title: FLT3 Inhibitors for Treating Acute Myeloid Leukemia.
abstract: FLT3 (Fms-like tyrosine kinase 3) inhibitors are tyrosine kinase inhibitors. The first-generation FLT3 inhibitors were developed several years ago and include midostaurin, lestaurtinib, sunitinib, and sorafenib. They are relatively nonspecific for FLT3, with other potential targets that include platelet-derived growth factor receptor, vascular endothelial growth factor receptor, KIT, and Janus kinase 2. The second-generation inhibitors, including quizartinib, crenolanib, PLX3397, and ASP2215, are more potent and selective than the first-generation inhibitors. The greater potency and selectivity promises greater efficacy in FLT3-mutated acute myelogenous leukemia (AML) (particularly in patients with a greater allele burden) and less toxicity. A number of receptor tyrosine kinase inhibitors are being studied across virtually all disease settings, including frontline, relapsed and refractory, and maintenance, mainly in patients with FLT3-mutated AML. The future of FLT3 inhibitors in the treatment of AML, in combination with chemotherapy or stem cell transplant, appears bright. The present report reviews the current data on FLT3 inhibitors.
authors.affiliation: King Faisal Specialist Hospital and Research Center Riadh, Riadh, Saudi Arabia.
authors.forename: Mona
authors.initials: M
authors.lastname: Hassanein
authors.affiliation: King Faisal Specialist Hospital and Research Center Riadh, Riadh, Saudi Arabia.
authors.forename: Muhamad H
authors.initials: MH
authors.lastname: Almahayni
authors.affiliation: King Faisal Specialist Hospital and Research Center Riadh, Riadh, Saudi Arabia.
authors.forename: Syed O
authors.initials: SO
authors.lastname: Ahmed
authors.affiliation: MD Anderson Cancer Center, Houston, TX.
authors.forename: Sameh
authors.initials: S
authors.lastname: Gaballa
authors.affiliation: King Faisal Specialist Hospital and Research Center Riadh, Riadh, Saudi Arabia. Electronic address: riadfakih@hotmail.com.
authors.forename: Riad
authors.initials: R
authors.lastname: El Fakih
mesh_terms: D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use*; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000627:therapeutic use; D002986:Clinical Trials as Topic; D019008:Drug Resistance, Neoplasm; D020440:Gene Duplication; D018380:Hematopoietic Stem Cell Transplantation; D006801:Humans; D015470:Leukemia, Myeloid, Acute / Q000188:drug therapy* / Q000235:genetics / Q000378:metabolism / Q000401:mortality; D009154:Mutation; D047428:Protein Kinase Inhibitors / Q000494:pharmacology / Q000627:therapeutic use*; D020080:Tandem Repeat Sequences; D016896:Treatment Outcome; D051941:fms-Like Tyrosine Kinase 3 / Q000037:antagonists & inhibitors* / Q000235:genetics / Q000378:metabolism
chemical_list: D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D051941:fms-Like Tyrosine Kinase 3
keywords: Acute myelogenous leukemia; Fms-like tyrosine kinase 3; Internal tandem duplication; Sorafenib; Tyrosine kinase inhibitors