Thioguanine

FDA label, Waylis Therapeutics LLC, oral, effective 2025-01-08. Full label on DailyMed

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Quoted from the FDA label. Product labels differ by manufacturer and change over time; confirm against the label for the product you are using.

Handling and access

NIOSH hazardous drug

Table 1

NIOSH lists thioguanine as a hazardous drug. AHFS class: 10:00 antineoplastic agents.

  • The package insert includes manufacturer's special handling information (MSHI). Follow it when preparing, administering, and disposing of this drug.

Handle with the precautions your facility uses for hazardous drugs (USP <800>). NIOSH's Managing Hazardous Drug Exposures lists controls by drug form and activity.

Source: NIOSH List of Hazardous Drugs in Healthcare Settings, 2024December 2024, updates through Jul 17, 2025

Dosing in kidney impairment

This label has no separate kidney-impairment dosing section. Check warnings and clinical pharmacology in the full label.

Drug interactions

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Label text (1 paragraph)

Drug Interactions There is usually complete cross-resistance between PURINETHOL (mercaptopurine) and TABLOID brand Thioguanine. As there is in vitro evidence that aminosalicylate derivatives (e.g., olsalazine, mesalazine, or sulphasalazine) inhibit the TPMT enzyme, they should be administered with caution to patients receiving concurrent thioguanine therapy (see WARNINGS).

Contraindications

Thioguanine should not be used in patients whose disease has demonstrated prior resistance to this drug. In animals and humans, there is usually complete cross-resistance between PURINETHOL (mercaptopurine) and TABLOID brand Thioguanine.

Safety data

Reported adverse events (FAERS)

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Source: FDA Adverse Event Reporting System via openFDA

Liver injury (LiverTox)

A

Likelihood score A: Well known cause of clinically apparent liver injury.

Thioguanine (also referred to as 6-thioguanine and as tioguanine) is a purine analogue that is used in the therapy of acute and chronic myelogenous leukemias. Thioguanine therapy is associated with minor, usually transient and asymptomatic elevations in serum aminotransferase levels and has also been linked to rare instances of cholestatic acute liver injury and to chronic liver injury, resulting in portal hypertension due to nodular regenerative hyperplasia.

ABCDEA: well known cause; E: unlikely cause. [HD]: high doses only.

Source: LiverTox: Thioguanine (NIDDK, public domain)Chapter updated Aug 17, 2017

Pregnancy and lactation

Pregnancy

Pregnancy Drugs such as thioguanine are potential mutagens and teratogens. Thioguanine may cause fetal harm when administered to a pregnant woman. Thioguanine has been shown to be teratogenic in rats when given in doses 5 times the human dose. When given to the rat on the 4th and 5th days of gestation, 13% of surviving placentas did not contain fetuses, and 19% of offspring were malformed or stunted. The malformations noted included generalized edema, cranial defects, and general skeletal hypoplasia, hydrocephalus, ventral hernia, situs inversus, and incomplete development of the limbs. There are no adequate and well-controlled studies in pregnant women.

If this drug is used during pregnancy, or if the patient becomes pregnant while taking the drug, the patient should be apprised of the potential hazard to the fetus. Women of childbearing potential should be advised to avoid becoming pregnant. Pregnancy Teratogenic Effects: See WARNINGS section.

Lactation

Lactation It is not known whether this drug is excreted in human milk. Because of the potential for tumorigenicity shown for thioguanine, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.

Breastfeeding (LactMed)

Thioguanine nucleosides are active intracellular metabolites of azathioprine and have been measured in breastmilk and in infant serum following maternal use of azathioprine as an immunosuppressant. Thioguanine levels in milk are low after immunosuppressant doses of the drug or of azathioprine. It might be desirable to monitor exclusively breastfed infants with a complete blood count with differential, and liver function tests if thioguanine is used during lactation, although some authors feel that monitoring is unnecessary. Most sources consider the thiopurines acceptable to use in low, immunosuppressant doses. Most sources consider breastfeeding to be contraindicated during maternal antineoplastic drug therapy, although antimetabolites such as thioguanine appear to pose the least risk to breastfed infants.

Source: LactMed: Thioguanine (NICHD, public domain)Revised Feb 15, 2024

Supply and cost

Drug shortage status

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Recalls (last 24 months)

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Therapeutic equivalence (Orange Book)

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Price ladder

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These are not what a patient pays at the pharmacy counter. They are what pharmacies, health plans, and government buyers pay, before manufacturer rebates. A patient's cost depends on their insurance (copay, coinsurance, or deductible) or the pharmacy's cash price.

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