Tegafur is an orally bioavailable prodrug form of 5-fluorouracil (5-FU; ). It is converted to 5-FU in vivo enzymatically or by cytochrome P450 oxidation. Tegafur inhibits proliferation of HT-29, BxPC-3, and Panc02 cells (IC50s = 201, 172, and 179 μM, respectively). It also reduces tumor growth in an HT-27 colon carcinoma mouse xenograft model when administered at a dose of 50 mg/kg and in a 4-1ST gastric carcinoma mouse xenograft model when used in combination with uracil. Formulations containing tegafur, in combination with uracil, have been used in the treatment of cancer.
화학적 성질
White Crystalline Powder
용도
Isotope labelled Tegafur (T013900), used as an antineoplastic.
Safety Profile
Poison by ingestion.
Moderately toxic to humans by intravenous
route. Moderately toxic experimentally by
intraperitoneal, intravenous, and
subcutaneous routes. Experimental
teratogenic data. Human systemic effects:
nausea and vomiting. Experimental
reproductive effects. Questionable human
carcinogen producing gastrointestinal
tumors. Human mutation data reported.
Used as an anti-cancer agent. When heated
to decomposition it emits very toxic fumes
of Fand NOx.
