Asengeprast

Asengeprast (development code FT011) is an experimental scleroderma drug candidate.^[1] It is a small molecule inhibitor of the G-protein coupled receptor GPR68 with antifibrotic activity.^[2] It is being developed by Certa Therapeutics.

Asengeprast

Chemical structure of asengeprast (FT011)
Clinical data
Other names	FT011
Identifiers
IUPAC name 2-[[(E)-3-(3-methoxy-4-prop-2-ynoxyphenyl)prop-2-enoyl]amino]benzoic acid
CAS Number	1001288-58-9
PubChem CID	23648966
ChemSpider	24664633
UNII	C6V7ZU2NPR
ChEMBL	ChEMBL1075834
Chemical and physical data
Formula	C20H17NO5
Molar mass	351.358 g·mol−1
3D model (JSmol)	Interactive image
SMILES COC1=C(C=CC(=C1)/C=C/C(=O)NC2=CC=CC=C2C(=O)O)OCC#C
InChI InChI=InChI=1S/C20H17NO5/c1-3-12-26-17-10-8-14(13-18(17)25-2)9-11-19(22)21-16-7-5-4-6-15(16)20(23)24/h1,4-11,13H,12H2,2H3,(H,21,22)(H,23,24)/b11-9+ Key:UIWZIDIJCUEOMT-PKNBQFBNSA-N

The European Medicines Agency (EMA) and the U.S. Food and Drug Administration (FDA) has granted orphan drug status to FT011, for systemic sclerosis (SSc).^[3]

Asengeprast has been reported to attenuate fibrosis and chronic heart failure in experimental diabetic cardiomyopathy.^[4] Asengeprast can also inhibit kidney fibrosis and prevent kidney failure.^[5] It was developed by structure-activity optimization of the antifibrotic activity of cinnamoyl anthranilates, by assessment of their ability to prevent TGF-beta-stimulated production of collagen.^[6]

See also

• Tranilast