Oltipraz: Clinical opportunities for cancer chemoprevention

Thomas W. Kensler, Kathy J. Helzlsouer

Research output: Contribution to journalArticlepeer-review


Oltipraz [4‐methyl‐5‐(2‐pyrazinyl)‐1,2‐dithiole‐3‐thione], orginally developed as an antischistosomal agent, protects against chemical carcinogenesis in lung, trachea, forestomach, small intestine, colon, breast, skin, liver and urinary bladder in rodents. Oltipraz induces electrophile detoxication enzymes, resulting in diminished carcinogen‐DNA adduct formation and reduced cytotoxicity, an important component of anticarcinogenic actions. Phase I trials of this drug have been recently conducted in the United States and indicate that the maximum tolerated dose is about 125 mg/day over a six‐month period. Grade I/II dose‐limiting toxicities included photosensitivity/heat intolerance, gastrointestinal, and neurologic toxicities. Ongoing studies are monitoring relationships between dose scheduling, drug plasma concentrations and pharmacodynamic action. Subsequent trials with this agent might most appropriately target individuals at high risk for occupational or environmental exposures to genotoxic carcinogens. Towards this end, a randomized, placebo‐controlled Phase II study is planned for people at high risk for exposure to aflatoxins and development of hepatocellular carcinoma. Modulation of biomarkers reflecting the biologically effective dose of aflatoxin will serve as study endpoints.

Original languageEnglish (US)
Pages (from-to)101-107
Number of pages7
JournalJournal of cellular biochemistry
Issue number22 S
StatePublished - 1995


  • Aflatoxin B
  • antischistosomiasis
  • carcinogen detoxication
  • enzyme induction
  • glutathione S‐transferases
  • hepatocellular carcinoma

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Biology
  • Cell Biology


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