Class/mechanism: Purine (guanine) analog, antimetabolite that interferes with DNA synthesis. Thioguanine competes with hypoxanthine and guanine for the enzyme hypoxanthine-guanine phosphoribosyltransferase (HGPRTase) and is converted to 6-thioguanylic acid (TGMP). TGMP interferes with several processes involving the synthesis of guanine nucleotides. It exerts pseudo-feedback inhibition of glutamine-5-phosphoribosylpyrophosphate amidotransferase, an early enzyme in the de novo pathway for purine ribonucleotide synthesis. TGMP is a competitive inhibitor of inosinic acid (IMP) dehydrogenase, interfering with the conversion of IMP to xanthylic acid (XMP). Thioguanylic acid is converted to thioguanosine diphosphate (TGDP) and thioguanosine triphosphate (TGTP), and they are eventually incorporated into RNA and DNA, which may cause additional cytotoxicity. Thioguanine is structurally and functionally similar to Mercaptopurine (6-MP).
For conciseness and simplicity, HemOnc.org currently will focus on treatment regimens and not list information such as: renal/hepatic dose adjustments, metabolism (including CYP450), excretion, monitoring parameters (although this will be considered for checklists), or manufacturer. Instead, for the most current information, please refer to your preferred pharmacopeias such as Micromedex, Lexicomp, UpToDate (courtesy of Lexicomp), or the prescribing information.
Diseases for which it is used
- Acute myeloid leukemia
- Acute promyelocytic leukemia
- B-cell acute lymphoblastic leukemia
- Waldenström macroglobulinemia
Patient drug information
- Thioguanine (Tabloid) patient drug information (Chemocare)
- Thioguanine (Tabloid) patient drug information (UpToDate)
History of changes in FDA indication
- 1/18/1966: Initial FDA approval
Also known as
- Generic names: 6-TG, 6-thioguanine, 2-Amino-6-Mercaptopurine
- Brand name: Tabloid