Repositioning Candidate Details
| Candidate ID: | R1028 |
| Source ID: | DB06486 |
| Source Type: | investigational |
| Compound Type: | small molecule |
| Compound Name: | Enzastaurin |
| Synonyms: | Enzastaurin |
| Molecular Formula: | C32H29N5O2 |
| SMILES: | CN1C=C(C2=CC=CC=C12)C1=C(C(=O)NC1=O)C1=CN(C2CCN(CC3=CC=CC=N3)CC2)C2=CC=CC=C12 |
| Structure: |
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| DrugBank Description: | Enzastaurin, an investigational, targeted, oral agent, will be evaluated at more than 100 sites worldwide for the treatment of relapsed glioblastoma multiforme (GBM), an aggressive and malignant form of brain cancer. |
| CAS Number: | 170364-57-5 |
| Molecular Weight: | 515.617 |
| DrugBank Indication: | Investigated for use/treatment in brain cancer, lymphoma (non-hodgkin's), and lung cancer. |
| DrugBank Pharmacology: | -- |
| DrugBank MoA: | Enzastaurin is an oral serine-threonine kinase inhibitor that is designed to suppress tumor growth through multiple mechanisms. Preclinical data indicate it may reduce the cell's ability to reproduce (cell proliferation), increase the natural death of the tumor cells (apoptosis), and inhibit tumor- induced blood supply (angiogenesis). Enzastaurin has been shown to inhibit signaling through the PKC-B and PI3K/AKT pathways. These pathways have been shown to be activated in a wide variety of cancers. In addition to glioblastoma, enzastaurin is also being studied in multiple other tumor types, including non-Hodgkin's lymphoma, colorectal cancer, non-small cell lung cancer, pancreatic cancer, and mantle cell lymphoma. |
| Targets: | Protein kinase C beta type; Aurora kinase B; Aurora kinase A; Cyclin-dependent kinase 15; Serine/threonine-protein kinase Chk1; Serine/threonine-protein kinase Chk2; RAC-alpha serine/threonine-protein kinase; Phosphatidylinositol 3-kinase regulatory subunit alpha |
| Inclusion Criteria: | Therapeutic strategy associated |
