Lestaurtinib: a multi-targeted FLT3 inhibitor
- 1 February 2009
- journal article
- review article
- Published by Taylor & Francis Ltd in Expert Review of Hematology
- Vol. 2 (1), 17-26
- https://doi.org/10.1586/17474086.2.1.17
Abstract
Internal tandem duplication mutations of FMS-like tyrosine kinase-3 (FLT3) have been associated with poor outcomes in acute myelogenous leukemia. Over the course of the last several years, multiple agents have been developed and studied as potential inhibitors of FLT3 with the hope of providing clinical benefit for these patients. Lestaurtinib, a multi-targeted indolocarbazole derivative that potently inhibits FLT3 autophosphorylation in vitro, has been the most extensively studied agent in clinical trials to date. Multiple late-phase trials are underway to study this agent in adult and pediatric leukemia. This article will summarize the historical development of the pharmacology of lestaurtinib, as well as the ongoing investigation of the agent in preclinical and clinical studies.Keywords
This publication has 71 references indexed in Scilit:
- Sorafenib in Advanced Hepatocellular CarcinomaThe New England Journal of Medicine, 2008
- Lapatinib Versus Hormone Therapy in Patients With Advanced Renal Cell Carcinoma: A Randomized Phase III Clinical TrialJournal of Clinical Oncology, 2008
- Sunitinib versus Interferon Alfa in Metastatic Renal-Cell CarcinomaThe New England Journal of Medicine, 2007
- Dasatinib in Imatinib-Resistant Philadelphia Chromosome–Positive LeukemiasThe New England Journal of Medicine, 2006
- Nilotinib in Imatinib-Resistant CML and Philadelphia Chromosome–Positive ALLThe New England Journal of Medicine, 2006
- Erlotinib in Previously Treated Non–Small-Cell Lung CancerThe New England Journal of Medicine, 2005
- Cytogenetics in acute leukemiaBlood Reviews, 2004
- Activating Mutations in the Epidermal Growth Factor Receptor Underlying Responsiveness of Non–Small-Cell Lung Cancer to GefitinibThe New England Journal of Medicine, 2004
- Imatinib Compared with Interferon and Low-Dose Cytarabine for Newly Diagnosed Chronic-Phase Chronic Myeloid LeukemiaThe New England Journal of Medicine, 2003
- Acute Myeloid LeukemiaThe New England Journal of Medicine, 1999