Asengeprast

📅 آخر تحديث: ٣٠ يوليو ٢٠٢٦
✍️ نُشر في: ٣٠ يوليو ٢٠٢٦
الموسوعة الحرة

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. ↑ زاميت إس سي، كوكس إيه جيه، غاو آر إم، تشانغ واي، جيلبرت آر إي، كروم إتش، وآخرون . (ديسمبر 2009). "تقييم وتحسين النشاط المضاد للتليف لسينامويل أنثرانيلات". رسائل الكيمياء العضوية والطبية الحيوية . 19 (24): 7003-7006 . doi : 10.1016/j.bmcl.2009.09.120 . PMID 19879136 .