azalanstat

Azalanstat is a synthetic imidazole compound that acts as a lanosterol 14α-demethylase (a cytochrome P450 enzyme) inhibitor. It has been shown to inhibit cholesterol synthesis in HepG2 cells, human fibroblasts, hamster hepatocytes, and hamster liver by targeting the cytochrome P450 enzyme lanosterol 14 alpha-demethylase. In animal studies, azalanstat lowered serum cholesterol in a dose-dependent manner, with a preferential reduction of low density lipoprotein (LDL) cholesterol and apolipoprotein B relative to high density lipoprotein (HDL) cholesterol and apolipoprotein A-1. It also indirectly inhibited hepatic microsomal HMG-CoA reductase activity, possibly at a post-transcriptional step, and stimulated hepatic cholesterol 7α-hydroxylase activity. Azalanstat reached the preclinical phase for the treatment of hyperlipidemia and possibly obesity, but development was discontinued and no marketing approvals are reported[1][3][4][5][7][9].

Other names

azalanstat dihydrochlorideazalanstat mesylate