Oltipraz Background

Oltipraz is a synthetic, commissioned 1,2-dithiole-3-thione originally acclimated in bodies as an antischistosomal agent. Beastly studies accept approved that oltipraz is a almighty inducer of Phase II detoxification enzymes, a lot of conspicuously glutathione-S-transferase (GST).

Oltipraz has been classified as a monofunctional inducer back it advantageously elevates Phase II detoxification enzymes, while alone hardly altering the announcement of the Phase I “activating” enzymes. Oltipraz finer induced quinone reductase in Hepa 1c1c7 beef abnormal in the aryl hydrocarbon receptor action appropriate by bifunctional inducers.

Dietary concentrations of oltipraz aftermath abundant inhibition of aflatoxin B1-induced hepatic tumorigenesis in rats. Levels of hepatic aflatoxin-DNA adducts and serum aflatoxin-albumin adducts decreased if biliary abolishment of aflatoxin-glutathione conjugants increased, accordingly accouterment predictive biomarkers that abstinent a chemopreventive effect. In added beastly studies, oltipraz was begin to arrest chemically induced carcinogenesis in bladder, colon, breast, stomach, and derma blight models.

In a Phase I study, a individual articulate dosage of oltipraz was accustomed to accustomed volunteers at dosage levels of 125, 250, 375, and 500 mg. There was no cogent aberration in half-life amid the four dosage levels nor in approval at the 125 and 250 mg levels. A alternation of baby trials evaluating individual articulate doses of oltipraz for up to 28 canicule aswell showed a abbreviate t1/2 (4.1-5.3 hours), a abiding abiding accompaniment afterwards aberration afterwards a loading dose, and added serum and urine concentrations with burning of a high-fat diet.