Crenolanib is a second-generation, type I tyrosine kinase inhibitor with activity against FLT3 (reviewed in Daver et al, 2019; Lim et al, 2017). It is currently in phase III clinical trials for treatment of FLT3-positive AML. The following FLT3 mutants are resistant to crenolanib-mediated inhibition:FLT3 F691L (Galanis et al, 2014)FLT3 D835H (Galanis et al, 2014)
Schlenk, RF, Levis, MJ, Daver, N, Russell, NH
Dubielecka, PM, Lim, SH, Raghunathan, VM
Levis, M, Small, D, Cortes, J, Ramachandran, A, Galanis, A, Rajkhowa, T, Ma, H
Loss of function of crenolanib-resistant FLT3 mutants [plasma membrane]
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