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. 2016 Apr 19;7:73–83. doi: 10.2147/JBM.S100283

Table 4.

Selected emerging FLT3 inhibitors

Compound Distinguishing characteristic(s) Selected trials References
Crenolanib (CP-868,596) Active toward all identified resistance-conferring FLT3 kinase domain mutations None published
n progress:
1. Phase II studies of crenolanib as a single agent in relapsed/refractory AML (NCT01522469, NCT01657682)
2. Phase II study of crenolanib + chemo in newly diagnosed AML (NCT02283177)
3. Studies of crenolanib + chemo in relapsed/refractory AML (Phase II: NCT02400281, Phase III: NCT02298166)
4. Phase II study of crenolanib after HSCT (NCT02400255)		 ClinicalTrials.gov38
Gilteritinib (ASP2215) Active toward FLT3 and Axl t1/2>48 hours Favorable toxicity profile Published:
1. Phase I/II trial of single-agent gilteritinib in relapsed/refractory AML
In progress:
1. Phase I study of gilteritinib as a single agent in relapsed/refractory AML (NCT02181660)
2. Phase I studies of gilteritinib + chemo in newly diagnosed AML (NCT02310321, NCT02236013)
3. Phase III study of gilteritinib vs salvage chemo in relapsed/refractory AML (NCT02421939)
4. Phase III study of gilteritinib as post-SCT maintenance therapy in AML (BMT CTN 1506)		 ClinicalTrials.gov37,39
Quizartinib (AC-220) Highly selective for FLT3-ITD
Not active toward FLT3-D835Y
Associated with QTc prolongation in vivo		 Published:
1. Phase I trial of single agent in relapsed/refractory AML
2. Phase II trial of single agent in AML: primary refractory or first relapse
3. Phase II trial of single agent in AML: relapsed or refractory to second line or HSCT
In progress:
1. Phase I/II study of quizartinib+azacitidine in AML or MDS (NCT01892371)
2. Phase III study of quizartinib vs salvage chemotherapy in relapsed/refractory AML (NCT02039726)
3. Phase I study of quizartinib as post-SCT maintenance therapy in AML (NCT01468467)
4. Phase I study of quizartinib in combination with induction and consolidation therapy in AML (NCT01390337)
5. Single-agent quizartinib in relapsed/refractory AML (Phase I: NCT00462761, Phase II: NCT01565668)		 ClinicalTrials.gov21,36,40

Notes: Agents for which development has been suspended or halted are not included (lestaurtinib, sunitinib, tandutinib; per Kiyoi35).

Abbreviations: AML, acute myeloid leukemia; BMT, bone marrow transplant; FLT3, fms-like tyrosine kinase; HSCT, hematopoietic stem cell therapy; ITD, internal tandem duplication; MDS, myelodysplastic syndrome; SCT, stem cell therapy; Chemo, chemotherapy; t1/2, half life; QTc, corrected QT interval; BMT CTN, Blood and Marrow Transplant Clinical Trials Network.