Lestaurtinib

Lestaurtinib
Systematic (IUPAC) name


(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
Identifiers
ATC code	None
PubChem	CID 126565
IUPHAR/BPS	5672
ChemSpider	112457
UNII	DO989GC5D1^N
KEGG	D04696^Y
ChEMBL	CHEMBL603469^N
Chemical data
Formula	C₂₆H₂₁N₃O₄
Molar mass	439.462 g/mol
SMILES C[C@@]12[C@](C[C@@H](O1)n3c4ccccc4c5c3c6n2c7ccccc7c6c8c5C(=O)NC8)(CO)O
InChI 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 Key:UIARLYUEJFELEN-LROUJFHJSA-N
^NY (what is this?) (verify)

Lestaurtinib (rINN, codenamed CEP-701) is a tyrosine kinase inhibitor structurally related to staurosporine. It was investigated by Cephalon as a treatment for various types of cancer. It is an inhibitor of the kinases FLT3,^[1] JAK2,^[2] TrkA, TrkB and TrkC.^[3]

Uses

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

Clinical trials

In 2009, it was in Phase II clinical trials for AML and Phase II clinical trials for myeloproliferative disorders.^[4]^[5]

References

↑ 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.
↑ 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.
↑ 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.
↑ "Oncology pipeline Oct 2009" (PDF).
↑ "Trials of Lestaurinib".

Targeted therapy / extracellular chemotherapeutic agents/antineoplastic agents (L01)

CI monoclonal antibodies ("-mab")

Receptor tyrosine kinase	ErbB: HER1/EGFR (Cetuximab Panitumumab) HER2/neu (Trastuzumab Trastuzumab emtansine)

Others for solid tumors	EpCAM (Catumaxomab Edrecolomab) VEGF-A (Bevacizumab)

Leukemia/lymphoma	lymphoid: CD20 (Ibritumomab Ofatumumab Rituximab Tositumomab), CD30 (Brentuximab), CD52 (Alemtuzumab) myeloid: CD33 (Gemtuzumab)

Tyrosine-kinase inhibitors ("-nib")

Receptor tyrosine kinase	ErbB: HER1/EGFR (Erlotinib Gefitinib Vandetanib) HER1/EGFR and HER2/neu (Afatinib Lapatinib Neratinib) RTK class III: C-kit and PDGFR (Axitinib Masitinib Pazopanib Sunitinib Sorafenib Toceranib) FLT3 (Lestaurtinib) VEGFR (Axitinib Cediranib Lenvatinib Nintedanib Pazopanib Regorafenib Semaxanib Sorafenib Sunitinib Tivozanib Toceranib Vandetanib) RET inhibitors: Vandetanib (Also VEGFR and EGFR). c-MET inhibitor: Cabozantinib (Also VEGFR2).

Non-receptor	bcr-abl (Imatinib Dasatinib Nilotinib Ponatinib) Src (Bosutinib) Janus kinase (Lestaurtinib Ruxolitinib Pacritinib) MAP2K (Cobimetinib Selumetinib Trametinib Binimetinib) EML4-ALK (Ceritinib Crizotinib) Bruton's (Ibrutinib)

Other

fusion protein against VEGF (Aflibercept)
proapoptotic peptide against ANXA2 and prohibitin (Adipotide)
exotoxin against IL-2 (Denileukin diftitox)
mTOR inhibitors
- Everolimus
- Temsirolimus
hedgehog inhibitors
- Sonidegib
- Vismodegib
CDK inhibitor (Palbociclib)

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Lestaurtinib

Uses

Clinical trials

See also

References