Drug intelligence / Profile preview

tioguanine (Wellcome Research Laboratories)

Development stage
Approved
Lead developer
GSK
Modality
Small Molecules
Administration
Oral
01

Overview

Tioguanine is a synthetic thiopurine antimetabolite and guanine analogue developed at Wellcome Research Laboratories. After intracellular activation to thioguanine nucleotides, it is incorporated into DNA and RNA and inhibits de novo purine synthesis, disrupting nucleic-acid synthesis and causing cytotoxicity. The exact record refers to **oral tioguanine** investigated by Memorial Sloan Kettering Cancer Center in a Phase II sequential-treatment study after intravenous methotrexate for relapsed or resistant Hodgkin lymphoma; methotrexate is a separate co-administered study drug, not part of tioguanine itself. Tioguanine is marketed as Tabloid and is FDA-approved for acute myeloid leukemia. ([clinicaltrials.gov](https://clinicaltrials.gov/study/NCT00587873))

Brand names
LanvisTabloid
Other names
2-amino-1,7-dihydro-6H-purine-6-thione2-amino-6-mercaptopurine6-TG6-thioguaninethioguanine
02

Targets

MSH2 (DNA mismatch repair protein MSH2)DNAHPRT1 (Hypoxanthine-guanine phosphoribosyltransferase)

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