Description: Lesraurtinib, also known as CEP701; KT 5555; SP 924, is an orally bioavailable indolocarbazole derivative with antineoplastic properties. Lestaurtinib inhibits autophosphorylation of FMS-like tyrosine kinase 3 (FLT3), resulting in inhibition of FLT3 activity and induction of apoptosis in tumor cells that overexpress FLT3.
Synonym: CEP701; CEP-701; CEP 701; KT5555; KT-5555; KT 5555; SP924; SP-924; SP 924. Lestaurtinib.
IUPAC/Chemical 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
PRICE AND AVAILABILITY
Chemical Formula: C26H21N3O4
Exact Mass: 439.15321
Molecular Weight: 439.46
Elemental Analysis: C, 71.06; H, 4.82; N, 9.56; O, 14.56
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, JAK2, TrkA, TrkB and TrkC. It is undergoing research for the treatment of acute myelogenous leukemia (AML) and myeloproliferative disorders. As of 2008, it was in Phase III clinical trials for AML and Phase II clinical trials for myeloproliferative disorders。
On 20 Jun 2009, Cephalon, Inc. announced results from a pivotal clinical trial of lestaurtinib (CEP-701) in patients with relapsed acute myelogenous leukemia (AML) expressing FLT3 activating mutations. The study was designed to show the benefit of lestaurtinib in this patient population when given in sequence with standard induction chemotherapy compared to those treated with standard induction chemotherapy alone. An analysis of the study showed that patients who were treated with lestaurtinib showed similar rates of complete response but no increased benefit in overall survival, compared to those who received induction chemotherapy alone.
“We are disappointed that this study with lestaurtinib did not demonstrate a benefit for this patient population but we remain committed to oncology clinical research and developing innovative therapies for life-threatening diseases,” said Dr. Lesley Russell, Executive Vice President and Chief Medical Officer at Cephalon. For detail, see: medicinalnewstoday.com..
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