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enzastaurin

Small moleculeexperimental

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. — Wikipedia

Clinical trial activity

51 trials · 22 clinical orgs · 0 marketing orgs

Phase 1
11
Phase 2
42
Phase 3
4
Phase 4
0

Earliest trial started Jun 1, 2002 (NCT00042666)

Timeline

2000s

  1. Jan 1, 2002

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2002

    Earliest Phase 2 Sponsor(trial)

  3. Jan 1, 2006

    Earliest Phase 3 Sponsor(trial)

Indications

Studied for

Mechanism of action

Chemistry & pharmacology

Loading structure…

SMILES

Cn1cc(C2=C(c3cn(C4CCN(Cc5ccccn5)CC4)c4ccccc34)C(=O)NC2=O)c2ccccc21
Mol. weight
515.62 g/mol
Lipinski Ro5
1 violation(s)
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • enzastaurin
  • enzastaurin
  • enzastaurin
  • enzastaurin
  • enzastaurin hcl
  • enzastaurin hcl
  • enzastaurin hydrochloride
  • enzastaurin hydrochloride
  • ly317615
  • ly317615
  • ly-317615
  • ly-317615
  • ly317615.hcl

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT05463679Phase 3Jan 31, 2024AYTU BioScience, Baylor University, Parexel, University of Washington
NCT03776071Phase 2Jun 30, 2019Denovo BioPharma
NCT03263026Phase 3Mar 20, 2018Denovo BioPharma
NCT01432951Phase 1Nov 1, 2011Eli Lilly
NCT01388335Phase 1Aug 1, 2011Eli Lilly
NCT00685633Phase 2Dec 1, 2008Eastern Cooperative Oncology Group, Johns Hopkins University, National Cancer Institute (NCI), New York University
NCT00744991Phase 2Sep 1, 2008Eli Lilly
NCT00718419Phase 2Jul 1, 2008Eli Lilly
NCT00709995Phase 2Jun 1, 2008Eli Lilly
NCT00612586Phase 2Feb 1, 2008Eli Lilly, Roche
NCT00536939Phase 2Nov 1, 2007Eli Lilly, Genentech
NCT00542919Phase 2Nov 1, 2007Eli Lilly
NCT00586508Phase 2Nov 1, 2007Eli Lilly, Genentech
NCT00533429Phase 2Oct 1, 2007Eli Lilly, Genentech
NCT00509821Phase 2Oct 1, 2007Eli Lilly
NCT00530621Phase 2Sep 1, 2007Eli Lilly
NCT00538681Phase 2Sep 1, 2007Eli Lilly
NCT00516607Phase 1Jul 1, 2007European Organisation for Research and Treatment of Cancer, University of Glasgow
NCT00503724Phase 1Jun 1, 2007Baylor University, National Cancer Institute (NCI), Pediatric Brain Tumor Consortium
NCT00466440Phase 2Jun 1, 2007Eli Lilly
Showing 20 of 51 trials
Page 1 / 3

Organizations

Research & Development (22)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Eli LillyFor profit414132002
National Cancer Institute (NCI)Government8122002
GenentechFor profit3012007
Baylor UniversityAcademic/Hospital2022007
Denovo BioPharmaFor profit2222018
Eastern Cooperative Oncology GroupAcademic/Hospital2212007
Gynecologic Oncology GroupAcademic/Hospital2112006
Johns Hopkins UniversityAcademic/Hospital2022006
AYTU BioScienceFor profit1112024
European Organisation for Research and Treatment of CancerAcademic/Hospital1112007
New York UniversityAcademic/Hospital1012008
Northwestern UniversityAcademic/Hospital1012006
ParexelFor profit1012024
Pediatric Brain Tumor ConsortiumAcademic/Hospital1112007
Pennsylvania State UniversityAcademic/Hospital1012007
RocheFor profit1012008
Rush UniversityAcademic/Hospital1012006
University of California, Los AngelesAcademic/Hospital1112002
University of California, San FranciscoAcademic/Hospital1012006
University of GlasgowAcademic/Hospital1012007
22 organizations
Page 1 / 2