Drug intelligence / Profile preview

tioguanine

Development stage
Approved
Lead developer
Glaxo Wellcome
Modality
Small Molecules
Administration
Oral
01

Overview

Tioguanine (also known as thioguanine) is a purine analog antineoplastic agent primarily used to treat acute myeloid leukemia (AML) and other types of leukemia. It works by interfering with DNA and RNA synthesis in cancer cells, which helps stop their growth and multiplication. It is a pro-drug that requires intracellular activation. Once inside cells, it's converted to thioguanine monophosphate (TGMP) by the enzyme hypoxanthine-guanine phosphoribosyl transferase (HGPRT). TGMP is further converted to di- and triphosphates, which are then incorporated into DNA, disrupting normal cell replication. This mechanism makes it specific for the S phase of the cell cycle and has some immunosuppressive activity.

Brand names
TabloidLanvis
Other names
thioguanine6-thioguanine2-amino-6-mercaptopurine2-amino-6-purinethiol2-aminopurin-6-thiol2-aminopurine-6-thiol6-mercaptoguanine6-mercapto-2-aminopurine
02

Targets

DNAHPRT1 (Hypoxanthine-guanine phosphoribosyltransferase)PPAT (Amidophosphoribosyltransferase)IMPDH (Inosine-5'-monophosphate dehydrogenase 1)

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