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    DRUG CLASS:

    DNA methylation inhibitor

    Related drugs:
    24d
    ASCENT1: Research Study Investigating How Well NDec Works in People With Sickle Cell Disease (clinicaltrials.gov)
    P2, N=96, Completed, Novo Nordisk A/S | Trial primary completion date: Dec 2024 --> Jul 2025
    Trial primary completion date
    |
    hydroxyurea • decitabine/ tetrahydrouridine (EPI01)
    1m
    Human fibrosarcoma cells selected for ultra-high doxorubicin resistance, acquire trabectedin cross-resistance, remain sensitive to recombinant methioninase, and have increased c-MYC expression. (PubMed, Front Oncol)
    The findings indicate that rMETase can overcome ultra-high doxorubicin resistance in fibrosarcoma cells, likely through targeting methionine addiction, a universal metabolic vulnerability of cancer. These results support the potential clinical application of methionine restriction therapy to treat doxorubicin-resistant STS.
    Journal
    |
    MYC (V-myc avian myelocytomatosis viral oncogene homolog)
    |
    doxorubicin hydrochloride • Yondelis (trabectedin) • ONCase (recombinant methionine α, γ-lyase)
    3ms
    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
    |
    RAG1 (Recombination Activating 1)
    |
    4'-Thio-2'-Deoxycytidine (TdCyd)
    3ms
    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)
    8ms
    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)
    8ms
    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)
    8ms
    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)
    8ms
    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)
    8ms
    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)
    10ms
    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
    |
    BRCA1 (Breast cancer 1, early onset) • BRCA2 (Breast cancer 2, early onset)
    |
    BRCA wild-type
    |
    Lynparza (olaparib) • ONCase (recombinant methionine α, γ-lyase)
    1year
    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)
    over1year
    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
    |
    TMB (Tumor Mutational Burden) • TNFA (Tumor Necrosis Factor-Alpha) • CD34 (CD34 molecule)
    |
    azacitidine