Lestaurtinib

Lestaurtinib
Clinical data
Routes of
administration		By mouth[1]
ATC code
  • None
Pharmacokinetic data
Protein bindinghighly protein-bound, especially to α-1 acid glycoprotein[1]
Metabolismliver P450 (CYP34A) enzyme system[1]
Identifiers
  • (5S,6S,8R)-6-Hydroxy-6-(hydroxymethyl)-5-methyl-7,8,14,15-tetrahydro-5H-16-oxa-4b,8a,14-triaza-5,8-methanodibenzo[b,h]cycloocta[jkl]cyclopenta[e]-as-indacen-13(6H)-one
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
KEGG
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC26H21N3O4
Molar mass439.471 g·mol−1
3D model (JSmol)
  • C[C@@]12[C@](C[C@@H](O1)n3c4ccccc4c5c3c6n2c7ccccc7c6c8c5C(=O)NC8)(CO)O
  • InChI=1S/C26H21N3O4/c1-25-26(32,12-30)10-18(33-25)28-16-8-4-2-6-13(16)20-21-15(11-27-24(21)31)19-14-7-3-5-9-17(14)29(25)23(19)22(20)28/h2-9,18,30,32H,10-12H2,1H3,(H,27,31)/t18-,25+,26+/m1/s1 ☒N
  • Key:UIARLYUEJFELEN-LROUJFHJSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Lestaurtinib (rINN, codenamed CEP-701) 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.[1] It is an inhibitor of the kinases fms-like tyrosine kinase 3 (FLT3),[2] Janus kinase 2 (JAK2),[3] tropomyosin receptor kinase (trk) A (TrkA), TrkB and TrkC.[4]

  1. ^ a b c d Shabbir M, Stuart R (2010). "Lestaurtinib, a multitargeted tyrosinse kinase inhibitor: from bench to bedside". Expert Opinion on Investigational Drugs. 19 (3): 427–36. doi:10.1517/13543781003598862. PMID 20141349. S2CID 13558158.
  2. ^ 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.
  3. ^ 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.
  4. ^ 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.{{cite journal}}: CS1 maint: multiple names: authors list (link)