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Thioguanine

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Thioguanine, Tabloid

  • See Also
  1. Chemotherapy
  2. Antimetabolite Chemotherapy
  • Indications
  1. Acute Myelogenous Leukemia (AML)
  2. Acute Lymphoblastic Leukemia (ALL, off-label use)
  • Mechanism
  1. Synthetic guanosine analog antimetabolite
  2. Thioguanine is phosphorylated by HGPRT (hypoxanthine-guanine phosphoribosyltransferase)
    1. Incorporated into DNA and RNA in place of guanosine
    2. Inhibits DNA and RNA synthesis
  3. Inhibits GPAT (Glutamine-5-phosphoribosylpyrophosphate amidotransferase)
    1. Inhibits Purine synthesis
  • Medications
  1. Thioguanine 40 mg scored tablets
  • Dosing
  1. See other references for disease specific dosing protocols
  • Adverse Effects
  1. Alopecia
  2. Hepatotoxicity
  3. Hyperuricemia
  4. Myelosuppression
  5. Thioprine-Related Toxicity (Severe)
    1. Associated with NUDT15 Gene Anomaly (Nudix Hydrolase 15 deficiency)
  • Safety
  1. Avoid in Pregnancy (any trimester)
    1. Use reliable Contraception
  2. Avoid in Lactation
  3. Monitoring
    1. Complete Blood Count
    2. Liver Function Tests
  • Resources
  1. Thioguanine (DailyMed)
    1. https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=4490128b-e73f-4849-9d6e-e8591639d771