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.
In 2013 it failed a phase III clinical trial for lymphoma.[1]
In 2022, there is an upcoming initial trial called PREVEnt to look into the effectiveness of Enzastaurin for the treatment of Vascular Elhers-Danlos syndrome (vEDS). [2] [3] [4]