molecules of the month

compound 20p

FXR nucl. receptor + TGR5 GPCR dual agonist

dual in vivo effects at 100 mpk PO

from merger of literature agonist fragments

Sci. Rep., Apr. 28, 2021

Fuji Yakuhin Co., Ltd., Saitama, JP

1 min read

The Fuji Yakuhin FXR/TGR5 non-bile acid dual agonist, compound 20p, simultaneously activates the FXR nuclear receptor and the unrelated TGR5 GPCR receptor when dosed orally in vivo. FXR has been a important target for liver disease, and a number of agonists have been in development, including one of last year’s Molecules of the Year. TGR5 is a receptor that stimulates GLP-1 peptide secretion when activated. Oral GLP-1R agonists have similarly been hotly pursued, and have also been featured a few times on Drug Hunter. The combined effect on both agonists was thought to be beneficial for hepatic diseases. By merging elements of FXR and TGR5 agonists, the authors were able to identify this potent dual agonist while maintaining properties for oral dosing. While dual…

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