Table 3.
GI50 values of FLT3 inhibitors against mutation types.
| Mutation type | GI50 (nM) [relative ratio to ITD] | |||
|---|---|---|---|---|
| Quizartinib | Sorafenib | Ponatinib | Crenolanib | |
| FLT3/ITD | 0.13 [1] | 1.3 [1] | 3.0 [1] | 1.3 [1] |
| FLT3/ITD+F691L | 102 [785] | 1189 [915] | 52 [17] | 67.8 [52.2] |
| FLT3/ITD+F691I | 122 [938] | 648 [498] | 4.2 [1.4] | – |
| FLT3/ITD+D835V | 120 [923] | 2209 [1699] | 349 [116] | – |
| FLT3/ITD+D835Y | 28 [215] | 675 [519] | 284 [95] | 8.7 [6.7] |
| FLT3/ITD+D835F | 166 [1277] | 2374 [1826] | 414 [138] | – |
| FLT3/ITD+D835H | 5.5 [42] | 164 [126] | 211 [70] | – |
| FLT3/ITD+D839G | 1.9 [15] | 112 [86] | 54 [18] | – |
| FLT3/ITD+Y842C | 33 [254] | 469 [361] | 229 [76] | – |
| FLT3/ITD+Y842H | 18 [138] | 260 [200] | 80 [27] | – |
Several resistant mutations have been acquired after the treatment of quizartinib, and most of them are resistant to sorafenib. However, ponatinib and crenolanib have inhibitory activities against those resistant mutations.