Enzastaurin

Enzastaurin

Names
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
CAS Number	170364-57-5  Y
3D model (JSmol)	Interactive image
ChEMBL	ChEMBL300138  N
ChemSpider	153463  N
ECHA InfoCard	100.233.143
IUPHAR/BPS	5693
KEGG	D11935
PubChem CID	176167
UNII	UC96G28EQF  Y
CompTox Dashboard (EPA)	DTXSID5044029
InChI InChI=1S/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39) N Key: AXRCEOKUDYDWLF-UHFFFAOYSA-N N InChI=1/C32H29N5O2/c1-35-19-25(23-9-2-4-11-27(23)35)29-30(32(39)34-31(29)38)26-20-37(28-12-5-3-10-24(26)28)22-13-16-36(17-14-22)18-21-8-6-7-15-33-21/h2-12,15,19-20,22H,13-14,16-18H2,1H3,(H,34,38,39) Key: AXRCEOKUDYDWLF-UHFFFAOYAP
SMILES O=C3C(\c2c1ccccc1n(c2)C)=C(/C(=O)N3)c5c4ccccc4n(c5)C7CCN(Cc6ncccc6)CC7
Properties
Chemical formula	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). N  verify  (what is  YN ?) Infobox references

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

In 2013 it failed a phase III clinical trial by Lilly for lymphoma. ^[1]

In July 2022, there was another phase III trial called PREVEnt by Aytu BioPharma to look into the effectiveness of enzastaurin for the treatment of Vascular Elhers-Danlos syndrome (vEDS). ^{[2] [3] [4] [5]} The trial was later indefinitely suspended in October 2022 to save costs. ^[6]

References

1. "Lilly Halts Development of Lymphoma Drug After Phase III Failure". GEN - Genetic Engineering and Biotechnology News. 2013-05-10. Retrieved 2025-11-11.
2. "Aytu BioPharma Announces Initiation of the AR101 PREVEnt Trial for the Treatment of Vascular Ehlers-Danlos Syndrome". ACCESS Newswire. 2022-07-20. Archived from the original on 2023-06-09. Retrieved 2025-11-11.
3. "PREVEnt Trial". preventvedstrial.com. Archived from the original on 2022-01-24. Retrieved 2022-01-19.
4. "Aytu BioPharma Adds Late-Stage Pediatric Onset Rare Disease Asset to Development Pipeline from Rumpus Therapeutics". BioSpace. Retrieved 2025-11-11.
5. "Clinical Trials". FIGHT vEDS. Retrieved 2022-01-19.
6. "Aytu BioPharma Announces Strategic Shift to Focus on Commercial Operations and Indefinite Suspension of Clinical Development Programs". ACCESS Newswire. 2022-10-13. Archived from the original on 2024-07-21. Retrieved 2025-11-11.

External links

• Enzastaurin hydrochloride, National Institutes of Health