Thioguanine (6-TG)

Indications
 Oral
Acute lymphoblastic leukaemia, Chronic myeloid leukaemia, Acute myeloid leukaemia
Adult: As a single agent chemotherapy: Initially 2 mg/kg/day, increased to 3 mg/kg/day after 4 wk if no improvement and no leukocyte or platelet depression. Alternatively, induction therapy: 100-200 mg/m2/day in 1-2 divided doses over a period of 5-20 days. Maintenance therapy: Intermittent or continuous daily doses between 60-200 mg/m2. In combination with other cytotoxic drugs: Refer to currently published protocols for dose, method and sequence of admin. Dose and duration depends on the combination of cytotoxic drug used.
Child: As a single agent chemotherapy: Initially 2 mg/kg/day, increased to 3 mg/kg/day after 4 wk if no improvement and no leukocyte or platelet depression. Alternatively, induction therapy: 60-200 mg/m2/day in 1-2 divided doses over a period of 5-20 days. Maintenance therapy: Intermittent or continuous daily doses between 60-200 mg/m2. In combination with other cytotoxic drugs: Refer to currently published protocols for dose, method and sequence of admin. Dose and duration depends on the combination of cytotoxic drug used.
Renal impairment: Dosage adjustment may be needed.
Hepatic impairment: Dosage adjustment may be needed.
Contraindications
 Pregnancy, lactation, prior resistance to drug. Immunisation with live vaccines.
Warnings / Precautions
 Renal or hepatic impairment. Inherited deficiency of thiopurine methyltransferase. Resistance to tioguanine therapy in Lesch-Nyhan syndrome. Monitor haemoglobin concentration, haematocrit, total WBC count, differential count and platelet count at least once a wk or more frequently during therapy. Discontinue treatment temporarily at first signs of unusually large decrease in leukocytes, platelets or haemoglobin. Resume therapy if leukocyte or platelet count increases or stays at an acceptable level for 2-3 days. Withhold therapy if there is worsening of LFT, jaundice, hepatomegaly, anorexia with tenderness in the right hypochondrium, or if there is evidence of toxic hepatitis, biliary stasis or severe bone marrow depression. Not recommended for maintenance therapy or long-term continuous treatments due to hepatotoxicity.
Adverse Reactions
 Myelosuppression especially leukopenia, thrombocytopenia, anaemia; hyperuricaemia; nausea; vomiting; diarrhoea; anorexia and stomatitis; rash; dermatitis; jaundice; increased risk of infections.
Potentially Fatal: Hepatotoxicity, life-threatening infections due to myelosupression.
Overdose Reactions
 Nausea, vomiting, malaise, hypotension, diaphoresis, myelosuppression and azotaemia. Induce emesis to reduce absorption of drug. Treatment is symptomatic and supportive. There is no known antidote. Haemodialysis unlikely to be helpful.
Drug Interactions
 Increased risk of heptotoxicity, portal hypertension and oesophageal varices during long-term continuous therapy with busulfan. Increased haematological toxicity with aminosalicylate derivatives (e.g. olsalazine, mesalazine or sulfasalazine), which may inhibit the thiopurine methyltransferase enzyme. May decrease phenytoin or carbamazepine levels.
See Below for More tioguanine Drug Interactions
Mechanism of Actions
 Tioguanine, an antineoplastic that acts as an antimetabolite, has actions similar to those of mercaptopurine. It is an analogue of the natural purine, guanine and is rapidly converted to ribonucleotides which are then incorporated into the DNA and RNA after repeated dosing. The cytotoxic effects arises from the substitution of the ribonucleotides into DNA.Tioguanine has some immunosuppressive activity and there is complete cross-resistance between tioguanine and mercaptopurine.
Absorption: Incomplete and variable absorption from GI tract. Average bioavailbility: 30%.
Distribution: Does not cross the blood-brain barrier significantly; crosses the placenta.
Metabolism: Rapidly and extensively metabolised in liver and other tissues. Inactivated mainly by methylation to aminomethylthiopurine; some are deaminated to thioxanthine which may be further oxidised by xanthine oxidase to thiouric acid. Inactivation is independent of xanthine oxidase and is unaffected by enzyme inhibition.
Excretion: Excreted in urine mainly as metabolites and unchanged drug (negligible).
Storage Conditions
 Oral: Store at 15-25°C (59-77°F).
ATC Classification
 L01BB03 - tioguanine ; Belongs to the class of antimetabolites, purine analogues. Used in the treatment of cancer.
Storage
 Oral: Store at 15-25°C (59-77°F).
Available As
  • Thioguanine (6-TG) 40 mg

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