Drug intelligence / Profile preview

trans-resveratrol + hesperetin

Development stage
Unknown
Lead developer
Hamad Bin Khalifa University
Modality
Small Molecules
Administration
Oral
01

Overview

Glyoxalase 1 inducer (specifically the trans-resveratrol and hesperetin combination, commercialized as GlucoRegulate) is a synergistic small-molecule formulation designed to increase the expression and activity of glyoxalase 1 (Glo1). Developed by the University of Warwick and commercialized by GloVitality, this dietary supplement activates the Nrf2 pathway to enhance the detoxification of methylglyoxal, a reactive dicarbonyl byproduct of glycolysis that drives dicarbonyl stress, insulin resistance, and vascular inflammation. By combining trans-resveratrol (which inhibits cAMP phosphodiesterases and activates sirtuin-1) with hesperetin (which activates protein kinase A), the formulation achieves potent pharmacological synergy at clinically translatable doses. It has been evaluated in Phase 2 clinical trials for the correction of insulin resistance, glycemic control, and vascular inflammation in overweight and obese subjects, and is being positioned for the prevention of type 2 diabetes and metabolic dysfunction-associated steatotic liver disease (MASLD).

Brand names
GlucoRegulate
Other names
Glo1 inducerGlo-1 inducerGlo 1 inducerGlyoxalase 1 inducerGlyoxalase1 inducerGlyoxalase-1 inducer
02

Targets

AMPK (Adenosine monophosphate–activated protein kinase)GLO1 (Glyoxalase 1)NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)PDE1 (Phosphodiesterase 1)PKA (Cyclic amp-dependent protein kinase)SIRT1 (NAD-dependent protein deacetylase sirtuin-1)

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