Table 2.
Drug | Type I or II inhibitor | Active as monotherapy | Cellular potency | Selectivity | Half-life | Protein binding (%) | Clinical resistance mechanisms | FDA-approved | FDA approved for AML indication |
---|---|---|---|---|---|---|---|---|---|
Midostaurin | I | No | ++ | + | 19 h | >99.8 | One reported case of an acquired FLT KD mutation (N676K41) | Yes, in combination with induction chemotherapy only | Yes |
Sorafenib | II | Yes | ++ | ++ | 25-48 h | 99.5 | FLT3 KD mutations (D835, F691L13,25) | Yes | No |
Quizartinib | II | Yes | +++ | +++ | ∼1.5 d | >99 | FLT3 KD mutations (D835, F691L)16 | No | Development ongoing |
Crenolanib | I | Yes | ++ | ++ | 6-8 h | 95.9 | F691L, Ras pathway mutations30 | No | Development ongoing |
Gilteritinib | I | Yes | ++ | ++ | 113 h | ∼94 | F691L, Ras pathway mutations31 | Yes | Yes |