Bitertanol (KWG 0599) is a triazole fungicide. Bitertanol inhibits demethylation, disrupts membrane function, and prevents sterol synthesis.

Bitertanol (10, 25, and 100 mg/kg) produced 2-, 4-, and 14-fold increases of 7-ethoxyresorufin O-deethylation activity in liver microsomes, respectively. Bitertanol (25 mg/kg) increased CYP1A1 protein in the liver, kidney, and lung by 10-, 13-, and 17-fold, respectively. Bitertanol produced smaller increases of CYP2B and CYP3A catalytic activity and protein than that of CYP1A1 in liver. Additions of 0.01-100 microM Bitertanol to liver microsomes from rats Bitertanol (25 mg/kg) inhibited microsomal 7-ethoxyresorufin O-demethylation activity (IC50=0.8 microM). Bitertanol (100 mg/kg) increased liver UDP-glucuronosyltransferase and glutathione S-transferase activities by 2-fold. Bitertanol (25 mg/kg) produced a minor increase in metabolic activation of benzo[a]pyrene by liver S-9 fraction in the Ames mutagenicity test while the increase was blocked by addition of 100 microM Bitertanol[2].