rebastinib
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
Earliest trial started Mar 1, 2009 (NCT00827138)
Timeline
2000s
- Jan 1, 2009
Earliest Phase 1 Sponsor(trial)
Indications
Mechanism of action
- Tyrosine-protein kinase ABLINHIBITOR
ABL1 inhibitor
Also potent against other kinases (Src, LYN, FGR, and HCK, KDR, FLT3 and TIE2)
Chemistry & pharmacology
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
- WikipediaBcr-Abl tyrosine-kinase inhibitor ↗
- ChEMBLCHEMBL1738757 ↗
Also known as
- dcc-2036
- dcc-2036
- dcc-2036
- dp-1919
- dp-1919
- rebastinib
- rebastinib
- rebastinib
- rebastinib
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT03717415 | Phase 1/Phase 2 (Phase 2) | Jan 2, 2019 | Deciphera Pharmaceuticals LLC |
| NCT03601897 | Phase 1/Phase 2 (Phase 2) | Sep 26, 2018 | Deciphera Pharmaceuticals LLC |
| NCT02824575 | Phase 1 | Jul 1, 2016 | Deciphera Pharmaceuticals LLC, Yeshiva University |
| NCT00827138 | Phase 1 | Mar 1, 2009 | City 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 |
Organizations
Research & Development (12)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Deciphera Pharmaceuticals LLC | For profit | 4 | 3 | 2 | 2009 |
| City of Hope National Medical Center | Academic/Hospital | 1 | 0 | 1 | 2009 |
| Emory University | Academic/Hospital | 1 | 0 | 1 | 2009 |
| Johns Hopkins University | Academic/Hospital | 1 | 0 | 1 | 2009 |
| Medical College of Wisconsin | Academic/Hospital | 1 | 0 | 1 | 2009 |
| Tufts University | Academic/Hospital | 1 | 0 | 1 | 2009 |
| University of Chicago | Academic/Hospital | 1 | 0 | 1 | 2009 |
| University of Kansas | Academic/Hospital | 1 | 0 | 1 | 2009 |
| University of Michigan | Academic/Hospital | 1 | 0 | 1 | 2009 |
| University of South Florida | Academic/Hospital | 1 | 0 | 1 | 2009 |
| University of Texas at Houston | Academic/Hospital | 1 | 0 | 1 | 2009 |
| Yeshiva University | Academic/Hospital | 1 | 1 | 1 | 2016 |