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sitagliptin + metformin hydrochloride
- Development stage
- Unknown
- Lead developer
- Merck
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
Sitagliptin + metformin hydrochloride is a fixed-dose combination (FDC) oral therapy for the management of type 2 diabetes mellitus. It combines two antihyperglycemic agents with complementary mechanisms of action: sitagliptin, a dipeptidyl peptidase-4 (DPP-4) inhibitor, and metformin hydrochloride, a biguanide. Sitagliptin works by slowing the inactivation of incretin hormones, such as glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic polypeptide (GIP), which increases insulin release and decreases glucagon levels in a glucose-dependent manner. Metformin hydrochloride primarily reduces hepatic glucose production, decreases intestinal absorption of glucose, and improves insulin sensitivity by increasing peripheral glucose uptake and utilization. The combination is available in both immediate-release (Janumet) and extended-release (Janumet XR) formulations and is widely used to improve glycemic control when treatment with metformin or sitagliptin alone is insufficient.
- Brand names
- JanumetJanumet XR
- Other names
- sitagliptin/metformin hydrochloridesitagliptin phosphate / metformin hydrochloride
02
Targets
DPP-4 (Dipeptidyl Peptidase-IV)AMPK (Adenosine monophosphate–activated protein kinase)ND1 (Mitochondrial electron transport chain complex I)
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