Oltipraz

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.¹ It is an effective inducer of phase I and II detoxifying enzymes, including glutathione S-transferases, UDP-glucuronosyltransferases, NAD(P)H:quinone oxidoreductase, microsomal epoxide hydrolase, and aflatoxin aldehyde reductase.^1,2 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.¹ 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.³

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1. Kensler, T.W., Qian, G.S., Chen, J.G., et al. Translational strategies for cancer prevention in liver. Nat. Rev. Cancer 3(5), 321-329 (2003).

2. Iida, K., Itoh, K., Kumagai, Y., et al. Nrf2 is essential for the chemopreventive efficacy of oltipraz against urinary bladder carcinogenesis. Cancer Res. 64(18), 6424-6431 (2004).

3. Merrell, M.D., Jackson, J.P., Augustine, L.M., et al. The Nrf2 activator oltipraz also activates the constitutive androstane receptor. Drug Metab. Dispos. 36(8), 1716-1721 (2008).