rebastinib

Small moleculeexperimental

Bcr-Abl tyrosine-kinase inhibitors (TKI) are the first-line therapy for most patients with chronic myelogenous leukemia (CML). More than 90% of CML cases are caused by a chromosomal abnormality that results in the formation of a so-called Philadelphia chromosome. This abnormality was discovered by Peter Nowell in 1960 and is a consequence of fusion between the Abelson (Abl) tyrosine kinase gene at chromosome 9 and the break point cluster (Bcr) gene at chromosome 22, resulting in a chimeric oncogene (Bcr-Abl) and a constitutively active Bcr-Abl tyrosine kinase that has been implicated in the pathogenesis of CML. Compounds have been developed to selectively inhibit the tyrosine kinase. — Wikipedia

Clinical trial activity

4 trials · 12 clinical orgs · 0 marketing orgs

Phase 1
4
Phase 2
2
Phase 3
0
Phase 4
0

Earliest trial started Mar 1, 2009 (NCT00827138)

Timeline

2000s

  1. Jan 1, 2009

    Earliest Phase 1 Sponsor(trial)

Indications

Mechanism of action

Chemistry & pharmacology

Loading structure…

SMILES

CNC(=O)c1cc(Oc2ccc(NC(=O)Nc3cc(C(C)(C)C)nn3-c3ccc4ncccc4c3)c(F)c2)ccn1
Mol. weight
553.6 g/mol
Lipinski Ro5
2 violation(s)
Rule of 3
No
Chirality
Achiral Molecule
Inorganic
No
Polymer
No

Oral

No

Parenteral

No

Topical

No

Sources

Also known as

  • dcc-2036
  • dcc-2036
  • dcc-2036
  • dp-1919
  • dp-1919
  • rebastinib
  • rebastinib
  • rebastinib
  • rebastinib

Clinical trials

NCT IDPhaseStart dateSponsor(s)
NCT03717415Phase 1/Phase 2 (Phase 2)Jan 2, 2019Deciphera Pharmaceuticals LLC
NCT03601897Phase 1/Phase 2 (Phase 2)Sep 26, 2018Deciphera Pharmaceuticals LLC
NCT02824575Phase 1Jul 1, 2016Deciphera Pharmaceuticals LLC, Yeshiva University
NCT00827138Phase 1Mar 1, 2009City of Hope National Medical Center, Deciphera Pharmaceuticals LLC, Emory University, Johns Hopkins University, Medical College of Wisconsin, Tufts University, University of Chicago, University of Kansas, University of Michigan, University of South Florida, University of Texas at Houston
Showing 4 of 4 trials
Page 1 / 1

Organizations

Research & Development (12)

OrganizationOrg typeTrialsAs lead sponsorPhasesEarliest year
Deciphera Pharmaceuticals LLCFor profit4322009
City of Hope National Medical CenterAcademic/Hospital1012009
Emory UniversityAcademic/Hospital1012009
Johns Hopkins UniversityAcademic/Hospital1012009
Medical College of WisconsinAcademic/Hospital1012009
Tufts UniversityAcademic/Hospital1012009
University of ChicagoAcademic/Hospital1012009
University of KansasAcademic/Hospital1012009
University of MichiganAcademic/Hospital1012009
University of South FloridaAcademic/Hospital1012009
University of Texas at HoustonAcademic/Hospital1012009
Yeshiva UniversityAcademic/Hospital1112016
12 organizations
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