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Comparative pharmacodynamic analysis of TAT-59 and tamoxifen in rats bearing DMBA-induced mammary carcinoma.

Abstract
TAT-59 suppressed the growth of DMBA-induced mammary tumors in rats earlier and more strongly than tamoxifen (TAM). After oral administration of the drugs, DP-TAT-59, one of the main metabolites of TAT-59, was found in 10- to 15-fold higher concentrations in both the tumor and blood compared to 4-OH-TAM, an active metabolite of TAM. In a 3-day antiuterotrophic test, every detected metabolite of TAT-59 showed stronger antiestrogenic activity than did TAM. In a competition assay, the affinity of the metabolites for estrogen receptors ranged from that of estradiol to that of TAM. These results suggest that the superior antiestrogenic activity of TAT-59 compared to TAM was either due to its higher penetration into tumor tissue or to the stronger antiestrogenic activity of its metabolites.
AuthorsT Toko, J Shibata, Y Sugimoto, H Yamaya, M Yoshida, K Ogawa, E Matsushima
JournalCancer chemotherapy and pharmacology (Cancer Chemother Pharmacol) Vol. 37 Issue 1-2 Pg. 7-13 ( 1995) ISSN: 0344-5704 [Print] Germany
PMID7497599 (Publication Type: Comparative Study, Journal Article)
Chemical References
  • Antineoplastic Agents, Hormonal
  • Estrogen Antagonists
  • Receptors, Estrogen
  • Tamoxifen
  • TAT 59
  • Estradiol
  • 9,10-Dimethyl-1,2-benzanthracene
Topics
  • 9,10-Dimethyl-1,2-benzanthracene
  • Animals
  • Antineoplastic Agents, Hormonal (pharmacokinetics)
  • Binding, Competitive
  • Estradiol (metabolism)
  • Estrogen Antagonists (pharmacokinetics)
  • Female
  • Mammary Neoplasms, Experimental (chemistry, drug therapy)
  • Rats
  • Rats, Sprague-Dawley
  • Receptors, Estrogen (analysis)
  • Tamoxifen (analogs & derivatives, pharmacokinetics, therapeutic use)

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