Drug intelligence / Profile preview

genistein 7-O-phosphate

Development stage
Preclinical
Modality
Small Molecules
Administration
Oral
01

Overview

Genistein 7-O-phosphate (G7P) is a water-soluble phosphate prodrug of the soy isoflavone genistein. It is generated through a biotransformation process using *Bacillus subtilis* var. natto BCRC80517 to overcome the poor aqueous solubility and low oral bioavailability of the parent compound. Upon oral administration, G7P is dephosphorylated by intestinal alkaline phosphatase to release active genistein, exhibiting approximately 3.7-fold higher oral bioavailability than genistein itself. Beyond its role as a prodrug, recent research has identified G7P as an antagonist of mechanosensitive cannabinoid receptor 1 (CB1) in endothelial cells. Preclinical studies have demonstrated its potential in preventing bone loss in osteoporosis models and reducing atherosclerotic plaque formation by reversing endothelial inflammation, oxidative stress, and endothelial-to-mesenchymal transition (EndMT) induced by disturbed blood flow.

Other names
genistein 7-phosphategenistein7-phosphategenistein-7-phosphategenistein-7-O-phosphategenistein7-O-phosphategenistein 7-O-phosphate
02

Targets

CNR1 (Cannabinoid receptor 1)

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