title: Lestaurtinib: a multi-targeted FLT3 inhibitor.
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.
authors.affiliation: Department of Oncology, Division of Hematologic Malignancies, Sidney Kimmel Comprehensive Cancer Center at Johns Hopkins, 1650 Orleans Street, Baltimore, MD 21231, USA.
authors.forename: Amir T
authors.initials: AT
authors.lastname: Fathi
authors.forename: Mark
authors.initials: M
authors.lastname: Levis
mesh_terms: D002227:Carbazoles / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D005663:Furans; D006801:Humans; D015470:Leukemia, Myeloid, Acute / Q000188:drug therapy* / Q000201:enzymology; D047428:Protein Kinase Inhibitors / Q000493:pharmacokinetics / Q000494:pharmacology / Q000627:therapeutic use*; D051941:fms-Like Tyrosine Kinase 3 / Q000037:antagonists & inhibitors* / Q000235:genetics
chemical_list: D002227:Carbazoles; D005663:Furans; D047428:Protein Kinase Inhibitors; C119379:lestaurtinib; D051941:fms-Like Tyrosine Kinase 3