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Description: A pyrimidine nucleoside analog that is used mainly in the treatment of leukemia, especially acute non-lymphoblastic leukemia. Cytarabine is an antimetabolite antineoplastic agent that inhibits the synthesis of DNA. Its actions are specific for the S phase of the cell cycle. It also has antiviral and immunosuppressant properties. (From Martindale, The Extra Pharmacopoeia, 30th ed, p472)
Drug Type: Small Molecule; Approved; Investigational
Pharmacology: Cytarabine is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute myelogenous leukemia and meningeal leukemia. Anti-metabolites masquerade as purine or pyrimidine - which become the building blocks of DNA. They prevent these substances becoming incorporated in to DNA during the 'S' phase (of the cell cycle), stopping normal development and division. Cytarabine is metabolized intracellularly into its active triphosphate form (cytosine arabinoside triphosphate). This metabolite then damages DNA by multiple mechanisms, including the inhibition of alpha-DNA polymerase, inhibition of DNA repair through an effect on beta-DNA polymerase, and incorporation into DNA. The latter mechanism is probably the most important. Cytotoxicity is highly specific for the S phase of the cell cycle.
Mechanism of Action: Cytarabine acts through direct DNA damage and incorporation into DNA. Cytarabine is cytotoxic to a wide variety of proliferating mammalian cells in culture. It exhibits cell phase specificity, primarily killing cells undergoing DNA synthesis (S-phase) and under certain conditions blocking the progression of cells from the G1 phase to the S-phase. Although the mechanism of action is not completely understood, it appears that cytarabine acts through the inhibition of DNA polymerase. A limited, but significant, incorporation of cytarabine into both DNA and RNA has also been reported.
Indication: For the treatment of acute non-lymphocytic leukemia, acute lymphocytic leukemia and blast phase of chronic myelocytic leukemia.
Half Life: 10 minutes
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Data Correlations | 18 studies

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Genes category icon Genes
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POLB 100 100
FAHD2A 100 100
Mbl1 99 99
XIRP1 96 96
RGN 94 94
EBF1 94 94
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Biogroups category icon Biogroups
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SNARE Interactions In Vesicular Tra… 100 100
Glutathione Metabolism 100 100
Fatty Acid Metabolism 100 100
Heme Biosynthesis 99 99
Pitx2 Pathway 99 99
Thioredoxin-like fold 98 98
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Individual Studies

  • Drug-Induced Renal Tubular Toxicity

    Rattus norvegicus Rattus norvegicus | RNA Expression   RNA Expression

    These data support the publication titled "A Gene Expression Signature that Predicts the Future Onset of Drug-Induced Renal Tubular Toxicity"

    Authors: Fielden MR, Eynon BP, Natsoulis G et al.

    Organization: Iconix Pharmaceuticals 325 E Middlefield…

  • Rhabdomyosarcoma A673 cell treatments: Cytarabine, Doxorubicin and Puromycin

    Homo sapiens Homo sapiens | RNA Expression   RNA Expression

    An increasing number of cancer-associated mutations have been identified. Unfortunately, little therapy today exploits these tumor-specific genetic lesions. Often, the resulting oncoproteins have been intractable to easy manipulation with current small molecule screening approaches. To overcome this…

    Authors: Stegmaier K, Wong JS, Ross KN et al.

    Organization: Dana-Farber Cancer Institute and Childre…
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Associated Researchers

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Thought leaders and organizations working on research involving cytidine.

View All Author iconAuthors
  • F Nina Papavasiliou
  • Tasuku Honjo
  • Kazuo Kinoshita
  • Yoko Endo
  • Grace Teng
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • M.D. Anderson Cancer Center
  • Vion Pharmaceuticals
  • Weill Medical College of Cornell University
  • Children's Oncology Group
  • Pacira Pharmaceuticals, Inc
View All Affiliations icon Organizations
  • Rockefeller University
  • Kyoto University
  • University of California
  • Albert Einstein College of Medicine
  • University of Massachusetts Medical School

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