Lestaurtinib

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Lestaurtinib


Clinical data
Pregnancy cat.	?
Legal status	?
Identifiers
ATC code	None
PubChem	CID 126565
UNII	DO989GC5D1^N
KEGG	D04696^Y
ChEMBL	CHEMBL603469^N
Chemical data
Formula	C₂₆H₂₁N₃O₄
Mol. 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^[update], it is in Phase II clinical trials for AML and Phase II clinical trials for myeloproliferative disorders.^[4]^[5]

See also [edit]

Janus kinase inhibitor

References [edit]

^ 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".
^ "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 Pazopanib Regorafenib Semaxanib Sorafenib Sunitinib Toceranib Vandetanib)

Non-receptor	bcr-abl (Imatinib Dasatinib Nilotinib Ponatinib) Src (Bosutinib) Janus kinase (Lestaurtinib Ruxolitinib) EML4-ALK (Crizotinib) RET inhibitors: Vandetanib (Also VEGFR and EGFR). c-MET inhibitor: Cabozantinib (Also VEGFR2).

Other

fusion protein against VEGF (Aflibercept)
proapoptotic peptide against ANXA2 and prohibitin (Adipotide)
exotoxin against IL-2 (Denileukin diftitox)
mTOR inhibitors (Everolimus
Temsirolimus)

tumr, epon, para

drug (L1i/1e/V03)

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