Unii-0789652qul

プロパティ

安全情報

説明

Mivotilate is an orally-active hepatoprotective agent introduced for the treatment of liver cirrhosis and hepatitis-B infection. It is a dithietanylidene malonate analogue of malotilate and is without the haemotological adverse effects associated with the latter. Mivotilate can be obtained by partial saponification of the corresponding diisopropylmalonate, conversion of the acid function into mixed anhydride then to the amide with an aminothiazole. It displays potent hepatoprotective activity in rat and mice liver injury models by a mechanism involving the inactivation of Kupffer cells. Mivotilate was shown to exert multiple effects on the hepatic cytochrome P450 system, particularly to inhibit CYP2E1 expression and to up-regulate the CYP1A1 expression. The low oral bioavailability of Mivotilate in rats (F<0.22%) could be primarilly attributed to poor absorption and considerable hepatic and gastrointestinal first-pass effects. Mivotilate prevents mutagenesis caused by agents such as benzo[a]pyrene and reduces skin tumors induced by these agents.