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Ref Type Journal Article
PMID (32040554)
Authors Tarver TC, Hill JE, Rahmat L, Perl AE, Bahceci E, Mori K, Smith CC
Title Gilteritinib is a clinically active FLT3 inhibitor with broad activity against FLT3 kinase domain mutations.
Journal Blood advances
Vol 4
Issue 3
Date 2020 Feb 11
URL
Abstract Text Gilteritinib is the first FMS-like tyrosine kinase 3 (FLT3) tyrosine kinase inhibitor (TKI) approved as monotherapy in acute myeloid leukemia with FLT3 internal tandem duplication and D835/I836 tyrosine kinase domain (TKD) mutations. Sequencing studies in patients have uncovered less common, noncanonical (NC) mutations in FLT3 and have implicated secondary TKD mutations in FLT3 TKI resistance. We report that gilteritinib is active against FLT3 NC and TKI resistance-causing mutations in vitro. A mutagenesis screen identified FLT3 F691L, Y693C/N, and G697S as mutations that confer moderate resistance to gilteritinib in vitro. Analysis of patients treated with gilteritinib revealed that 2/9 patients with preexisting NC FLT3 mutations responded and that secondary TKD mutations are acquired in a minority (5/31) of patients treated with gilteritinib. Four of 5 patients developed F691L mutations (all treated at <200 mg). These studies suggest that gilteritinib has broad activity against FLT3 mutations and limited vulnerability to resistance-causing FLT3 TKD mutations, particularly when used at higher doses.

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Molecular Profile Treatment Approach
Gene Name Source Synonyms Protein Domains Gene Description Gene Role
Therapy Name Drugs Efficacy Evidence Clinical Trials
Drug Name Trade Name Synonyms Drug Classes Drug Description
Gene Variant Impact Protein Effect Variant Description Associated with drug Resistance
FLT3 E778K missense unknown FLT3 E778K lies within the protein kinase domain of the Flt3 protein (UniProt.org). E778K has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 E786K missense unknown FLT3 E786K lies within the protein kinase domain of the Flt3 protein (UniProt.org). E786K has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 G631R missense unknown FLT3 G631R lies within the protein kinase domain of the Flt3 protein (UniProt.org). G631R has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 G669R missense unknown FLT3 G669R lies within the protein kinase domain of the Flt3 protein (UniProt.org). G669R has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 G757E missense unknown FLT3 G757E lies within the protein kinase domain of the Flt3 protein (UniProt.org). G757E has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 G822E missense unknown FLT3 G822E lies within the protein kinase domain of the Flt3 protein (UniProt.org). G822E has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 G846D missense unknown FLT3 G846D lies within the protein kinase domain of the Flt3 protein (UniProt.org). G846D has been identified in the scientific literature (PMID: 32040554, PMID: 31013658), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 H721Y missense unknown FLT3 H721Y lies within the protein kinase domain of the Flt3 protein (UniProt.org). H721Y has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 M837I missense unknown FLT3 M837I lies within the protein kinase domain of the Flt3 protein (UniProt.org). M837I has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 M837K missense unknown FLT3 M837K lies within the protein kinase domain of the Flt3 protein (UniProt.org). M837K has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 M855T missense unknown FLT3 M855T lies within the protein kinase domain of the Flt3 protein (UniProt.org). M855T has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 N609T missense unknown FLT3 N609T lies within the protein kinase domain of the Flt3 protein (UniProt.org). N609T has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 N841H missense unknown FLT3 N841H lies within the protein kinase domain of the Flt3 protein (UniProt.org). N841H has been identified in the scientific literature (PMID: 32040554, PMID: 24623852, PMID: 16990784), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 N841T missense unknown FLT3 N841T lies within the activation loop of the protein kinase domain of the Flt3 protein (PMID: 25837374). N841T has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 N841Y missense unknown FLT3 N841Y lies within the activation loop of the protein kinase domain of the Flt3 protein (PMID: 25837374). N841Y has been identified in the scientific literature (PMID: 32040554, PMID: 15178581), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Apr 2022).
FLT3 R845S missense unknown FLT3 R845S lies within the activation loop of the protein kinase domain of the Flt3 protein (PMID: 25837374). R845S has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 S705N missense unknown FLT3 S705N lies within the protein kinase domain of the Flt3 protein (UniProt.org). S705N has been identified in the scientific literature (PMID: 32040554), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, Aug 2022).
FLT3 Y693C missense unknown FLT3 Y693C lies within the protein kinase domain of the Flt3 protein (UniProt.org). Y693C has been demonstrated to promote secondary drug resistance in the context of FLT3 internal tandem duplication (FLT3-ITD) mutations (PMID: 32040554, PMID: 35395091), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, May 2022). Y
FLT3 Y693N missense unknown FLT3 Y693N lies within the protein kinase domain of the Flt3 protein (UniProt.org). Y693N has been demonstrated to promote secondary drug resistance in the context of FLT3 internal tandem duplication (FLT3-ITD) mutations (PMID: 32040554, PMID: 35395091), but has not been biochemically characterized and therefore, its effect on Flt3 protein function is unknown (PubMed, May 2022). Y
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
FLT3 exon 14 ins FLT3 N841T hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N841T in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835A hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835A in culture (PMID: 32040554). 32040554
FLT3 I836del hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 I836del in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 F691L FLT3 D835V acute myeloid leukemia predicted - resistant Gilteritinib Case Reports/Case Series Actionable In a Phase I trial, a patient with acute myeloid leukemia harboring FLT3 ITD with FLT3 D835Y and F691L was resistant to Xospata (gilteritinib) (PMID: 32040554). 32040554
FLT3 N841I hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 N841I in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 F691L acute myeloid leukemia resistant Gilteritinib Case Reports/Case Series Actionable In a Phase I trial, three patients with acute myeloid leukemia harboring FLT3 ITD with FLT3 F691L were resistant to Xospata (gilteritinib) (PMID: 32040554). 32040554
FLT3 D839G hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 D839G in culture (PMID: 32040554). 32040554
FLT3 D835Y hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 D835Y in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 E778K hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 E778K in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 N609T hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N609T in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835I hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835I in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835V acute myeloid leukemia resistant Quizartinib Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring FLT3 ITD with FLT3 D835V were resistant to Vanflyta (quizartinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 N841I hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N841I in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 F691L acute myeloid leukemia resistant Quizartinib Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring FLT3 ITD with FLT3 F691L were resistant to Vanflyta (quizartinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 Y693N FLT3 D835V hematologic cancer resistant Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D835V and FLT3 Y693N were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 N841K hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N841K in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 N841K acute myeloid leukemia resistant Quizartinib Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring FLT3 ITD with FLT3 N841K were resistant to Vanflyta (quizartinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 E786K hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 E786K in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D839H hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D839H in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835V hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835V in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 M837I hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 M837I in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835H acute myeloid leukemia sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in acute myeloid leukemia cells harboring FLT3 ITD with FLT3 D835H in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 N841H hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N841H in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 F691L hematologic cancer resistant Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 F691L demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 G697S hematologic cancer resistant Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 G697S demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 H721Y hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 H721Y in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D839N hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D839N in culture (PMID: 32040554). 32040554
FLT3 R845S hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 R845S in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835H acute myeloid leukemia resistant Quizartinib Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring FLT3 ITD with FLT3 D835H were resistant to Vanflyta (quizartinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835V acute myeloid leukemia sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in acute myeloid leukemia cells harboring FLT3 ITD with FLT3 D835V in culture (PMID: 32040554). 32040554
FLT3 Y842C hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 Y842C in culture (PMID: 32040554). 32040554
FLT3 D835V hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 D835V in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835Y hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835Y in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 G669R hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G669R in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835E hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835E in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 G822E hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G822E in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 K429E hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 K429E in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 R845G hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 R845G in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 Y842C hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 Y842C in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835G hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835G in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 Y842H hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 Y842H in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 Y842C acute myeloid leukemia sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in acute myeloid leukemia cells harboring FLT3 ITD with FLT3 Y842C in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D839G hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D839G in culture (PMID: 32040554). 32040554
FLT3 N841T hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 N841T in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 G697S FLT3 D835V hematologic cancer resistant Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D835V and FLT3 G697S were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D698N hematologic cancer resistant Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D698N demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 N841K acute myeloid leukemia sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in acute myeloid leukemia cells harboring FLT3 ITD with FLT3 N841K in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 G846S hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G846S in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 R834Q hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 R834Q in culture (PMID: 32040554). 32040554
FLT3 N841Y acute myeloid leukemia predicted - sensitive Gilteritinib Case Reports/Case Series Actionable In a Phase I trial, Xospata (gilteritinib) resulted in a partial response in an acute myeloid leukemia patient harboring FLT3 N841Y (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 G757E hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G757E in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D698N FLT3 D835V hematologic cancer resistant Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D835V and FLT3 D698N were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835Y acute myeloid leukemia sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in acute myeloid leukemia cells harboring FLT3 ITD with FLT3 D835Y in culture (PMID: 32040554). 32040554
FLT3 N841Y hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 N841Y in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 I836del hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 I836del in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 M664I hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 M664I in culture (PMID: 32040554). 32040554
FLT3 D835F hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 D835F in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 Y693N hematologic cancer resistant Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 Y693N demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 Y842C acute myeloid leukemia resistant Quizartinib Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring FLT3 ITD with FLT3 Y842C were resistant to Vanflyta (quizartinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 G631R hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G631R in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835H hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835H in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 G846D hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G846D in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835N hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835N in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 F691L acute myeloid leukemia resistant Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring FLT3 ITD with FLT3 F691L were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835del hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835del in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 S705N hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 S705N in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D839A hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D839A in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 G846R hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G846R in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 A848P hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 A848P in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 Y693C FLT3 D835V hematologic cancer resistant Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D835V and FLT3 Y693C were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 Y693C hematologic cancer resistant Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 Y693C demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 N841Y hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N841Y in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835Y acute myeloid leukemia resistant Quizartinib Preclinical - Cell culture Actionable In a preclinical study, acute myeloid leukemia cells harboring FLT3 ITD with FLT3 D835Y were resistant to Vanflyta (quizartinib) in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 D835F hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835F in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 M837K hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 M837K in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 M855T hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 M855T in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 N676K hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N676K in culture (PMID: 32040554). 32040554
FLT3 N676K hematologic cancer sensitive Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 N676K in culture (PMID: 32040554). 32040554
FLT3 exon 14 ins FLT3 F691L FLT3 D835V hematologic cancer resistant Gilteritinib Preclinical - Cell culture Actionable In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D835V and FLT3 F691L were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). 32040554