Drug intelligence / Profile preview

tiazofurin

Development stage
Discontinued
Lead developer
National Cancer Institute
Modality
Small Molecules
Administration
Intravenous
01

Overview

Tiazofurin is a synthetic nucleoside analogue and small molecule antineoplastic agent. It is metabolized intracellularly to thiazole‐4‐carboxamide adenine dinucleotide (TAD), an analogue of NAD, which acts as a potent and selective inhibitor of inosine monophosphate dehydrogenase (IMPDH). IMPDH is the rate-limiting enzyme in de novo purine synthesis; its inhibition leads to reduced guanylate levels, thereby impeding tumor cell growth. Tiazofurin was investigated for cancer treatment, particularly chronic myeloid leukemia (CML), but development was discontinued due to side effects such as pleuropericarditis and flu-like syndrome. The drug also exhibits antiviral activity and may be considered for emerging viral diseases[1][2][3][5][6].

Other names
tiazofurinetiazofurinumtiazofurinariboxamide2-beta-D-ribofuranosylthiazole-4-carboxamide2-(β-D-ribofuranosyl)-4-thiazolecarboxamide2-ribofuranosylthiazole-4-carboxamideTCAR
02

Targets

IMPDH (Inosine-5'-monophosphate dehydrogenase 1)

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