Drug intelligence / Profile preview

GlucoRegulate

Development stage
Unknown
Lead developer
Glocentrica
Modality
Small Molecules
Administration
Oral
01

Overview

GlucoRegulate (trans-resveratrol + hesperetin, also known as tRES-HESP) is a patented, synergistic co-formulation of two plant-derived small molecules: trans-resveratrol and hesperetin. It is designed as a pharmacological inducer of glyoxalase 1 (Glo1) to alleviate dicarbonyl stress and improve metabolic health. The formulation works by activating the transcription factor Nrf2 (nuclear factor erythroid 2-related factor 2) through the antioxidant response element (ARE) in the GLO1 gene, thereby increasing Glo1 expression and activity. This leads to the detoxification of the reactive dicarbonyl glycating agent methylglyoxal (MG), reducing protein glycation, the unfolded protein response (UPR), and low-grade inflammation. Developed by Glocentrica and marketed by GloVitality, the formulation is in clinical development as a precision dietary supplement or nutraceutical. In a Phase 2a clinical trial (NCT02095873) in overweight and obese subjects, once-daily oral administration of the formulation (90 mg trans-resveratrol and 120 mg hesperetin) significantly increased Glo1 activity, decreased plasma methylglyoxal, improved insulin sensitivity, and lowered fasting and postprandial glucose levels.

Brand names
GlucoRegulate
Other names
Glo1 inducer formulationGlo-1 inducer formulationGlo 1 inducer formulationGlyoxalase 1 inducer formulationGlyoxalase1 inducer formulationGlyoxalase-1 inducer formulationtRES-HESPtRES+HESPtrans-resveratrol + hesperetintrans-resveratrol and hesperetin combination
02

Targets

NFE2L2 (Nuclear factor (erythroid-derived 2)-like 2)

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