Oltipraz, originally identified as an antischistosomiasis agent, is a potent anticarcinogen in a variety of animal models of cancer at concentrations of ~200 mg/kg. It is an effective inducer of phase I and II detoxifying enzymes, including glutathione S-tranferases, UDP-glucuronosyltransferases, NAD(P)H:quinone oxidoreductase, microsomal epoxide hydrolase, and aflatoxin aldehyde reductase. Induction of these metabolic enzymes by oltipraz has been linked to the transcription factor nuclear factor E2-related factor 2 and its activation of the antioxidant response element. In mice, oltipraz at 150 mg/kg can also induce expression of CYP2B, a gene regulated by the constitutive androstane receptor, a transcription factor important in the detoxification of endobiotic and xenobiotic substances.
