Asengeprast

Asengeprast
	Chemical structure of asengeprast (FT011)
Clinical data
Other names	FT011
Identifiers
	IUPAC name 2-[[(E)-3-(3-methoxy-4-prop-2-ynoxyphenyl)prop-2-enoyl]amino]benzoic acid;
CAS Number	1001288-58-9;
PubChem CID	23648966;
ChemSpider	24664633;
UNII	C6V7ZU2NPR;
ChEMBL	ChEMBL1075834;
Chemical and physical data
Formula	C20H17NO5
Molar mass	351.358 g·mol−1
3D model (JSmol)	Interactive image;
	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.^[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]

References

^ "Asengeprast Ligand page". IUPHAR/BPS Guide to PHARMACOLOGY.
^ "Certa Therapeutics website".
^ Inácio P (23 July 2024). "Certa's FT011 granted orphan drug status in Europe for SSc". Scleroderma News.
^ 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.
^ 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.
^ 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.

[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.

[1]

See also

References