Drug intelligence / Profile preview

sitagliptin + dapagliflozin + lobeglitazone

Development stage
Phase 4
Lead developer
Yonsei University
Modality
Small Molecules
Administration
Oral
01

Overview

Sitagliptin + dapagliflozin + lobeglitazone is a triple combination therapy investigated for the management of type 2 diabetes mellitus. This regimen combines three distinct classes of glucose-lowering agents: sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor; dapagliflozin, a sodium-glucose cotransporter 2 (SGLT2) inhibitor; and lobeglitazone, a thiazolidinedione (TZD). Sitagliptin works by preventing the degradation of incretin hormones, thereby enhancing glucose-dependent insulin secretion and suppressing glucagon release. Dapagliflozin promotes the renal excretion of glucose by inhibiting its reabsorption in the proximal tubule. Lobeglitazone acts as a peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonist, improving insulin sensitivity in muscle, fat, and liver tissues. This combination is typically evaluated in patients who have inadequate glycemic control on standard therapies, aiming to provide comprehensive metabolic control through complementary mechanisms.

Other names
sitagliptin/dapagliflozin/lobeglitazone combinationSGLT2i and TZD add-on to DPP4iSGLT-2i and TZD add-on to DPP4iSGLT 2i and TZD add-on to DPP4i
02

Targets

DPP-4 (Dipeptidyl Peptidase-IV)PPARG (Peroxisome proliferator-activated receptor gamma)SGLT2 (Sodium-glucose cotransporter protein subunit 2)

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