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Enzastaurin


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.

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). The trial was later indefinitely suspended in October 2022 to save costs.

References

References

  1. (2013-05-10). "Lilly Halts Development of Lymphoma Drug After Phase III Failure".
  2. (2022-07-20). "Aytu BioPharma Announces Initiation of the AR101 PREVEnt Trial for the Treatment of Vascular Ehlers-Danlos Syndrome".
  3. "PREVEnt Trial".
  4. "Aytu BioPharma Adds Late-Stage Pediatric Onset Rare Disease Asset to Development Pipeline from Rumpus Therapeutics".
  5. "Clinical Trials".
  6. (2022-10-13). "Aytu BioPharma Announces Strategic Shift to Focus on Commercial Operations and Indefinite Suspension of Clinical Development Programs".
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