Lestaurtinib

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Lestaurtinib
Lestaurtinib.png
Identifiers
CAS Registry Number  YesY
ATC code None
PubChem CID: 126565
IUPHAR/BPS 5672
UNII DO989GC5D1 N
KEGG D04696 YesY
ChEMBL CHEMBL603469 N
Chemical data
Formula C26H21N3O4
Molecular mass 439.462 g/mol
 N (what is this?)  (verify)

Lestaurtinib (rINN, codenamed CEP-701) is a tyrosine kinase inhibitor structurally related to staurosporine, and is being developed by Cephalon.

It is an inhibitor of FLT3,[1] JAK2,[2] TrkA, TrkB and TrkC.[3]

Uses[edit]

It is undergoing research for the treatment of acute myelogenous leukemia (AML) and myeloproliferative disorders.

As of 2009, it is in Phase II clinical trials for AML and Phase II clinical trials for myeloproliferative disorders.[4][5]

See also[edit]

References[edit]

  1. ^ Knapper S, Burnett AK, Littlewood T et al. (November 2006). "A phase 2 trial of the FLT3 inhibitor lestaurtinib (CEP701) as first-line treatment for older patients with acute myeloid leukemia not considered fit for intensive chemotherapy". Blood 108 (10): 3262–70. doi:10.1182/blood-2006-04-015560. PMID 16857985. 
  2. ^ Hexner EO, Serdikoff C, Jan M et al. (June 2008). "Lestaurtinib (CEP701) is a JAK2 inhibitor that suppresses JAK2/STAT5 signaling and the proliferation of primary erythroid cells from patients with myeloproliferative disorders". Blood 111 (12): 5663–71. doi:10.1182/blood-2007-04-083402. PMC 2424161. PMID 17984313. 
  3. ^ Revill, P., Serradell, N., Bolos, J., Rosa, E. (2007). "Lestaurtinib". Drugs of the Future 32 (3): 215. doi:10.1358/dof.2007.032.03.1084137. 
  4. ^ "Oncology pipeline Oct 2009" (PDF). 
  5. ^ "Trials of Lestaurinib".