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metformin + sitagliptin
- Development stage
- Unknown
- Lead developer
- Bristol Myers Squibb
- Modality
- Small Molecules
- Administration
- Oral
01
Overview
MTF-3110 is a fixed-dose combination (FDC) of the biguanide metformin (500 mg) and the dipeptidyl peptidase-4 (DPP-4) inhibitor sitagliptin (50 mg). Developed by MTF Australia Pty Ltd, it is currently being evaluated in Phase 2 clinical trials for the treatment of Latent Autoimmune Diabetes in Adults (LADA). LADA is a form of autoimmune diabetes that typically presents in adulthood and is characterized by the presence of islet autoantibodies and a slower progression toward insulin dependence compared to classic type 1 diabetes. The therapeutic rationale for MTF-3110 in LADA involves preserving pancreatic beta-cell function through a dual mechanism: metformin reduces metabolic stress and may modulate immune responses via AMP-activated protein kinase (AMPK) activation, while sitagliptin increases levels of glucagon-like peptide-1 (GLP-1), which promotes beta-cell survival and potentially exerts further immunomodulatory effects through DPP-4 (CD26) inhibition.
- Other names
- metformin + sitagliptin
02
Targets
AMPK (Adenosine monophosphate–activated protein kinase)GPD2 (Glycerol-3-phosphate dehydrogenase 2)OCT1 (Organic cation transporter 1)DPP-4 (Dipeptidyl Peptidase-IV)ND1 (Mitochondrial electron transport chain complex I)
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