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

Toshiyuki Toko, Jiro Shibata, Yoshikazu Sugimoto, Hidetoshi Yamaya, Masahiko Yoshida, Kazuo Ogawa, Eiji Matsushima

Research output: Contribution to journalArticle

13 Citations (Scopus)

Abstract

TAT-59 suppressed the growth fo 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.

Original languageEnglish
Pages (from-to)7-13
Number of pages7
JournalCancer Chemotherapy and Pharmacology
Volume37
Issue number1-2
DOIs
Publication statusPublished - 1995 Jan 1
Externally publishedYes

Keywords

  • Anti-estrogenic activity
  • DMBA-induced mammary tumor
  • Pharmacodynamics
  • TAT-59

ASJC Scopus subject areas

  • Oncology
  • Toxicology
  • Pharmacology
  • Cancer Research
  • Pharmacology (medical)

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