Enzastaurin

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.

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
3D model (JSmol)
ChEMBL
ChemSpider
ECHA InfoCard 100.233.143
KEGG
UNII
  • 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
  • O=C3C(\c2c1ccccc1n(c2)C)=C(/C(=O)N3)c5c4ccccc4n(c5)C7CCN(Cc6ncccc6)CC7
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).
☒N verify (what is checkY☒N ?)
Infobox references

Trials

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
  1. Lilly Halts Development of Lymphoma Drug After Phase III Failure
  2. "New vEDS clinical trial". PREVEnt Trial. Retrieved 2022-01-19.
  3. "Aytu BioPharma Adds Late-Stage Pediatric Onset Rare Disease Asset to Development Pipeline from Rumpus Therapeutics". BioSpace. Retrieved 2022-01-19.
  4. "Clinical Trials". FIGHT vEDS 3.0. Retrieved 2022-01-19.
This article is issued from Wikipedia. The text is licensed under Creative Commons - Attribution - Sharealike. Additional terms may apply for the media files.