Asengeprast
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| Other names
FT011
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3D model (JSmol)
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CompTox Dashboard (EPA)
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| Properties | |
| C17H20NO5 | |
| Molar mass | 318.349 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). | |
| Infobox references | |
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) have 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] 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.[5]
References
- ↑ "Asengeprast | Ligand page | IUPHAR/BPS Guide to PHARMACOLOGY".
- ↑ "Certa Therapeutics website".
- ↑ "Scleroderma News". 23 July 2024.
- ↑ Zhang, Y; Edgley, AJ; Cox, AJ; Powell, AK; Wang, B; Kompa, AR; Stapleton, DI; Zammit, SC; Williams, SJ; Krum, H; Gilbert, RE; Kelly, DJ (May 2012). "FT011, a new anti-fibrotic drug, attenuates fibrosis and chronic heart failure in experimental diabetic cardiomyopathy". European Journal of Heart Failure. 14 (5): 549–62. doi:10.1093/eurjhf/hfs011. PMID 22417655.
- ↑ Zammit, Steven C.; Cox, Alison J.; Gow, Renae M.; Zhang, Yuan; Gilbert, Richard E.; Krum, Henry; Kelly, Darren J.; Williams, Spencer J. (December 2009). "Evaluation and optimization of antifibrotic activity of cinnamoyl anthranilates". Bioorganic & Medicinal Chemistry Letters. 19 (24): 7003–7006. doi:10.1016/j.bmcl.2009.09.120. PMID 19879136.
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