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Tioguanine Brand names, Tioguanine Analogs

Tioguanine Brand Names Mixture

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Tioguanine Chemical_Formula


Tioguanine RX_link


Tioguanine fda sheet

Tioguanine FDA

Tioguanine msds (material safety sheet)

Tioguanine MSDS

Tioguanine Synthesis Reference

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

Tioguanine Molecular Weight

167.193 g/mol

Tioguanine Melting Point

>360 oC

Tioguanine H2O Solubility

36.3 mg/mL

Tioguanine State


Tioguanine LogP


Tioguanine Dosage Forms

Oral tablets

Tioguanine Indication

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

Tioguanine 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).

Tioguanine Absorption

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

Tioguanine side effects and Toxicity

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

Tioguanine 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.

Tioguanine Organisms Affected

Humans and other mammals