Table 1.
FLT3 inhibitors in clinical development
| Tandutinib | Lestaurtinib | Sorafenib | Midostaurin | Quizartinib | Gilteritinib | Crenolanib | FF‐10101 | |
|---|---|---|---|---|---|---|---|---|
| FLT3 kinase inhibition IC50 (nmol/L) | 220 | 3 | 58 | 6.3 | 1.6 | 0.29 | 1.3 | 0.2 |
| Plasma/Medium ratios of GI50 values in FLT3‐ITD‐expressing‐cells | Unknown | 350 | 88.3 | 300 | 18 | 22.8 | 20.5 | 26.2 |
| Growth inhibition to Wt‐FLT3 and ITD‐FLT3‐co–expressing‐32D GI50 (nmol/L) | ||||||||
| FL (0 ng/mL) | Unknown | 9.7 | 5.3 | 20.3 | 1.4 | 8.9 | 23.4 | 1.4 |
| FL (10 ng/mL) | Unknown | 9.2 | 16.0 | 22.7 | 6.5 | 36.4 | 43.5 | 7.5 |
| Inhibitory type | Type II | Type I | Type II | Type I | Type II | Type I | Type I | Type I (Covalent) |
| Other targets |
PDGFR KIT |
TRKA PKC KDR PDGFR |
RAF VEGFR PDGFR KIT |
PKC KDR KIT PDGFR |
KIT |
AXL LTK ALK |
KIT PDGFR RET |
FMS |
| Development stage for AML | Withdrawn | Phase 2 | Phase 3 | Approved as combination with chemo for AML | Approved as single agent for R/R AML | Approved as single agent for R/R AML | Phase 3 | Phase 1/2a |