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    DRUG CLASS:

    DNA methylation inhibitor

    Related drugs:
    1m
    Azanucleoside treatment leads to B-cell precursor acute lymphoblastic leukemia. (PubMed, Blood Neoplasia)
    5-Aza-4'-thio-2'-deoxycytidine (ATC) is an azanucleoside cytidine analog under investigation in preclinical studies for solid tumors as a promising DNA methyltransferase 1 (DNMT1) inhibitor...Bisulfite sequencing and treatment with a noncovalent DNMT1 inhibitor indicated that methylated cytosines were preferred targets for mutagenesis. This study reveals that ATC exposure leads to both DNMT1-dependent and -independent mutagenesis and provides a direct link between ATC exposure, a complex mutational signature, and malignant transformation.
    Journal
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    RAG1 (Recombination Activating 1)
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    4'-Thio-2'-Deoxycytidine (TdCyd)
    2ms
    ASCENT1: Research Study Investigating How Well NDec Works in People With Sickle Cell Disease (clinicaltrials.gov)
    P2, N=96, Completed, Novo Nordisk A/S | Active, not recruiting --> Completed | Trial primary completion date: Aug 2025 --> Dec 2024
    Trial completion • Trial primary completion date
    |
    hydroxyurea • decitabine/ tetrahydrouridine (EPI01)
    6ms
    A Study of Oral Tetrahydrouridine-Decitabine in Relapsed or Refractory Myelodysplastic Syndromes (MDS) (clinicaltrials.gov)
    P1, N=20, Recruiting, EpiDestiny, Inc. | Not yet recruiting --> Recruiting
    Enrollment open
    |
    decitabine/ tetrahydrouridine (EPI01)
    6ms
    A Study of Oral Tetrahydrouridine-Decitabine in Relapsed or Refractory Myelodysplastic Syndromes (MDS) (clinicaltrials.gov)
    P1, N=20, Not yet recruiting, EpiDestiny, Inc.
    New P1 trial
    |
    decitabine/ tetrahydrouridine (EPI01)
    6ms
    A Study of Nicotinamide With Oral Tetrahydrouridine and Decitabine to Treat High Risk Sickle Cell Disease (clinicaltrials.gov)
    P1, N=20, Recruiting, EpiDestiny, Inc. | Trial completion date: Apr 2024 --> Apr 2027 | Trial primary completion date: Mar 2024 --> Oct 2026
    Trial completion date • Trial primary completion date
    |
    decitabine/ tetrahydrouridine (EPI01)
    7ms
    To Study the Oral Bioavailability of a New Combination Formation of Decitabine and Tetrahydrouridine in Healthy Males (clinicaltrials.gov)
    P1, N=10, Completed, EpiDestiny, Inc. | Recruiting --> Completed
    Trial completion
    |
    decitabine/ tetrahydrouridine (EPI01)
    7ms
    ASCENT1: Research Study Investigating How Well NDec Works in People With Sickle Cell Disease (clinicaltrials.gov)
    P2, N=84, Active, not recruiting, Novo Nordisk A/S | Trial primary completion date: Dec 2024 --> Aug 2025 | Recruiting --> Active, not recruiting
    Enrollment closed • Trial primary completion date
    |
    hydroxyurea • decitabine/ tetrahydrouridine (EPI01)
    8ms
    Efficacy of Methionine Restriction and the PARP-inhibitor Olaparib and Their Combination on BRCA1 Mutant and Wild-type Triple-negative Breast Cancer Cell Lines. (PubMed, Anticancer Res)
    Methionine restriction and olaparib showed synergistic efficacy on the BRCA1-mutant TNBC cell line HCC1937. The BRCA1-mutant cell line MDA-MB-436 was most sensitive to rMETase. The BRCA1/2 wild-type TNBC cell line MDA-MB-231 was sensitive to a methionine-free medium but resistant to olaparib. Therefore, methionine restriction has clinical potential for BRCA1/2 wild-type and BRCA1-mutant olaparib-resistant and -sensitive TNBC.
    Preclinical • Journal • BRCA Biomarker • PARP Biomarker
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    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
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    BRCA wild-type
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    Lynparza (olaparib) • ONCase (recombinant methionine α, γ-lyase)
    12ms
    A Study to Test How Either a Capsule or a Tablet With NDec (Decitabine and Tetrahydrouridine) Works in the Body of Healthy People (clinicaltrials.gov)
    P1, N=44, Completed, Novo Nordisk A/S | Recruiting --> Completed
    Trial completion
    |
    decitabine/ tetrahydrouridine (EPI01)
    1year
    Molecular profiling of pre- and post- 5-azacytidine myelodysplastic syndrome samples identifies predictors of response. (PubMed, Front Oncol)
    This classifier outperformed a previously developed gene signature in a second MDS patient cohort, but signatures of hematological responses were unable to predict survival. Overall, these studies characterize the molecular consequences of AZA treatment in MDS HSPCs and identify a potential tool for predicting AZA therapy responses and overall survival prior to initiation of therapy.
    Journal • Tumor mutational burden
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    TMB (Tumor Mutational Burden) • TNFA (Tumor Necrosis Factor-Alpha) • CD34 (CD34 molecule)
    |
    azacitidine
    1year
    The Adrenal Pheochromocytoma Cell Line PC12 Efficiently Promotes the Regeneration Capability of Adipose Tissue-Derived Mesenchymal Stem Cells in Myogenesis: A Particular Approach to Improving Skeletal Muscle Cell Regeneration. (PubMed, Iran J Med Sci)
    Differentiation of ADSCs was induced by using 3 μg/mL 5-azacytidine for 24 hours...Coculturing PC12 cells and ADSCs improves the efficiency of myogenic differentiation. However, the effectiveness of myogenic differentiation depends on the proportions of administered PC12 cells.
    Preclinical • Journal
    |
    MUTYH (MutY homolog)
    |
    azacitidine
    1year
    Identification of SLC22A17 DNA methylation hotspot as a potential biomarker in cutaneous melanoma. (PubMed, J Transl Med)
    The SLC22A17 methDNA hotspot could represent a promising biomarker for CM, highlighting the regulatory role of methDNA on SLC22A17 expression. These results pave the way for the identification of novel epigenetic biomarkers and therapeutic targets for the management of CM patients.
    Journal • Epigenetic controller
    |
    SLC22A3 (Solute Carrier Family 22 Member 3)
    |
    azacitidine