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Tioguanin Brand names, Tioguanin Analogs

Tioguanin Brand Names Mixture

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Tioguanin Chemical_Formula


Tioguanin RX_link


Tioguanin fda sheet

Tioguanin FDA

Tioguanin msds (material safety sheet)

Tioguanin MSDS

Tioguanin Synthesis Reference

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

Tioguanin Molecular Weight

167.193 g/mol

Tioguanin Melting Point

>360 oC

Tioguanin H2O Solubility

36.3 mg/mL

Tioguanin State


Tioguanin LogP


Tioguanin Dosage Forms

Oral tablets

Tioguanin Indication

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

Tioguanin 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).

Tioguanin Absorption

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

Tioguanin side effects and Toxicity

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

Tioguanin 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.

Tioguanin Organisms Affected

Humans and other mammals