Table 1.
A comprehensive overview of first-generation FLT3 inhibitors utilized in clinical trials for AML treatment.
| Drug | Targeted Mutation | Study (Ref.) | Usage | Benefit | |
|---|---|---|---|---|---|
| Front-line therapy | Midostaurin | FLT3-ITD/TKD | RATIFY (phase III) [30] |
Standard of care “3 + 7” + Midostaurin | OS: 74.7 vs. 25.6 mo |
| FLT3 | - | In combination with Azacitidine (not eligible for IC) | OS: 22 wks | ||
| Sorafenib | FLT3-ITD | NCT02196857 (phase II) and NCT01254890 (phase I/II) [31] | In combination with Azacitidine (not eligible for IC) |
OS: 8.3 mo | |
| FLT3 | SORAML (phase II) [32] | Standard of care “3 + 7” + Sorafenib | EFS: 21 vs. 9 mo | ||
| Lestauritinib | FLT3 | - | Various intensive TX | OS: 46% vs. 45% | |
| Relapsed/refractory disease | Midostaurin | FLT3 | NCT00045942 (phase II b) [33] | Monotherapy | OS: 130 d |
| Maintenance post-HCT | Sorafenib | FLT3-ITD | SORMAIN (phase II) [34] | Monotherapy | 55 OS: NR |
| Midostaurin | FLT3-ITD | RADIUS (phase II) [35] | Monotherapy | 22 OS: NR |
Abbreviations: FLT3, FMS- like tyrosine kinase; ITD, internal tandem duplication; TKD, tyrosine kinase domain; HCT, hematopoietic cell transplantation; OS, overall survival; IC, intensive chemotherapy; mo, months; NR, not reached.