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Thioguanine Brand names, Thioguanine Analogs

Thioguanine Brand Names Mixture

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Thioguanine Chemical_Formula


Thioguanine RX_link

Thioguanine fda sheet

Thioguanine FDA

Thioguanine msds (material safety sheet)

Thioguanine MSDS

Thioguanine Synthesis Reference

Elion et al.; J.Amer.Chem.Soc.; 81;1898,1901 (1959)

Thioguanine Molecular Weight

167.193 g/mol

Thioguanine Melting Point

>360 oC

Thioguanine H2O Solubility

36.3 mg/mL

Thioguanine State


Thioguanine LogP


Thioguanine Dosage Forms

Oral tablets

Thioguanine Indication

For remission induction and remission consolidation treatment of acute nonlymphocytic leukemias.

Thioguanine Pharmacology

Thioguanine is an antineoplastic anti-metabolite used in the treatment of several forms of leukemia including acute nonlymphocytic 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. Thioguanine was first synthesized and entered into clinical trial more than 30 years ago. It is a 6-thiopurine analogue of the naturally occurring purine bases hypoxanthine and guanine. Intracellular activation results in incorporation into DNA as a false purine base. An additional cytotoxic effect is related to its incorporation into RNA. Thioguanine is cross-resistant with mercaptopurine. Cytotoxicity is cell cycle phase-specific (S-phase).

Thioguanine Absorption

Absorption of an oral dose is incomplete and variable, averaging approximately 30% of the administered dose (range: 14% to 46%)

Thioguanine side effects and Toxicity

Oral, mouse: LD50 = 160 mg/kg. Symptoms of overdose include nausea, vomiting, malaise, hypotension, and diaphoresis.

Thioguanine Patient Information


Patients should be informed that the major toxicities of thioguanine are related to
myelosuppression, hepatotoxicity, and gastrointestinal toxicity. Patients should never
be allowed to take the drug without medical supervision and should be advised to consult
their physician if they experience fever, sore throat, jaundice, nausea, vomiting, signs
of local infection, bleeding from any site, or symptoms suggestive of anemia. Women of
childbearing potential should be advised to avoid becoming pregnant.

Thioguanine Organisms Affected

Humans and other mammals