enzastaurin

Enzastaurin is an orally available, synthetic bisindolylmaleimide and small-molecule serine/threonine kinase inhibitor with antineoplastic activity. It selectively inhibits protein kinase C beta (PKCβ), a key enzyme involved in tumor-induced angiogenesis, cell proliferation, and survival. By binding to the ATP-binding site of PKCβ, enzastaurin suppresses signaling through the PKCβ and PI3K/AKT pathways—both commonly activated in various cancers—leading to reduced tumor cell proliferation, increased apoptosis, and inhibition of tumor-induced blood supply (antiangiogenesis). Originally developed as an antiangiogenic cancer therapy by Eli Lilly, it has been investigated for multiple indications including glioblastoma multiforme (GBM), diffuse large B-cell lymphoma (DLBCL), Ehlers-Danlos syndrome (vEDS), non-Hodgkin's lymphoma, colorectal cancer, lung cancer, pancreatic cancer, mantle cell lymphoma and others. Despite promising preclinical results and orphan drug status for some rare diseases such as DLBCL and vEDS, clinical efficacy was limited in late-stage trials for several cancers.

Brand names

Kinenza

Other names

Enzastaurin hydrochloride