Chemistry:Enzastaurin

From HandWiki

Enzastaurin is a synthetic bisindolylmaleimide with potential antineoplastic activity. Binding to the ATP-binding site, enzastaurin selectively inhibits protein kinase C beta, an enzyme involved in the induction of vascular endothelial growth factor (VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply, preventing growth.

Trials

In 2013 it failed a phase III clinical trial by Lilly for lymphoma.[1]

In July 2022, there was another phase III trial called PREVEnt by Aytu BioPharma to look into the effectiveness of enzastaurin for the treatment of Vascular Elhers-Danlos syndrome (vEDS).[2][3][4][5] The trial was later indefinitely suspended in October 2022 to save costs.[6]

References

  1. ↑ "Lilly Halts Development of Lymphoma Drug After Phase III Failure" (in en-US). 2013-05-10. https://www.genengnews.com/news/lilly-halts-development-of-lymphoma-drug-after-phase-iii-failure/. 
  2. ↑ "Aytu BioPharma Announces Initiation of the AR101 PREVEnt Trial for the Treatment of Vascular Ehlers-Danlos Syndrome" (in en). 2022-07-20. https://www.accesswire.com/709075/Aytu-BioPharma-Announces-Initiation-of-the-AR101-PREVEnt-Trial-for-the-Treatment-of-Vascular-Ehlers-Danlos-Syndrome. 
  3. ↑ "PREVEnt Trial" (in en-US). https://preventvedstrial.com/. 
  4. ↑ "Aytu BioPharma Adds Late-Stage Pediatric Onset Rare Disease Asset to Development Pipeline from Rumpus Therapeutics" (in en-US). https://www.biospace.com/aytu-biopharma-adds-late-stage-pediatric-onset-rare-disease-asset-to-development-pipeline-from-rumpus-therapeutics. 
  5. ↑ "Clinical Trials" (in en). https://www.fightveds.org/clinical-trials. 
  6. ↑ "Aytu BioPharma Announces Strategic Shift to Focus on Commercial Operations and Indefinite Suspension of Clinical Development Programs" (in en). 2022-10-13. https://www.accesswire.com/720110/aytu-biopharma-announces-strategic-shift-to-focus-on-commercial-operations-and-indefinite-suspension-of-clinical-development-programs. 



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