Asengeprast
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Other names
FT011
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3D model (JSmol)
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PubChem CID
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UNII | |
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Properties | |
C20H17NO5 | |
Molar mass | 351.358 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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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
[edit]References
[edit]- ^ "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.
- ^ Gilbert RE, Zhang Y, Williams SJ, Zammit SC, Stapleton DI, Cox AJ, Krum H, Langham R, Kelly DJ (2012). "A purpose-synthesised anti-fibrotic agent attenuates experimental kidney diseases in the rat". PLOS ONE. 7 (10): e47160. doi:10.1371/journal.pone.0047160. PMC 3468513. PMID 23071743.
- ^ Zammit SC, Cox AJ, Gow RM, Zhang Y, Gilbert RE, Krum H, Kelly DJ, Williams SJ (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.