oltipraz

Oltipraz is a synthetic dithiolethione compound with potential chemopreventive and anti-angiogenic properties. It functions as a Nrf2 activator, which binds to antioxidant response elements (AREs) and induces Phase-I and Phase-II drug-metabolizing enzymes including CYP2B and NQO1. Oltipraz affects the metabolism and disposition of chemical carcinogens, principally through the induction of electrophile detoxication enzymes. It also increases mRNA levels of multiple hepatic xenobiotic transporters and elevates expression of genes encoding anti-oxidant and multidrug resistance-associated proteins. Originally developed by Rhône-Poulenc (later Sanofi/sanofi-aventis) as an antischistosomal drug, oltipraz has been investigated for cancer prevention in various tissues including bladder, blood, colon, kidney, liver, lung, pancreas, stomach, trachea, skin, and mammary tissue. It has also been studied for liver fibrosis, liver cirrhosis, and non-alcoholic fatty liver disease.

Other names

4-Methyl-5-(2-pyrazinyl)-1,2-dithiole-3-thione4-methyl-5-(2-pyrazinyl)-3H-1,2-dithiole-3-thione