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    DRUG CLASS:

    Menin-MLL inhibitor

    Related drugs:
    4d
    Research Progress on the KMT2A-AFF3 Fusion Gene in Childhood Acute Lymphoblastic Leukemia: Mechanisms, Clinical Implications, and Therapeutic Strategies. (PubMed, Curr Issues Mol Biol)
    This review highlights the evidence defining its poor prognosis, which is primarily driven by profound chemoresistance to conventional therapies, including glucocorticoids. Finally, we discuss the rapidly evolving therapeutic landscape, detailing the limitations of standard intensive chemotherapy and the immense promise of novel targeted strategies, such as Menin inhibitors (e.g., Revumenib), DOT1L inhibitors, and immunotherapies (e.g., CAR-T cells, Blinatumomab), which hold the potential to revolutionize outcomes for this high-risk leukemia subtype.
    Review • Journal
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    KMT2A (Lysine Methyltransferase 2A) • AFF1 (AF4/FMR2 Family Member 1) • MEIS1 (Meis Homeobox 1) • MME (Membrane Metalloendopeptidase) • DOT1L (DOT1 Like Histone Lysine Methyltransferase) • AFF3 (AF4/FMR2 Family Member 3)
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    Blincyto (blinatumomab) • Revuforj (revumenib)
    5d
    SNDX-5613-0706: Evaluation of Revumenib in Participants With Colorectal Cancer and Other Solid Tumors (clinicaltrials.gov)
    P1/2, N=42, Completed, Syndax Pharmaceuticals | Active, not recruiting --> Completed | Trial completion date: Aug 2027 --> Jun 2025 | Trial primary completion date: Dec 2025 --> Jun 2025
    Trial completion • Trial completion date • Trial primary completion date
    |
    Stivarga (regorafenib) • Revuforj (revumenib)
    12d
    Study to Assess Safety, Tolerability, PK, and PD of Multiple Doses of ZE63-0302 Administrated Orally in T2DM Patients. (clinicaltrials.gov)
    P1, N=60, Recruiting, Eilean Therapeutics | Not yet recruiting --> Recruiting
    Enrollment open
    12d
    Сlinical Study Aiming to Evaluate the Safety, Tolerability, Pharmacokinetics and Pharmacodynamics of Single and Multiple Ascending Doses of ZE63-0302 in Healthy Volunteers (clinicaltrials.gov)
    P1, N=82, Completed, Eilean Therapeutics | Recruiting --> Completed | Trial completion date: Jun 2025 --> Nov 2025
    Trial completion • Trial completion date • First-in-human
    |
    itraconazole
    13d
    Ziftomenib + Mezigdomide in Adolesc. and Adults w/ R/R AML (clinicaltrials.gov)
    P1, N=24, Not yet recruiting, Massachusetts General Hospital
    New P1 trial
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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
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    Komzifti (ziftomenib) • mezigdomide (CC-92480)
    13d
    A Study of Revumenib and Mezigdomide in People With Leukemia (clinicaltrials.gov)
    P1/2, N=52, Recruiting, Memorial Sloan Kettering Cancer Center
    New P1/2 trial
    |
    NPM1 (Nucleophosmin 1) • KMT2A (Lysine Methyltransferase 2A) • NUP98 (Nucleoporin 98 And 96 Precursor 2)
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    MSK-IMPACT
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    Revuforj (revumenib) • mezigdomide (CC-92480)
    25d
    ALLG BM15: A Double-blind, Phase I/II, Randomised Study to Compare the Efficacy of Enzomenib Versus Placebo as Maintenance after Allogeneic Haematopoietic Stem Cell Transplantation in Subjects with Acute Myeloid Leukaemia (AML). (ACTRN12626000019303)
    P2, N=53, Not yet recruiting, Australasian Leukaemia and Lymphoma Group
    New P2 trial
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    enzomenib (DSP-5336)
    1m
    Food Effect Study in Healthy Volunteers (clinicaltrials.gov)
    P1, N=60, Active, not recruiting, Biomea Fusion Inc. | Recruiting --> Active, not recruiting
    Enrollment closed
    |
    icovamenib (BMF-219)
    1m
    A Study of 14C-Bleximenib (Radiolabeled) in Participants With Acute Leukemia (clinicaltrials.gov)
    P1, N=10, Recruiting, Janssen Research & Development, LLC
    New P1 trial
    |
    bleximenib (JNJ-6617)
    2ms
    A Phase IB Trial of Subcutaneous Blinatumomab in Combination With Revumenib for Patients With KMT2A-rearranged Acute Lymphoblastic Leukemia (clinicaltrials.gov)
    P1, N=20, Not yet recruiting, M.D. Anderson Cancer Center
    New P1 trial
    |
    clonoSEQ
    |
    Revuforj (revumenib)
    2ms
    REVEAL-ND NPM1: Study of Revumenib in Combination With Intensive Chemotherapy in Newly Diagnosed Acute Myeloid Leukemia (AML) With a NPM1 Mutation (clinicaltrials.gov)
    P3, N=468, Recruiting, Syndax Pharmaceuticals | Not yet recruiting --> Recruiting
    Enrollment open
    |
    cytarabine • Revuforj (revumenib)
    2ms
    Menin inhibitors as targeted therapy in KMT2A-Rearranged acute leukemia: A comprehensive review of current advances and therapeutic implications. (PubMed, Med Oncol)
    Among them, revumenib and ziftomenib have advanced furthest in clinical testing. Ongoing trials are now evaluating menin inhibitors in rational combinations, frontline regimens, and maintenance therapy. Collectively, these advances highlight menin inhibition as a transformative strategy in acute leukemia, reshaping therapy through precision-targeted epigenetic intervention.
    Review • Journal
    |
    NPM1 (Nucleophosmin 1) • KMT2A (Lysine Methyltransferase 2A) • HOXA9 (Homeobox A9) • MEIS1 (Meis Homeobox 1) • MEN1 (Menin 1)
    |
    NPM1 mutation • KMT2A rearrangement
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    Revuforj (revumenib) • Komzifti (ziftomenib)