Oltipraz

Oltipraz is a synthetic organosulfur compound belonging to the dithiolethione class. It was developed as a chemopreventive agent with the aim of reducing cancer risk by enhancing the body's detoxification pathways. The compound is known to induce phase II detoxifying enzymes, including glutathione S-transferases, NAD(P)H:quinone oxidoreductase 1, and UDP-glucuronosyltransferases, largely through activation of the Nrf2 signaling pathway. By upregulating these enzymes, oltipraz promotes the conjugation and elimination of electrophilic carcinogens and their metabolites, potentially lowering DNA adduct formation in liver and other tissues.

Clinical research has evaluated oltipraz as a cancer chemopreventive agent, particularly in populations with high exposure to aflatoxins. Trials have reported enzyme induction and reductions in certain biomarkers of exposure, such as aflatoxin–DNA adducts, but results on cancer incidence and long-term outcomes have been inconsistent. As a result, oltipraz has not become a broadly approved preventive therapy for cancer and is generally studied within experimental or trial settings rather than as a standard clinical intervention.

Safety considerations noted in trials include gastrointestinal symptoms and skin rashes. Long-term safety data remain limited, and the use of oltipraz for public health chemoprevention has not progressed to widespread implementation in most regions. Mechanistically, it remains of interest for understanding how activating phase II detoxification pathways might contribute to reducing carcinogen burden, but its role in routine clinical practice is not established.

Oltipraz is part of the broader class of dithiolethione derivatives studied for chemoprevention and modulating detoxification enzymes through the Nrf2 pathway.