Table 1.
Mutations associated with resistance to FLT3 inhibitors.
FLT3 Inhibitor | Class, Type | Mutation/Amino Acid Change | Tyrosine Kinase Domain |
---|---|---|---|
PKC412 (Midostaurin) | First generation; Type 1 | N676K [24] 672E [23] N676D [25,142] F691L, G697R [25] N676I, N676S, F691I [142] |
TKD1 |
Sunitinib | First generation; Type 1 | A627P, F691L [33] D835Y [31] Y842C [33] |
TKD1 TKD2 |
Lestaurtinib | First generation; Type 1 | A627P [33] | TKD1 |
Sorafenib | First generation; Type 2 | F691L [31,33,142] A627P [33] D835H [31,143] D835V/F/I/del/Y/A [143] F691I, Y842N [142] Y842C [33] |
TKD1 TKD2 |
Tandutinib | First generation; Type 2 | D835Y [144] | TKD2 |
Quizartinib | Second generation; Type 2 | F691L [31,33,73] A627P [33] D835V/F/I/del/Y [31,73,143] D835H [31] Y842C/H [73] |
TKD1 TKD2 |
Gilteritinib | Second generation, Type 1 | F961L [145,146] | TKD1 |
Crenolanib | Second generation, Type 1 | F691L [147] | TKD1 |