lestaurtinib
Small moleculeexperimental
Lestaurtinib is a tyrosine kinase inhibitor structurally related to staurosporine. This semisynthetic derivative of the indolocarbazole K252a was investigated by Cephalon as a treatment for various types of cancer. It is an inhibitor of the kinases fms-like tyrosine kinase 3 (FLT3), Janus kinase 2 (JAK2), tropomyosin receptor kinase (trk) A (TrkA), TrkB and TrkC. — Wikipedia
Clinical trial activity
11 trials · 7 clinical orgs · 0 marketing orgs
Phase 1
3
Phase 2
10
Phase 3
1
Phase 4
0
Earliest trial started Jan 1, 2002 (NCT00030186)
Timeline
Indications
Studied for
- Leukemia · Phase 3
- Leukemia, Myeloid · Phase 2
- Leukemia, Myeloid, Acute · Phase 2
- Multiple Myeloma · Phase 2
- Neuroblastoma · Phase 1
- Polycythemia Vera · Phase 2
- Precursor B-Cell Lymphoblastic Leukemia-Lymphoma · Phase 3
- Precursor Cell Lymphoblastic Leukemia-Lymphoma · Phase 3
- Primary Myelofibrosis · Phase 2
- Prostatic Neoplasms · Phase 2
- Psoriasis · Phase 2
- Thrombocythemia, Essential · Phase 1/Phase 2
- Thrombocytosis · Phase 2
Mechanism of action
- Tyrosine-protein kinase JAK2INHIBITOR
JAK2 inhibitor
FLT3 inhibitor
- Tyrosine-protein kinase receptor RETINHIBITOR
RET inhibitor
- Nerve growth factor receptor Trk-AINHIBITOR
NTRK1 inhibitor
NTRK2 inhibitor
- NT-3 growth factor receptorINHIBITOR
NTRK3 inhibitor
Chemistry & pharmacology
Loading structure…
SMILES
C[C@]12O[C@H](C[C@]1(O)CO)n1c3ccccc3c3c4c(c5c6ccccc6n2c5c31)CNC4=O- Mol. weight
- 439.47 g/mol
- Lipinski Ro5
- Pass
- Rule of 3
- No
- Chirality
- Single Stereoisomer
- Inorganic
- No
- Polymer
- No
Oral
No
Parenteral
No
Topical
No
Sources
- WikipediaLestaurtinib ↗
- ChEMBLCHEMBL603469 ↗
Also known as
- a-154475
- a-154475
- a-1544750
- a-1544750
- cep701
- cep 701
- cep-701
- cep-701
- cep-701
- cep-701
- kt-555
- kt-555
- kt5555
- kt-5555
- kt-5555
- kt-5555
- lestaurtinib
- lestaurtinib
- lestaurtinib
- lestaurtinib
- sp924
- sp924
- sp-924
- sp-924
- spm-924
- spm-924
Clinical trials
| NCT ID | Phase | Start date | Sponsor(s) |
|---|---|---|---|
| NCT00668421 | Phase 1/Phase 2 (Phase 2) | Apr 1, 2008 | Icahn School of Medicine at Mount Sinai, Myeloproliferative Disorders Research Consoritum, National Cancer Institute (NCI) |
| NCT00557193 | Phase 3 | Jan 1, 2008 | National Cancer Institute (NCI) |
| NCT00586651 | Phase 2 | Dec 1, 2007 | Cephalon |
| NCT00469859 | Phase 1/Phase 2 (Phase 2) | Jun 1, 2007 | Johns Hopkins University, National Cancer Institute (NCI) |
| NCT00494585 | Phase 2 | Jun 1, 2007 | Cephalon, University of Texas at Houston |
| NCT00242827 | Phase 2 | Apr 1, 2006 | Cephalon |
| NCT00236119 | Phase 2 | Jun 1, 2005 | Cephalon |
| NCT00081601 | Phase 2 | Mar 1, 2004 | Cephalon |
| NCT00079482 | Phase 2 | Oct 1, 2003 | Cephalon |
| NCT00084422 | Phase 1 | Aug 1, 2003 | National Cancer Institute (NCI), University of Pennsylvania |
| NCT00030186 | Phase 2 | Jan 1, 2002 | Cephalon |
Showing 11 of 11 trials
Page 1 / 1
Organizations
Research & Development (7)
| Organization | Org type | Trials | As lead sponsor | Phases | Earliest year |
|---|---|---|---|---|---|
| Cephalon | For profit | 7 | 6 | 1 | 2002 |
| National Cancer Institute (NCI) | Government | 4 | 3 | 3 | 2003 |
| Icahn School of Medicine at Mount Sinai | Academic/Hospital | 1 | 1 | 1 | 2008 |
| Johns Hopkins University | Academic/Hospital | 1 | 0 | 1 | 2007 |
| Myeloproliferative Disorders Research Consoritum | Academic/Hospital | 1 | 0 | 1 | 2008 |
| University of Pennsylvania | Academic/Hospital | 1 | 0 | 1 | 2003 |
| University of Texas at Houston | Academic/Hospital | 1 | 1 | 1 | 2007 |
7 organizations
Page 1 / 1