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Description: Decitabine is indicated for treatment of patients with myelodysplastic syndrome (MDS). It is a chemical analogue of cytidine, a nucleoside present in DNA and RNA. Cells in the presence of Decitabine incorporate it into DNA during replication and RNA during transcription. The incorporation of Decitabine into DNA or RNA inhibits methyltransferase thereby causing demethylation in that sequence. This adversely affects the way that cell regulatory proteins are able to bind to the DNA/RNA substrate.
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Decitabine is an analogue of the natural nucleoside 2'-deoxycytidine. It functions in the same way as 5-Azacytidine.
Mechanism of Action: Decitabine is believed to exert its antineoplastic effects after phosphorylation and direct incorporation into DNA and inhibition of DNA methyltransferase, causing hypomethylation of DNA and cellular differentiation or apoptosis. Decitabine inhibits DNA methylation in vitro, which is achieved at concentrations that do not cause major suppression of DNA synthesis. Decitabine-induced hypomethylation in neoplastic cells may restore normal function to genes that are critical for the control of cellular differentiation and proliferation. In rapidly dividing cells, the cytotoxicity of decitabine may also be attributed to the formation of covalent adducts between DNA methyltransferase and decitabine incorporated into DNA. Non-proliferating cells are relatively insensitive to decitabine.
Indication: For treatment of patients with myelodysplastic syndromes (MDS) including previously treated and untreated, de novo and secondary MDS of all French-American-British subtypes (refractory anemia, refractory anemia with ringed sideroblasts, refractory anemia with excess blasts, refractory anemia with excess blasts in transformation, and chronic myelomonocytic leukemia) and intermediate-1, intermediate-2, and high-risk International Prognostic Scoring System groups.
Half Life: The terminal phase elimination half-life is 0.51 +/- 0.31 hours.
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Data Correlations | 10 studies

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Genes category icon Genes
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TKTL1 100 100
DAZL 97 97
541466 91 91
GAGE7 91 91
GAGE7B 89 89
RP13-36C9.3 88 88
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Biogroups category icon Biogroups
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GAGE 100 100
MAGE protein 89 89
Histone core 82 82
Pentose Phosphate Pathway 81 81
Natural Killer Cell Mediated Cytoto… 80 80
All Peptidase Inhibitors 80 80
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Individual Studies

  • Hypermethylated genes in lung cancer

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    Promoter hypermethylation coupled with loss of heterozygosity at the same locus results in loss of gene function in many tumor cells. In an effort to identify new cancer-specific methylation markers, we employed a high throughput global expression profiling approach in lung cancer cells.

    Authors: Shames DS, Girard L, Gao B et al.

    Organization: UT Southwestern Hamon Center Minna 6000 …

  • 5-aza-dC treated glioblastoma cultures

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    Glioblastoma, the most aggressive and least treatable form of malignant glioma, is the most common human brain tumor. Although many regions of allelic loss occur in glioblastomas, relatively few tumor suppressor genes have been found mutated at such loci. To address the possibility that epigenetic a…

    Authors: Mueller WC, Louis DN

    Organization: Charité Universitätsmedizin Berlin Neuro…
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Associated Researchers

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Thought leaders and organizations working on research involving 5-aza-2'-deoxycytidine.

View All Author iconAuthors
  • Peter A Jones
  • Gerda Egger
  • Richard L Momparler
  • Gangning Liang
  • Hagop M Kantarjian
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • M.D. Anderson Cancer Center
  • Eisai Inc.
  • SuperGen
  • USC/Norris Comprehensive Cancer Center
  • National Cancer Institute (NCI)
View All Affiliations icon Organizations
  • University of Texas M. D. Anderson Cancer Center
  • University of Southern California
  • Johns Hopkins Medical Institutions
  • University of Freiburg Medical Center
  • University of Goettingen

Clinical Trials | 124 trials

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