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    GENE:

    FLT3 (Fms-related tyrosine kinase 3)

    i
    Other names: FLT3, Fms Related Tyrosine Kinase 3, Receptor-Type Tyrosine-Protein Kinase FLT3, Stem Cell Tyrosine Kinase 1, Fms-Like Tyrosine Kinase 3, CD135, FLK-2, STK1, Growth Factor Receptor Tyrosine Kinase Type III, Fetal Liver Kinase 2
    3d
    TROPHY-15: MRD-guided Maintenance Post-HCT: Gilteritini vs Sorafenib (clinicaltrials.gov)
    P3, N=594, Recruiting, The First Affiliated Hospital of Soochow University | Not yet recruiting --> Recruiting
    Enrollment open
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    FLT3 (Fms-related tyrosine kinase 3)
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    FLT3-ITD mutation
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    sorafenib • Xospata (gilteritinib)
    3d
    Aclarubicin Plus With Azacitidine and Venetoclax in the Treatment of Acute Myeloid Leukemia (clinicaltrials.gov)
    P1/2, N=112, Not yet recruiting, Shanghai Jiao Tong University School of Medicine
    New P1/2 trial
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    FLT3 (Fms-related tyrosine kinase 3) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2)
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    Venclexta (venetoclax) • azacitidine • aclarubicin
    4d
    Discovery of GBA-16-24 as a highly potent, selective ATR inhibitor for the treatment of FLT3-mutated acute myeloid leukemia. (PubMed, RSC Med Chem)
    In addition, when combined with clinically approved FLT3 inhibitors, GBA-16-24 exhibits synergistic anti-AML effects. Therefore, our findings introduce a promising ATR inhibitor and propose the combination of ATR and FLT3 inhibition as a novel synthetic lethal strategy for treating FLT3-mutated AML.
    Journal
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    FLT3 (Fms-related tyrosine kinase 3)
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    FLT3 mutation
    4d
    Advances in Pyrazolopyrimidine Scaffold: Synthetic Strategies and Biological Applications (2019-Present). (PubMed, Arch Pharm (Weinheim))
    The latter scaffolds have also been efficiently and sustainably approached through recent synthetic methodologies, such as multicomponent reactions, microwave-assisted synthesis, and green chemistry methodologies. Several derivatives have been shown to have strong anticancer, antimicrobial, anti-inflammatory, and antiviral effects, usually through the action on important enzymes, including CDK2, FLT3, VEGFR-2, PIM-1, and Topoisomerase IIa.
    Review • Journal
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    FLT3 (Fms-related tyrosine kinase 3) • KDR (Kinase insert domain receptor) • PIM1 (Pim-1 Proto-Oncogene) • CDK2 (Cyclin-dependent kinase 2)
    4d
    Polθ activity modulates sensitivity to standard therapies in DNMT3A-deficient leukemia. (PubMed, Cell Rep Med)
    Polθ inhibitors enhance the anti-leukemic effects of standard drugs such as FLT3 kinase inhibitor quizartinib, cytarabine ± doxorubicin, and etoposide in vitro and in mice with DNMT3Amut leukemia. Altogether, Polθ is an attractive target in DNMT3Amut hematological malignancies.
    Journal • PARP Biomarker
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    FLT3 (Fms-related tyrosine kinase 3) • DNMT3A (DNA methyltransferase 1) • MSH2 (MutS Homolog 2) • PARP1 (Poly(ADP-Ribose) Polymerase 1) • MSH3 (MutS Homolog 3)
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    cytarabine • doxorubicin hydrochloride • etoposide IV • Vanflyta (quizartinib)
    5d
    CA-4948 102: Dose Escalation/ Expansion Study of CA-4948 as Monotherapy in Patients With Acute Myelogenous Leukemia (AML) or Myelodysplastic Syndrome (MDS) (clinicaltrials.gov)
    P1/2, N=366, Suspended, Curis, Inc. | Recruiting --> Suspended
    Trial suspension • IO biomarker
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    FLT3 (Fms-related tyrosine kinase 3) • SF3B1 (Splicing Factor 3b Subunit 1) • U2AF1 (U2 Small Nuclear RNA Auxiliary Factor 1)
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    FLT3 mutation • SF3B1 mutation
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    Venclexta (venetoclax) • emavusertib (CA-4948)
    6d
    Total Marrow and Lymphoid Irradiation, Fludarabine, and Melphalan Before Donor Stem Cell Transplant in Treating Participants With High-Risk Acute Leukemia or Myelodysplastic Syndrome (clinicaltrials.gov)
    P1, N=36, Suspended, City of Hope Medical Center | Recruiting --> Suspended
    Trial suspension
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    FLT3 (Fms-related tyrosine kinase 3) • NPM1 (Nucleophosmin 1) • HLA-DRB1 (Major Histocompatibility Complex, Class II, DR Beta 1) • HLA-B (Major Histocompatibility Complex, Class I, B) • HLA-C (Major Histocompatibility Complex, Class I, C)
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    melphalan • fludarabine IV
    7d
    Twenty Years of Therapeutic Leukocytapheresis in Newly Diagnosed Acute Myeloid Leukemia: Insights From A Single Center. (PubMed, J Clin Apher)
    LCP remains a valuable therapeutic option for patients with HL in newly diagnosed AML. Our long-term experience supports its safety and efficacy, particularly in symptomatic patients, as a bridge to definitive therapy regardless of treatment intensity eligibility.
    Retrospective data • Journal
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    FLT3 (Fms-related tyrosine kinase 3) • NPM1 (Nucleophosmin 1) • KMT2A (Lysine Methyltransferase 2A)
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    FLT3-ITD mutation • NPM1 mutation • KMT2A rearrangement
    8d
    GFH009X2101: Study of SLS009 (Formerly GFH009) a Potent Highly Selective CDK9 Inhibitor in Patients With Hematologic Malignancies and High-Risk Newly Diagnosed AML (clinicaltrials.gov)
    P1/2, N=160, Recruiting, Sellas Life Sciences Group | Trial completion date: Dec 2025 --> Dec 2027 | Trial primary completion date: Dec 2025 --> Dec 2026
    Trial completion date • Trial primary completion date
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    PD-L1 (Programmed death ligand 1) • KRAS (KRAS proto-oncogene GTPase) • FLT3 (Fms-related tyrosine kinase 3) • IDH1 (Isocitrate dehydrogenase (NADP(+)) 1) • IDH2 (Isocitrate Dehydrogenase (NADP(+)) 2) • NPM1 (Nucleophosmin 1) • SF3B1 (Splicing Factor 3b Subunit 1) • ASXL1 (ASXL Transcriptional Regulator 1) • SRSF2 (Serine and arginine rich splicing factor 2) • BCOR (BCL6 Corepressor) • U2AF1 (U2 Small Nuclear RNA Auxiliary Factor 1) • STAG2 (Stromal Antigen 2) • DDX41 (DEAD-Box Helicase 41) • ZRSR2 (Zinc Finger CCCH-Type, RNA Binding Motif And Serine/Arginine Rich 2)
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    TP53 mutation • KRAS mutation • FLT3-ITD mutation • Chr del(17p) • IDH1 mutation • IDH2 mutation • FLT3 mutation • TP53 wild-type • NPM1 mutation • KRAS wild-type • Chr del(11q) • ASXL1 mutation • SF3B1 mutation • EZH2 mutation • NRAS wild-type • SRSF2 mutation • IDH wild-type
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    Venclexta (venetoclax) • azacitidine • tambiciclib (SLS009)
    8d
    A phase I/II study of gilteritinib in combination with chemotherapy in newly diagnosed patients with AML in Asia: final analysis. (PubMed, Ther Adv Hematol)
    All patients enrolled in phase II received induction and consolidation therapy with gilteritinib 120 mg/day plus chemotherapy (induction: ⩽2 cycles, idarubicin/cytarabine once-daily; consolidation: ⩽4 cycles, cytarabine twice-daily) followed by maintenance with gilteritinib 120 mg/day monotherapy (⩽26 cycles). Induction and consolidation with gilteritinib plus chemotherapy, and maintenance with gilteritinib monotherapy were well tolerated in ND patients in Asia with FLT3 mut+ AML and had favorable efficacy compared with historical data. This trial was registered with the ClinicalTrials.gov identifier NCT02310321.
    P1/2 data • Journal
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    FLT3 (Fms-related tyrosine kinase 3)
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    FLT3 mutation
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    cytarabine • Xospata (gilteritinib) • idarubicin hydrochloride
    10d
    An oncogenic, truncated FGFR1 variant cooperates with SPFQ/NONO to regulate gene transcription in FGFR1-driven leukaemia. (PubMed, Br J Haematol)
    In addition, treatment with the NONO inhibitor auranofin suppresses cell proliferation of tnFGFR1-transformed cells in vitro mitigating leukaemia progression in vivo in a mouse model. Thus, future targeting of this tnFGFR1 transcription complex may provide a means for treating tnFGFR1-driven leukaemia.
    Journal
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    FLT3 (Fms-related tyrosine kinase 3) • FGFR1 (Fibroblast growth factor receptor 1)