Table 3. FLT3 inhibitors in clinical... | American Society of Hematology

Table 3.

FLT3 inhibitors in clinical development

Tyrosine kinase inhibitor	Class	Receptor activity*	FLT3 IC₅₀†	Clinical trials	Toxicity
PKC412^94,95,97,113	Benzoylstaurosporine	PKC	528 nM	Phase 2: AML with/without FLT3-ITD	Nausea, emesis, fatigue
		PDGFR
		KDR
		KIT
		FLT3
		ABL
CEP-701^98-102	Indolocarbazole	FLT3	2-3 nM	Phase 2: AML with FLT3-ITD	Nausea, emesis, fatigue
		TRKA
		KDR
		PKC
		PDGFR
		EGFR
CT35318^103-105	Piperazinyl quinazoline	KIT	170-220 nM	Phase 1: AML/MDS with/without FLT3-ITD	Generalized weakness, fatigue, nausea, vomiting
		PDGFR
		FLT3		Phase 2: AML with FLT3-ITD
		FMS
SU5416^106-109	Indolinone	FLT3	250 nM	Phase 2: Refractory AML/MDS/MPD/MM	Fatigue, nausea, sepsis, bone pain
		KDR
		KIT		Phase 2: Refractory AML (c-KIT⁺)
SU11248^110,111	Indolinone	FLT3	10 nM	Phase 1: AML	Nausea, fatigue, cardiac dysfunction‡
		KDR
		PDGFR

Tyrosine kinase inhibitor	Class	Receptor activity*	FLT3 IC₅₀†	Clinical trials	Toxicity
PKC412^94,95,97,113	Benzoylstaurosporine	PKC	528 nM	Phase 2: AML with/without FLT3-ITD	Nausea, emesis, fatigue
		PDGFR
		KDR
		KIT
		FLT3
		ABL
CEP-701^98-102	Indolocarbazole	FLT3	2-3 nM	Phase 2: AML with FLT3-ITD	Nausea, emesis, fatigue
		TRKA
		KDR
		PKC
		PDGFR
		EGFR
CT35318^103-105	Piperazinyl quinazoline	KIT	170-220 nM	Phase 1: AML/MDS with/without FLT3-ITD	Generalized weakness, fatigue, nausea, vomiting
		PDGFR
		FLT3		Phase 2: AML with FLT3-ITD
		FMS
SU5416^106-109	Indolinone	FLT3	250 nM	Phase 2: Refractory AML/MDS/MPD/MM	Fatigue, nausea, sepsis, bone pain
		KDR
		KIT		Phase 2: Refractory AML (c-KIT⁺)
SU11248^110,111	Indolinone	FLT3	10 nM	Phase 1: AML	Nausea, fatigue, cardiac dysfunction‡
		KDR
		PDGFR

MM indicates multiple myeloma.

Receptor activity in descending order of potency.

FLT3 autophosphorylation in vitro.

Cardiac toxicity observed in AML patients with prior anthracycline use.