Asengeprast
Chemical structure of asengeprast (FT011)
Names
Other names
FT011
Identifiers
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).
Tracking categories (test):

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

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] 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

edit
  1. ^ "Certa Therapeutics website".
  2. ^ "University of Melbourne - Research".
  3. ^ "Scleroderma News".
  4. ^ 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.
  5. ^ 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.