Therapy Detail

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Therapy Name Lestaurtinib
Synonyms
Therapy Description

Lestaurtinib (CEP-701) inhibits JAK2, FLT3 and NTRK1-3, resulting in antiproliferative activity (PMID: 10415871, PMID: 17143529, PMID: 17442779, PMID: 17984313, PMID: 32441887).

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Lestaurtinib CEP-701|KT-5555|A-154475|SP924 CSF1R Inhibitor 28 FLT3 Inhibitor 66 JAK2 Inhibitor - ATP competitive 15 Trk Receptor Inhibitor (Pan) 31 Lestaurtinib (CEP-701) inhibits JAK2, FLT3 and NTRK1-3, resulting in antiproliferative activity (PMID: 10415871, PMID: 17143529, PMID: 17442779, PMID: 17984313, PMID: 32441887).

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Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FLT3 exon 14 ins FLT3 D839G hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 D839G in culture (PMID: 34768286). 34768286
FLT3 I836T hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 I836T in culture (PMID: 28077790). 28077790
FLT3 I836D FLT3 I836L hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 I836D and I836L in culture (PMID: 28077790). 28077790
FLT3 exon 14 ins FLT3 Y842C acute myeloid leukemia sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring a FLT3 internal tandem duplication and expressing FLT3 Y842C demonstrated sensitivity to Lestaurtinib (CEP-701) in culture (Blood 2009 114:3776). detail...
FLT3 exon 14 ins FLT3 D835V hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 D835V in culture (PMID: 34768286). 34768286
FLT3 D835N hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 D835N in culture (PMID: 28077790). 28077790
FLT3 Y572del hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) decreased proliferation in transformed cells expressing FLT3 Y572del in culture (PMID: 33914060). 33914060
JAK2 V617F JAK2 M929I hematologic cancer predicted - sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing the JAK2 V617F and JAK2 M929I double mutation were sensitive to treatment with Lestaurtinib (CEP-701) in culture, demonstrating growth inhibition (PMID: 21926964). 21926964
FLT3 Q575del hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) decreased downstream signaling and proliferation in transformed cells expressing FLT3 Q575del in culture (PMID: 33914060). 33914060
FLT3 exon 14 ins FLT3 F621L acute myeloid leukemia sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring a FLT3 internal tandem duplication (ITD) and expressing FLT3 F621L demonstrated sensitivity to Lestaurtinib (CEP-701) in culture (Blood 2009 114:3776). detail...
FLT3 exon 14 ins FLT3 Y842H hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 Y842H in culture (PMID: 34768286). 34768286
FLT3 D835A hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 D835A in culture (PMID: 28077790). 28077790
FLT3 D835G hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 D835G in culture (PMID: 28077790). 28077790
JAK2 V617F JAK2 G935R hematologic cancer resistant Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing the JAK2 V617F and JAK2 G935R double mutation demonstrated resistance to Lestaurtinib (CEP-701) in culture (PMID: 21926964). 21926964
FLT3 I836S hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 I836S in culture (PMID: 28077790). 28077790
JAK2 V617F JAK2 E985K hematologic cancer resistant Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing the JAK2 V617F and JAK2 E985K double mutation demonstrated resistance to Lestaurtinib (CEP-701) in culture (PMID: 21926964). 21926964
FLT3 S574del hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) decreased proliferation in transformed cells expressing FLT3 S574del in culture (PMID: 33914060). 33914060
FLT3 D835K FLT3 D835L hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) inhibited Flt3 autophosphorylation and viability in transformed cells expressing FLT3 D835L and D835K in culture (PMID: 28077790). 28077790
FLT3 exon 14 ins FLT3 F691L hematologic cancer resistant Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3-ITD and FLT3 F691L demonstrated resistance to Lestaurtinib (CEP-701) in culture (PMID: 34768286). 34768286
FLT3 exon 14 ins FLT3 F691L acute myeloid leukemia decreased response Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring a FLT3 internal tandem duplication and expressing FLT3 F691L demonstrated a decreased response to Lestaurtinib (CEP-701) compared to treated cells harboring a FLT3 ITD and expressing FLT3 Y842C (Blood 2009 114:3776). detail...
JAK2 V617F JAK2 Y931C hematologic cancer resistant Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, cells expressing the JAK2 V617F and JAK2 Y931C double mutation demonstrated resistance to Lestaurtinib (CEP-701) in culture (PMID: 21926964). 21926964
FLT3 exon 14 ins FLT3 D835Y hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 D835Y in culture (PMID: 34768286). 34768286
FLT3 E573del hematologic cancer sensitive Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, Lestaurtinib (CEP-701) decreased proliferation in transformed cells expressing FLT3 E573del in culture (PMID: 33914060). 33914060
JAK2 V617F JAK2 R938L hematologic cancer resistant Lestaurtinib Preclinical Actionable In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 R938L double mutation demonstrated resistance to Lestaurtinib (CEP-701) in culture (PMID: 21926964). 21926964
FLT3 exon 14 ins FLT3 A627P hematologic cancer resistant Lestaurtinib Preclinical - Cell culture Actionable In a preclinical study, transformed hematologic cells co-expressing FLT3 ITD and FLT3 A627P were resistant to treatment with Lestaurtinib (CEP-701) in culture (PMID: 22858906). 22858906
JAK2 V617F JAK2 I960V hematologic cancer resistant Lestaurtinib Preclinical Actionable In a preclinical study, immune cells expressing the JAK2 V617F and JAK2 I960V double mutation demonstrated resistance to Lestaurtinib (CEP-701) in culture (PMID: 21926964). 21926964

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Clinical Trial Phase Therapies Title Recruitment Status Covered Countries Other Countries


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