SGLT2 Inhibitors (Gliflozins): A New Class of Drugs to treat Type 2 Diabetes:

Dr. P.Naina MohamedPharmacologist

Introduction Sodium-Glucose Linked Transporter 2 (SGLT2) inhibitors are a new class of oral

drugs to treat type 2 diabetes mellitus (Type 2 DM). Sodium-Glucose Linked Transporters (SGLT) or Sodium-dependent glucose

cotransporters are a family of glucose transporter. There are two kinds of SGLTs: SGLT1 and SGLT2. SGLT1 is found in intestinal mucosa of the small intestine and proximal straight

tubule (PST) of nephron. SGLT2 is found in proximal convoluted tubule (PCT) of nephron. Both SGLT1 and SGLT2 are responsible for the renal glucose reabsorption. Approximately 90% of glucose is reabsorbed by SGLT2 at PCT and only around 10%

of glucose is reabsorbed by SGLT1 at PST.

SGLT2 Inhibitors SGLT2 Inhibitors include:

Dapagliflozin (Farxiga) Canagliflozin (Invokana) Empagliflozin (Jardiance) Ipragliflozin Tofogliflozin Remogliflozin etabonate Sergliflozin etabonate

Dapagliflozin is the first drug to be developed in this class. But, its approval was rejected in 2012 by Food and Drug Administration (FDA) due to safety concerns. Later it was approved by FDA on 8th Jan 2014. Previously it was approved by EU in 2011.

Canagliflozin is the first drug to be approved by FDA which got the approval by 29th Mar 2013.

Empagliflozin got the FDA approval by 1st Aug 2014. Ipragliflozin (ASP-1941), is in Phase III clinical trials.

Tofogliflozin, is also in Phase III clinical trials.

Remogliflozin etabonate, is in phase IIb trials. Sergliflozin etabonate, discontinued after Phase II trials. SGLT2 inhibitors can improve glycemic control in conjunction with

exercise and a healthy diet. They can be used either alone or in combination with other antidiabetics

such as metformin, sulfonylureas, pioglitazone and insulin.

Mechanism of Action

Effects on Weight

Effects on Blood Pressure

Adverse Effects

Contraindications

Possible Drug Interactions

Referenceshttp://diabetes.diabetesjournals.org/content/61/9/2199.fullhttp://www.medscape.com/viewarticle/760248http://www.diabetesincontrol.com/articles/91-/14495-sglt2-i

nhibitors-a-new-class-of-diabetes-medicationshttp

://spectrum.diabetesjournals.org/content/22/2/92.full.pdfhttp://www.micromedexsolutions.comhttp://

www.diabetes.co.uk/diabetes-medication/sglt2-inhibitors.html

http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm345848.htm

http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/ucm380829.htm

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