Chemopreventive activity of oltipraz

Pharmacol Ther. 1998 Apr;78(1):17-27. doi: 10.1016/s0163-7258(97)00164-2.


The antischistosomal agent oltipraz [5-(2-pyrazinyl)-4-methyl-1,2-dithiol-3-thione] has been shown to inhibit chemically induced carcinogenesis in a variety of animal models. Of greatest interest is its unique ability to protect several target organs from structurally diverse carcinogens. Molecular and biochemical studies suggest that oltipraz affords cellular protection by inducing the expression of a battery of Phase II detoxification enzymes. Induction of glutathione S-transferase, gamma-glutamylcysteine synthetase and DT-diaphorase has been observed in human tissues following the administration of a single oral dosage of oltipraz. Preclinical and clinical data continue to support the development of oltipraz as a chemopreventive agent for clinical usage.

Publication types

  • Review

MeSH terms

  • Administration, Oral
  • Animals
  • Anticarcinogenic Agents / pharmacology*
  • Anticarcinogenic Agents / therapeutic use
  • Biological Availability
  • Clinical Trials, Phase I as Topic
  • Clinical Trials, Phase II as Topic
  • Enzyme Induction / drug effects
  • Glutamate-Cysteine Ligase / biosynthesis
  • Glutathione Transferase / biosynthesis
  • Humans
  • NAD(P)H Dehydrogenase (Quinone) / biosynthesis
  • Pyrazines / pharmacology*
  • Pyrazines / therapeutic use
  • Reverse Transcriptase Inhibitors / pharmacology*
  • Reverse Transcriptase Inhibitors / therapeutic use
  • Schistosomicides / pharmacology*
  • Schistosomicides / therapeutic use
  • Thiones
  • Thiophenes
  • Tissue Distribution


  • Anticarcinogenic Agents
  • Pyrazines
  • Reverse Transcriptase Inhibitors
  • Schistosomicides
  • Thiones
  • Thiophenes
  • oltipraz
  • NAD(P)H Dehydrogenase (Quinone)
  • Glutathione Transferase
  • Glutamate-Cysteine Ligase