テガフール

外観

白色～ほとんど白色粉末～結晶

用途

生体内でフルオロウラシルへ と代謝されて DNA 合成阻害を示します。

効能

抗悪性腫瘍薬, 代謝拮抗薬

商品名

フトラフール (大鵬薬品工業); フトラフール (大鵬薬品工業); フトラフール (大鵬薬品工業); フトラフール (大鵬薬品工業)

説明

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.

化学的特性

White Crystalline Powder

使用

Isotope labelled Tegafur (T013900), used as an antineoplastic.

安全性プロファイル

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.