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

Sodium-Glucose Linked Transporter 2 (SGLT2) inhibitors such as Dapagliflozin (Farxiga), Canagliflozin (Invokana) and Empagliflozin (Jardiance) are a new class of oral drugs available to treat type 2 diabetes mellitus (Type 2 DM).

1. Dr. P.Naina Mohamed
Pharmacologist

2. 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.

3. 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 8
th
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 29
th

Mar 2013.
Empagliflozin got the FDA approval by 1
st
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.

4. Mechanism of Action

5. Effects on Weight

6. Effects on Blood Pressure

7. Adverse Effects

8. Contraindications

9. Possible Drug Interactions

10. References
http://diabetes.diabetesjournals.org/content/61/9/2199.full
http://www.medscape.com/viewarticle/760248
http://www.diabetesincontrol.com/articles/91-/14495-sglt2-inhibitors-a-new-class-of-diabetes-medications
http://spectrum.diabetesjournals.org/content/22/2/92.full.pdf
http://www.micromedexsolutions.com
http://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/ucm3808
29.htm
http://www.fda.gov/NewsEvents/Newsroom/PressAnnouncements/uc
m407637.htm?
source=govdelivery&utm_medium=email&utm_source=govdelivery