HOMEPRODUCTSCOMPANYCONTACTFAQResearchDictionaryPharmaSign Up FREE or Login

Tiazofurin: a new antitumor agent.

Abstract
Tiazofurin is an interesting drug now entering Phase I trials, with marked preclinical antitumor activity against P388 and L1210 leukemias, and the Lewis lung carcinoma. Schedule dependency favoring frequent administration has been noted. The drug has a novel mechanism of action, being metabolized to an inhibitory cofactor of inosine monophosphate dehydrogenase. Tiazofurin is widely distributed after i.v. administration exhibiting a triphasic pattern of plasma decay, with a terminal half-life of 3-16 h in the three species studied. Approximately 90% of the drug was excreted unchanged in the urine within 24 h. A significant potential for the slower release of intracellularly retained drug exists. Anticipated organ toxicities based on the studies described include myelotoxicity, hepatotoxicity and nephrotoxicity. These were mild and reversible at lower doses, and were not seen at levels corresponding to the starting doses in man. A potential for hyperuricemia exists; this should be easily controllable by the use of allopurinol, without compromising the drug's antitumor effect. Phase I trials under the sponsorship of the NCI are underway in a number of institutions.
AuthorsP J O'Dwyer, D D Shoemaker, H N Jayaram, D G Johns, D A Cooney, S Marsoni, L Malspeis, J Plowman, J P Davignon, R D Davis
JournalInvestigational new drugs (Invest New Drugs) Vol. 2 Issue 1 Pg. 79-84 ( 1984) ISSN: 0167-6997 [Print] United States
PMID6381381 (Publication Type: Journal Article, Review)
Chemical References
  • Antineoplastic Agents
  • Ribonucleosides
  • Uric Acid
  • Ribavirin
  • tiazofurin
Topics
  • Animals
  • Antineoplastic Agents (adverse effects, pharmacology, toxicity)
  • Humans
  • Mice
  • Ribavirin (adverse effects, analogs & derivatives, pharmacology, toxicity)
  • Ribonucleosides (pharmacology)
  • Uric Acid (blood)

Join CureHunter, for free Research Interface BASIC access!

Take advantage of free CureHunter research engine access to explore the best drug and treatment options for any disease. Find out why thousands of doctors, pharma researchers and patient activists around the world use CureHunter every day.
Realize the full power of the drug-disease research graph!


Choose Username:
Email:
Password:
Verify Password:
Enter Code Shown: