COMPARATIVE PHARMACODYNAMIC ANALYSIS OF TAT-59 AND TAMOXIFEN IN RATS BEARING DMBA-INDUCED MAMMARY-CARCINOMA

Citation
T. Toko et al., COMPARATIVE PHARMACODYNAMIC ANALYSIS OF TAT-59 AND TAMOXIFEN IN RATS BEARING DMBA-INDUCED MAMMARY-CARCINOMA, Cancer chemotherapy and pharmacology, 37(1-2), 1995, pp. 7-13
Citations number
24
Language
INGLESE
art.tipo
Article
Categorie Soggetti
Pharmacology & Pharmacy",Oncology
ISSN journal
0344-5704
Volume
37
Issue
1-2
Year of publication
1995
Pages
7 - 13
Database
ISI
SICI code
0344-5704(1995)37:1-2<7:CPAOTA>2.0.ZU;2-7
Abstract
TAT-59 suppressed the growth fo DMBA-induced mammary tumors in rats ea rlier and more strongly than tamoxifen (TAM). After oral administratio n 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 bl ood compared to 4-OH-TAM, an active metabolite of TAM. In a 3-day anti uterotrophic test, every detected metabolite of TAT-59 showed stronger antiestrogenic activity than did TAM. In a competition assay, the aff inity of the metabolites for estrogen receptors ranged from that of es tradiol to that of TAM. These results suggest that the superior anties trogenic activity of TAT-59 compared to TAM was either due to its high er penetration into tumor tissue or to the stronger antiestrogenic act ivity of its metabolites.