Radotinib

Radotinib is a selective second generation tyrosine kinase inhibitor that targets both the wild-type and mutant forms of Bcr-Abl, with an IC₅₀ value of 30.6 nM in Ba/F3 human chronic myeloid leukemia cells expressing the wild-type form.¹ Radotinib also inhibits platelet-derived growth factor receptors (PDGFRs) α and β with IC₅₀ values of 75.5 and 130 nM, respectively.^2,3 Binding of radotinib to Bcr-Abl in vitro inhibits the phosphorylation of the downstream signaling mediator CrkL.³ In acute myeloid leukemia cells, in vitro treatment with radotinib at doses of 10-100 µM reduces viability, activates the mitochondrial apoptosis pathway, and promotes expression of the differentiation marker CD11b.²

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1. Zabriskie, M.S., Vellore, N.A., Gantz, K.C., et al. Radotinib is an effective inhibitor of native and kinase domain-mutant BCR-ABL1. Leukemia 29(9), 1939-1942 (2015).

2. Heo, S.-K., Noh, E.-K., Yoon, D.-J., et al. Radotinib induces apoptosis of CD11b+ cells differentiated from acute myeloid leukemia cells. PLoS One 10(6), e0129853 (2015).

3. Kim, S.-H., Menon, H., Jootar, S., et al. Efficacy and safety of radotinib in chronic phase chronic myeloid leukemia patients with resistance or intolerance to BCR-ABL1 tyrosine kinase inhibitors. Haematologica 99(7), 1191-1196 (2014).