Therapy Detail

Therapy Name Lestaurtinib
Synonym
Therapy Description

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

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Lestaurtinib CEP-701 CSF1R Inhibitor 23 FLT3 Inhibitor 50 JAK2 Inhibitor - ATP competitive 14 Trk Receptor Inhibitor (Pan) 23 Lestaurtinib (CEP-701) inhibits JAK2, FLT3 and NTRK1-3, resulting in antiproliferative activity (PMID: 17143529, PMID: 17442779, PMID: 17984313).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
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 lestauranib in culture (PMID: 21926964). 21926964
ETV6-NTRK3 Advanced Solid Tumor sensitive Lestaurtinib Preclinical Actionable In a preclinical study, transformed cells expressing the fusion, ETV6-NTRK3, were treated with Lestaurtinib (CEP-701), which resulted in inhibition of ETV6-NTRK3 autophosphorylation and restoration of Tgf-b1 signaling (PMID: 16258068). 16258068
Unknown unknown pancreatic ductal adenocarcinoma not applicable Lestaurtinib Preclinical Actionable In preclinical studies, lestaurtinib has been shown to have an antitumor effect in xenograft models of pancreatic ductal adenocarcinoma (PMID: 10473107). 10473107
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...
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...
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 Lestauranib in culture (PMID: 21926964). 21926964
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...
Clinical Trial Phase Therapies Title Recruitment Status