Thioguanine
- Atc Codes:L01BB03
- CAS Codes:154-42-7#5580-03-0
- PHARMGKB ID:154-42-7#5580-03-0
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Austria: Thioguanin; Belgium: Lanvis; Czech Republic: Lanvis; Estonia: Lanvis; France: Lanvis; Germany: Thioguanin, Thioguanine; Greece: Lanvis, Thioguanine; Ireland: Lanvis; Italy: Tioguanina; Latvia: Lanvis; Lithuania: Lanvis; Netherlands: Lanvis; Poland: Lanvis; Romania: Lanvis; Slovakia: Lanvis; Spain: Tioguanina; Sweden: Lanvis; UK: Lanvis.
North America
Canada: Lanvis; USA: Thioguanine.
Latin America
Argentina: Lanvis; Brazil: Lanvis.
Drug combinations
Chemistry
Thioguanine: C~5~H~5~N~5~S xH~2~O. Mw: 167.19 (anhydrous). (1) 6H-Purine-6-thione, 2-amino-1,7-dihydro-; (2) 2-Aminopurine-6(1H)-thione. CAS-154-42-7; CAS-5580-03-0 (hemihydrate)(1965).
Pharmacologic Category
Antineoplastic Agents; Antimetabolites; Purine Antagonist. (ATC-Code: L01BB03).
Mechanism of action
Purine analog incorporated into DNA and RNA resulting in blockage of synthesis and metabolism of purine nucleotides.
Therapeutic use
Treatment of acute myelogenous (nonlymphocytic) leukemia. Treatment of chronic myelogenous leukemia and granulocytic leukemia.
Pregnancy and lactiation implications
Potentially teratogenic. Excretion in breast milk unknown (use caution).
Unlabeled use
Contraindications
Hypersensitivity to thioguanine or any component of the formulation. Pregnancy.
Warnings and precautions
Myelosuppression is a common dose-related toxicity (may be delayed). Patients with genetic deficiency of thiopurine methyltransferase (TPMT) or who are receiving drugs which inhibit this enzyme (mesalazine, olsalazine, sulfasalazine) may be highly sensitive to myelosuppressive effects. Not recommended for long-term continuous therapy due to potential for hepatotoxicity (hepatic veno-occlusive disease). Potentially carcinogenic. Use with caution in hepatic and renal impairment. Caution with history of previous therapy resistance with either thioguanine or mercaptopurine (there is usually complete cross-resistance between these two).