Enzastaurin is a synthetic bisindolylmaleimide with potential antineoplastic activity. Binding to the ATP-binding site, enzastaurin selectively inhibits

protein kinase C In cell biology, protein kinase C, commonly abbreviated to PKC (EC 2.7.11.13), is a family of protein kinase enzymes that are involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and t ...

beta, an enzyme involved in the induction of

vascular endothelial growth factor Vascular endothelial growth factor (VEGF, ), originally known as vascular permeability factor (VPF), is a signal protein produced by many cells that stimulates the formation of blood vessels. To be specific, VEGF is a sub-family of growth factors ...

(VEGF)-stimulated neo-angiogenesis. This agent may decrease tumor blood supply, preventing growth.

Trials

In 2013 it failed a phase III clinical trial for

lymphoma Lymphoma is a group of blood and lymph tumors that develop from lymphocytes (a type of white blood cell). The name typically refers to just the cancerous versions rather than all such tumours. Signs and symptoms may include enlarged lymph node ...

.Lilly Halts Development of Lymphoma Drug After Phase III Failure
/ref> 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).

References

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External links

Enzastaurin hydrochloride
National Institutes of Health 2-Pyridyl compounds Piperidines Bisindolylmaleimides Orphan drugs