II. Indications

III. 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

IV. Medications

  1. Thioguanine 40 mg scored tablets

V. Dosing

  1. See other references for disease specific dosing protocols

VI. 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)

VII. 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

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Related Studies

Ontology: Thioguanine (C0039902)

Definition (CHV) a kind of cancer treatment drug
Definition (CHV) a kind of cancer treatment drug
Definition (CHV) a kind of cancer treatment drug
Definition (NCI) A synthetic guanosine analogue antimetabolite. Phosphorylated by hypoxanthine-guanine phosphoribosyltransferase, thioguanine incorporates into DNA and RNA, resulting in inhibition of DNA and RNA syntheses and cell death. This agent also inhibits glutamine-5-phosphoribosylpyrophosphate amidotransferase, thereby inhibiting purine synthesis. (NCI04)
Definition (NCI_NCI-GLOSS) An anticancer drug that belongs to the family of drugs called antimetabolites.
Definition (CSP) thioguanine is USP.
Definition (MSH) An antineoplastic compound which also has antimetabolite action. The drug is used in the therapy of acute leukemia.
Definition (PDQ) A synthetic guanosine analogue antimetabolite. Phosphorylated by hypoxanthine-guanine phosphoribosyltransferase, thioguanine incorporates into DNA and RNA, resulting in inhibition of DNA and RNA syntheses and cell death. This agent also inhibits glutamine-5-phosphoribosylpyrophosphate amidotransferase, thereby inhibiting purine synthesis. Check for "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43669&idtype=1" active clinical trials or "http://www.cancer.gov/Search/ClinicalTrialsLink.aspx?id=43669&idtype=1&closed=1" closed clinical trials using this agent. ("http://nciterms.nci.nih.gov:80/NCIBrowser/ConceptReport.jsp?dictionary=NCI_Thesaurus&code=C876" NCI Thesaurus)
Concepts Pharmacologic Substance (T121) , Organic Chemical (T109)
MSH D013866
SnomedCT 387407006, 72623000
LNC LP30750-1, LP31792-2, MTHU014979, MTHU027390
English 6-Thioguanine, Thioguanine, 6 thioguanine, 6H-Purine-6-thione, 2-amino-1,7-dihydro-, Tioguanine, thioguanine, 6 Thioguanine, 2-Amino 6MP, 2-Amino-1,7-dihydro-6H-purine-6-thione, 2-Amino-6-purinethiol, 2-Aminopurin-6-thiol, 2-Aminopurine-6(1H)-thione, 2-Aminopurine-6-thiol, 6 Mercaptoguanine, 6-Mercapto-2-aminopurine, 6H-Purine-6-thione, 2-amino-1,7-dihydro- (9CI), 6-mercaptoguanine, 6-thioguanine, THIOGUANINE 06, 2-amino-6-mercaptopurine (thioguanine) (medication), thioguanine (medication), 2-amino-6-mercaptopurine (thioguanine), THIOGUANINE, 2-Amino-6-Purinethiol, 2 Amino 6 Purinethiol, Thioguanine [Chemical/Ingredient], tioguanine, Tioguanin, 6-Mercaptoguanine, 2-Mercapto-6-aminopurine, 6-Amino-2-mercaptopurine, 2-Amino-6-mercaptopurine, 6-TG, TG, Thioguanine (product), Thioguanine (substance)
Swedish Tioguanin
Czech thioguanin
Finnish Tioguaniini
Russian TIOGUANIN, 6-TIOGUANIN, 6-ТИОГУАНИН, ТИОГУАНИН
Japanese チオグアニン, 6-チオグアニン
German THIOGUANIN 06, 6-Thioguanin, Thioguanin
Italian 6-Tioguanina, Tioguanina
Polish Tioguanina
Spanish 2-amino-6-mercaptopurina, 6-tioguanina, tioguanina (producto), tioguanina (sustancia), tioguanina, 6-Tioguanina, Tioguanina
French Thioguanine, Tioguanine
Portuguese 6-Tioguanina, Tioguanina