Drug intelligence / Profile preview

ertugliflozin + sitagliptin

Development stage
Approved
Lead developer
Merck
Modality
Small Molecules
Administration
Oral
01

Overview

Steglujan is a fixed-dose combination of ertugliflozin and sitagliptin, indicated for the treatment of type 2 diabetes mellitus. Ertugliflozin is an inhibitor of the sodium-glucose cotransporter 2 (SGLT2), the primary transporter responsible for reabsorbing glucose from the glomerular filtrate back into the circulation. By inhibiting SGLT2, ertugliflozin reduces renal reabsorption of filtered glucose and lowers the renal threshold for glucose, thereby increasing urinary glucose excretion. Sitagliptin is a dipeptidyl peptidase-4 (DPP-4) inhibitor, which exerts its action by slowing the inactivation of incretin hormones, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP). These hormones are released by the intestine throughout the day, and levels increase in response to a meal. By increasing and prolonging active incretin levels, sitagliptin increases insulin release and decreases glucagon levels in the circulation in a glucose-dependent manner. The combination was co-developed by Merck and Pfizer.

Brand names
Steglujan
Other names
ertugliflozin/sitagliptinsitagliptin/ertugliflozin
02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)SLC22A8 (Organic anion transporter 3)OCT2 (Organic cation transporter 2)SGLT2 (Sodium-glucose cotransporter protein subunit 2)GSEC (Gamma-Secretase Complex)

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