Drug intelligence / Profile preview

metformin

Development stage
Approved
Lead developer
Bristol Myers Squibb
Modality
Small Molecules
Administration
Oral
01

Overview

Metformin is a biguanide antihyperglycemic agent and the main first-line medication for the treatment of type 2 diabetes mellitus. It is also used off-label for insulin resistance in polycystic ovary syndrome (PCOS) and sometimes as an adjunct to reduce metabolic syndrome risk in people taking antipsychotic medications. Metformin works primarily by decreasing hepatic glucose production (gluconeogenesis), reducing intestinal absorption of glucose from food intake and increasing insulin sensitivity by enhancing peripheral glucose uptake and utilization. It also increases GDF15 secretion which may reduce appetite and caloric intake. The drug inhibits mitochondrial complex I activity—a mechanism believed to underlie its antidiabetic effects[1][4][7]. Metformin does not cause weight gain and has a low risk of hypoglycemia when used alone[5][7]. First described in 1922 and introduced as a medication in France in 1957 after human studies by Jean Sterne[7], it is now available worldwide as both branded and generic formulations.

Brand names
FortametGlucophageGlucophage XRGlumetzaRiometRiomet ERACT metFORMINAG-metFORMIN - BlackberryAG-metFORMIN - UnflavoredAPO-metFORMINAPO-metFORMIN ERAURO-metFORMINAVA-metFORMINBio-metFORMIN
Other names
ObimetGluforminDianbenDiabexDiaforminMetsolSioforMetfogammaGlifor
02

Targets

Presenilin enhancer protein 2 (PEN-2) / lysosomal vacuolar-type H+-ATPase (v-ATPase) complexHMGB1 (High mobility group protein B1)ND1 (Mitochondrial electron transport chain complex I)CYP3A4 (Cytochrome P450 3A4)DHFR (Dihydrofolate reductase)

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