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entospletinib

Small moleculeexperimental

Entospletinib is an experimental drug for the treatment of various types of cancer under development by Gilead Sciences. It is an inhibitor of spleen tyrosine kinase (Syk). It has entered clinical trials for acute myeloid leukaemia (AML), chronic lymphocytic leukemia (CLL), diffuse large B cell lymphoma (DLBCL), graft-versus-host disease (GvHD), hematological malignancies, mantle cell lymphoma (MCL), and non-Hodgkin lymphoma (NHL). — Wikipedia

Clinical trial activity

17 trials · 11 clinical orgs · 0 marketing orgs

Phase 1
12
Phase 2
10
Phase 3
1
Phase 4
0

Earliest trial started Oct 1, 2010 (NCT01181700)

Timeline

2010s

  1. Jan 1, 2010

    Earliest Phase 1 Sponsor(trial)

  2. Jan 1, 2013

    Earliest Phase 2 Sponsor(trial)

2020s

  1. Jan 1, 2021

    Earliest Phase 3 Sponsor(trial)

Indications

Studied for

Mechanism of action

Chemistry & pharmacology

Loading structure…

SMILES

c1cn2cc(-c3ccc4cn[nH]c4c3)nc(Nc3ccc(N4CCOCC4)cc3)c2n1
Mol. weight
411.47 g/mol
Lipinski Ro5
Pass
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • 6-(1h-indazol-6-yl)-n-(4-morpholinophenyl)imidazo(1,2-a)pyrazin-8-amine
  • entospletinib
  • entospletinib
  • entospletinib
  • entospletinib
  • gs-9973
  • gs-9973
  • gs-9973
  • gs-9973

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT05020665Phase 3Nov 30, 2021Kronos Bio
NCT03225924Phase 1/Phase 2 (Phase 2)Jul 26, 2017CHU UCL Namur, The Lymphoma Academic Research Organisation, University of Lyon, University of Montpellier
NCT03010358Phase 1/Phase 2 (Phase 2)Jun 1, 2017National Cancer Institute (NCI), Oregon Health and Science University
NCT03135028Phase 1May 18, 2017Gilead Sciences
NCT02983617Phase 2Apr 6, 2017German CLL Study Group, Gilead Sciences
NCT03013998Phase 1/Phase 2 (Phase 2)Nov 1, 2016Beat AML
NCT02701634Phase 2May 27, 2016Gilead Sciences
NCT02568683Phase 1/Phase 2 (Phase 2)Feb 11, 2016Gilead Sciences
NCT02521376Phase 1Nov 16, 2015Gilead Sciences
NCT02343939Phase 1/Phase 2 (Phase 2)Jul 1, 2015Gilead Sciences
NCT02457598Phase 1Jun 16, 2015Gilead Sciences
NCT02404220Phase 1May 28, 2015Gilead Sciences
NCT01796470Phase 2Jun 1, 2013Gilead Sciences
NCT01841489Phase 1May 1, 2013Gilead Sciences
NCT01799889Phase 2Mar 14, 2013Gilead Sciences
NCT01272375Phase 1Jan 1, 2011Pfizer
NCT01181700Phase 1Oct 1, 2010Pfizer
Showing 17 of 17 trials
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Organizations

Research & Development (11)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Gilead SciencesFor profit111122013
PfizerFor profit2212010
Beat AMLAcademic/Hospital1112016
CHU UCL NamurAcademic/Hospital1012017
German CLL Study GroupAcademic/Hospital1012017
Kronos BioFor profit1112021
National Cancer Institute (NCI)Government1012017
Oregon Health and Science UniversityAcademic/Hospital1112017
The Lymphoma Academic Research OrganisationAcademic/Hospital1112017
University of LyonAcademic/Hospital1012017
University of MontpellierAcademic/Hospital1012017
11 organizations
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