metformin + sitagliptin + lobeglitazone

This therapeutic regimen is an initial triple combination therapy evaluated by Seoul National University Bundang Hospital for the treatment of drug-naïve patients with type 2 diabetes mellitus. The regimen consists of three small molecule agents: metformin (a biguanide), sitagliptin (a dipeptidyl peptidase-4 inhibitor), and lobeglitazone (a thiazolidinedione and PPARγ agonist). Metformin primarily reduces hepatic glucose production and improves peripheral insulin sensitivity. Sitagliptin prevents the degradation of incretin hormones like GLP-1, thereby enhancing glucose-dependent insulin secretion. Lobeglitazone acts as an insulin sensitizer by activating peroxisome proliferator-activated receptor gamma (PPARγ). A Phase 4 clinical trial (NCT02188186) demonstrated that this initial triple therapy approach provides superior glycemic control compared to conventional stepwise dual therapy in Korean patients with high baseline HbA1c levels (9.0%-12.0%), while maintaining a low risk of hypoglycemia.

Other names

Initial triple combinationInitial triple combination-Seoul National University Bundang Hospital-type 2 diabetes mellitusMetformin/Sitagliptin/Lobeglitazone triple therapy