Enzastaurin
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Names | |
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Preferred IUPAC name 3-(1-Methyl-1H-indol-3-yl)-4-(1-{1-[(pyridin-2-yl)methyl]piperidin-4-yl}-1H-indol-3-yl)-1H-pyrrole-2,5-dione | |
Other names LY-317615 | |
Identifiers | |
3D model (JSmol) | |
ChEMBL | |
ChemSpider | |
ECHA InfoCard | 100.233.143 |
KEGG | |
PubChem CID | |
UNII | |
CompTox Dashboard (EPA) | |
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Properties | |
C32H29N5O2 | |
Molar mass | 515.617 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa). |
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
[edit]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]
References
[edit]- ^ Lilly Halts Development of Lymphoma Drug After Phase III Failure
- ^ "New vEDS clinical trial". PREVEnt Trial. Retrieved 2022-01-19.
- ^ "Aytu BioPharma Adds Late-Stage Pediatric Onset Rare Disease Asset to Development Pipeline from Rumpus Therapeutics". BioSpace. Retrieved 2022-01-19.
- ^ "Clinical Trials". FIGHT vEDS 3.0. Retrieved 2022-01-19.
External links
[edit]- Enzastaurin hydrochloride, National Institutes of Health