Chemistry: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.
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
References
- ↑ "Asengeprast Ligand page". IUPHAR/BPS Guide to PHARMACOLOGY. https://www.guidetopharmacology.org/GRAC/LigandDisplayForward?tab=clinical&ligandId=13202.
- ↑ "Certa Therapeutics website". https://certatherapeutics.com/.
- ↑ "Certa's FT011 granted orphan drug status in Europe for SSc". Scleroderma News. 23 July 2024. https://sclerodermanews.com/news/orphan-drug-status-europe-granted-ft011-certa-therapy-ssc/.
- ↑ "FT011, a new anti-fibrotic drug, attenuates fibrosis and chronic heart failure in experimental diabetic cardiomyopathy". European Journal of Heart Failure 14 (5): 549–562. May 2012. doi:10.1093/eurjhf/hfs011. PMID 22417655.
- ↑ "A purpose-synthesised anti-fibrotic agent attenuates experimental kidney diseases in the rat". PLOS ONE 7 (10). 2012. doi:10.1371/journal.pone.0047160. PMID 23071743. Bibcode: 2012PLoSO...747160G.
- ↑ "Evaluation and optimization of antifibrotic activity of cinnamoyl anthranilates". Bioorganic & Medicinal Chemistry Letters 19 (24): 7003–7006. December 2009. doi:10.1016/j.bmcl.2009.09.120. PMID 19879136.
 |  |
