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Description: An immunosuppressive agent used in combination with cyclophosphamide and hydroxychloroquine in the treatment of rheumatoid arthritis. According to the Fourth Annual Report on Carcinogens (NTP 85-002, 1985), this substance has been listed as a known carcinogen. (Merck Index, 11th ed)
Drug Type: Small Molecule; Approved
Pharmacology: Azathioprine is a chemotherapy drug, now rarely used for chemotherapy but more for immunosuppression in organ transplantation and autoimmune disease such as rheumatoid arthritis or inflammatory bowel disease or Crohn's disease. It is a pro-drug, converted in the body to the active metabolite 6-mercaptopurine. Azathioprine acts to inhibit purine synthesis necessary for the proliferation of cells, especially leukocytes and lymphocytes. It is a safe and effective drug used alone in certain autoimmune diseases, or in combination with other immunosuppressants in organ transplantation. Its most severe side effect is bone marrow suppression, and it should not be given in conjunction with purine analogues such as allopurinol. The enzyme thiopurine S-methyltransferase (TPMT) deactivates 6-mercaptopurine. Genetic polymorphisms of TPMT can lead to excessive drug toxicity, thus assay of serum TPMT may be useful to prevent this complication.
Mechanism of Action: Azathioprine antagonizes purine metabolism and may inhibit synthesis of DNA, RNA, and proteins. It may also interfere with cellular metabolism and inhibit mitosis. The mechanism of action of azathioprine in rheumatoid arthritis is not known but is most likely related to its immunosuppresive action.
Indication: For use as an adjunct in the prevention of rejection in renal homotransplantation. Also for the management of severe, active rheumatoid arthritis unresponsive to rest, aspirin or other nonsteroidal anti-inflammatory drugs, or to agents in the class of which gold is an example.
Half Life: Approximately 5 hours for the unchanged drug and its metabolites.
Molecular weight: 277.264 g/mol
Molecular formula: C9H7N7O2S
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Data Correlations | 1 study

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Genes category icon Genes
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ALAS2 100 100
CYP17A1 96 96
A2M 93 93
PRPH 89 89
FCN2 89 89
EGR1 89 89
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Biogroups category icon Biogroups
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Lysine Biosynthesis 100 100
Type II keratin 99 99
Alkaloid Biosynthesis I 99 99
ACE Inhibitor Pathway 99 99
Glucocorticoid Mineralocorticoid Me… 98 98
I43 - oprin 98 98
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Individual Studies

  • Non-genotoxic Hepatocarcinogens (Iconix study)

    Rattus norvegicus Rattus norvegicus | RNA Expression   RNA Expression

    We have developed a short-term in vivo rat assay that predicts whether non-genotoxic chemicals are likely to induce hepatic tumors based on transcript profiles in the liver. Using a large independent test set, assay accuracy was found to be superior to existing pathological and genomic markers. Comp…

    Authors: Fielden MR, Brennan R, Gollub J

    Organization: Iconix Biosciences 325 E. Middlefield Rd…
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Associated Researchers

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Thought leaders and organizations working on research involving azathioprine.

View All Author iconAuthors
  • A Ansari
  • Severine Vermeire
  • M Arenas
  • Bernard Duclos
  • Paul Rutgeerts
View All Clinical trial sponsors icon Clinical Trials Sponsors
  • Assistance Publique - Hôpitaux de Paris
  • Hospices Civils de Lyon
  • National Heart, Lung, and Blood Institute (NHLBI)
  • National Institute of Allergy and Infectious Diseases (NIAID)
  • Schering-Plough
View All Affiliations icon Organizations
  • University of California
  • Stanford University School of Medicine
  • Massachusetts Institute of Technology
  • Genentech Inc
  • Leuven University Hospitals

Clinical Trials | 670 trials

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