Crenolanib is active against models of drug-resistant FLT3-ITD−positive acute myeloid leukemia
Open Access
- 21 November 2013
- journal article
- Published by American Society of Hematology in Blood
- Vol. 122 (22), 3607-3615
- https://doi.org/10.1182/blood-2013-07-513044
Abstract
Key Points The tyrosine kinase inhibitor crenolanib has type 1 inhibitor properties and has potent activity against FLT3-activating mutations. Crenolanib is active in vitro and in vivo against FLT3 inhibitor-resistant FLT3-ITD/D835 mutations.Keywords
This publication has 33 references indexed in Scilit:
- Synergistic growth-inhibitory effects of ponatinib and midostaurin (PKC412) on neoplastic mast cells carrying KIT D816VHaematologica, 2013
- Validation of ITD mutations in FLT3 as a therapeutic target in human acute myeloid leukaemiaNature, 2012
- Selective FLT3 inhibition of FLT3-ITD+ acute myeloid leukaemia resulting in secondary D835Y mutation: a model for emerging clinical resistance patternsLeukemia, 2012
- Activity of the Multikinase Inhibitor Sorafenib in Combination With Cytarabine in Acute Myeloid LeukemiaJNCI Journal of the National Cancer Institute, 2011
- Antileukemic Effects of Novel First- and Second-Generation FLT3 Inhibitors: Structure-Affinity ComparisonGenes & Cancer, 2010
- Imatinib Upregulates Compensatory Integrin Signaling in a Mouse Model of Gastrointestinal Stromal Tumor and Is More Effective When Combined with DasatinibMolecular Cancer Research, 2010
- Phase I Study of the Safety, Tolerability, and Pharmacokinetics of Oral CP-868,596, a Highly Specific Platelet-Derived Growth Factor Receptor Tyrosine Kinase Inhibitor in Patients With Advanced CancersJournal of Clinical Oncology, 2009
- AC220 is a uniquely potent and selective inhibitor of FLT3 for the treatment of acute myeloid leukemia (AML)Blood, 2009
- KIT kinase mutants show unique mechanisms of drug resistance to imatinib and sunitinib in gastrointestinal stromal tumor patientsProceedings of the National Academy of Sciences, 2009
- Comparison of imatinib mesylate, dasatinib (BMS-354825), and nilotinib (AMN107) in an N-ethyl-N-nitrosourea (ENU)–based mutagenesis screen: high efficacy of drug combinationsBlood, 2006