Asengeprast

Last updated

Asengeprast
Asengeprast.svg
Chemical structure of asengeprast (FT011)
Clinical data
Other namesFT011
Identifiers
  • 2-[[(E)-3-(3-methoxy-4-prop-2-ynoxyphenyl)prop-2-enoyl]amino]benzoic acid
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
Chemical and physical data
Formula C20H17NO5
Molar mass 351.358 g·mol−1
3D model (JSmol)
  • COC1=C(C=CC(=C1)/C=C/C(=O)NC2=CC=CC=C2C(=O)O)OCC#C
  • 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. [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

  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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