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Asengeprast

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Chemical compound

Pharmaceutical compound
Asengeprast
Chemical structure of asengeprast (FT011)
Clinical data
Other namesFT011
Identifiers
IUPAC name
  • 2-amino]benzoic acid
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC20H17NO5
Molar mass351.358 g·mol
3D model (JSmol)
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

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. 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).

Asengeprast has been reported to attenuate fibrosis and chronic heart failure in experimental diabetic cardiomyopathy. Asengeprast can also inhibit kidney fibrosis and prevent kidney failure. 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.

See also

References

  1. "Asengeprast Ligand page". IUPHAR/BPS Guide to PHARMACOLOGY.
  2. "Certa Therapeutics website".
  3. Inácio P (23 July 2024). "Certa's FT011 granted orphan drug status in Europe for SSc". Scleroderma News.
  4. Zhang Y, Edgley AJ, Cox AJ, Powell AK, Wang B, Kompa AR, et al. (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): 549–562. doi:10.1093/eurjhf/hfs011. PMID 22417655.
  5. Gilbert RE, Zhang Y, Williams SJ, Zammit SC, Stapleton DI, Cox AJ, et al. (2012). "A purpose-synthesised anti-fibrotic agent attenuates experimental kidney diseases in the rat". PLOS ONE. 7 (10): e47160. Bibcode:2012PLoSO...747160G. doi:10.1371/journal.pone.0047160. PMC 3468513. PMID 23071743.
  6. Zammit SC, Cox AJ, Gow RM, Zhang Y, Gilbert RE, Krum H, et al. (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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