Table 1.

List of BCR-ABL1 KD mutations poorly sensitive to imatinib, dasatinib, nilotinib, bosutinib, and ponatinib based on the integration of published studies (2001–2018) reporting the mutation status of TKI-resistant patients and experimental data

Mutations poorly sensitive to imatinib	M237V, I242T, M244 V, K247R, L248V, G250E, G250R, Q252R, Q252H, Y253F, Y253H, E255K, E255V, E258D, W261L, L273M, E275K, E275Q, D276G, T277A, E279K, V280A, V289I, V289I, V289A, E292Q, E292V, I293V, L298V, F311L, F311I, T315I, F317L, F317V, F317I, F317C, Y320C, L324Q, Y342H, M343T, A344V, A350V, M351T, E355D, E355G, E355A, F359V, F359I, F359C, F359L, D363Y, L364I, A365V, A366G, L370P, V371A, E373K, V379I, A380T, F382L, L384M, L387F, L387V, M388L, H396R, H396P, H396A, A397P, S417F, S417Y, I418S, I418V, A433T, S438C, E450K, E450G, E450A, E450V, E453G, E453A, E453K, E453V, E453Q, E459K, E459V, E459G, E459Q, M472I, P480L, F486S
Mutations poorly sensitive to dasatinib	V299L, T315I, T315A, F317L, F317V, F317I, F317C
Mutations poorly sensitive to nilotinib	Y253H, E255K, E255V, T315I, F359V, F359I, F359C
Mutations poorly sensitive to bosutiniba	E255V, E255K, V299L, T315I
Mutations poorly sensitive to ponatinib	T315M, T315L

^aIn contrast to the other second-generation TKIs, there is still limited data available on mutations associated with clinical resistance to bosutinib in vivo. In vitro data suggest that the E255K and, to a lesser extent, the E255V might be poorly sensitive to bosutinib [15]

TKI tyrosine kinase inhibitor

The most frequent imatinib-resistant mutations are highlighted in boldface