucosuria which improves the glycemic index. Accordingly, SGLT2 inhibitors have found to be the promising class of antidiabetic agents for the management of type 2 diabetes mellitus. A large number of SGLT2 inhibitors have developed through structural modification and investigated for their ability to selectivity inhibit SGLT2 transporters with better bioavailability.

Areas covered: This review comprises a summary of patent applications (2013–2018) of SGLT2 inhibitors with focus on chemical structural advancement and therapeutic potentials in the management of diabetes and related disorders.

Expert opinion: SGLT2 inhibitors exert multiple metabolic benefits, including reduced glycated hemoglobin (HbA1c), improved glycemic control (fasting and postprandial), reduced body weight, reduced systolic and diastolic blood pressure and improved HDL cholesterol. Due to the virtue of no interference with insulin action and secretion, their efficacy remains the same even in presence of progressive β cell failure in type 2 diabetes. Additionally, few members of this class have been reported to exhibit cardioprotective, renoprotective, and anticancer activity. However, more study on the long-term outcomes in patients taking SGLT2 inhibitors is warranted.

KEYWORDS:

• SGLT transporters
• SGLT2 inhibitors
• type 2 diabetes mellitus
• antidiabetic agent

Article highlights

• SGLT2 inhibitors exert their antihyperglycemic effects by reducing renal tubular glucose reabsorption, thereby decreasing the blood glucose level without insulin action.

• SGLT2 inhibitors have demonstrated additional metabolic benefits of weight loss and blood pressure lowering.

• SGLT2 inhibitors have reported to exhibit cardioprotective, renoprotective, and anticancer activity.

• Patents concerning SGLT2 inhibitors are reviewed, which have potential applications for treatment of diabetes.

• Reported SGLT2 inhibitors were developed with the aim to increase efficacy and selectivity to SGLT2 for the better management of diabetes and associated disorders.

This box summarizes key points contained in the article.

Declaration of interest

J Pandey received a fellowship from CSIR, New Delhi and AK Tamrakar was supported by a grant from CSIR, New Delhi. The authors have no other relevant affiliations or financial involvement with any organization or entity with a financial interest in or financial conflict with the subject matter or materials discussed in the manuscript apart from those disclosed.

Reviewer disclosures

Peer reviewers on this manuscript have no relevant financial or other relationships to disclose.

Additional information

Funding

This paper was not funded.