thioguanine

Thioguanine is a purine antimetabolite and a guanine analogue used primarily in the treatment of acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML). It acts as a prodrug that is converted intracellularly into thioguanine nucleotides, which are subsequently incorporated into DNA and RNA. This incorporation triggers DNA damage responses and inhibits de novo purine synthesis, ultimately leading to cell cycle arrest and apoptosis. In the context of the Alliance for Clinical Trials in Oncology (formerly CALGB), thioguanine has been evaluated as part of intensive, pediatric-inspired chemotherapy regimens (such as the CALGB 10403 protocol) for adolescents and young adults with untreated ALL to improve outcomes compared to traditional adult protocols.

Brand names

Tabloid

Other names

tioguanine2-amino-6-mercaptopurine2-amino-1,7-dihydro-6H-purine-6-thione