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

doi:10.1007/BF00685623

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 journal › Article › peer-review

4 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 language	English
Pages (from-to)	7-13
Number of pages	7
Journal	Cancer Chemotherapy and Pharmacology
Volume	37
Issue number	1-2
DOIs	https://doi.org/10.1007/BF00685623
Publication status	Published - 1995 Jan 1
Externally published	Yes

Keywords

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

ASJC Scopus subject areas

Oncology
Toxicology
Pharmacology
Cancer Research
Pharmacology (medical)

UN SDGs

This output contributes to the following UN Sustainable Development Goals (SDGs)

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10.1007/BF00685623

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

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.",

keywords = "Anti-estrogenic activity, DMBA-induced mammary tumor, Pharmacodynamics, TAT-59",

author = "Toshiyuki Toko and Jiro Shibata and Yoshikazu Sugimoto and Hidetoshi Yamaya and Masahiko Yoshida and Kazuo Ogawa and Eiji Matsushima",

year = "1995",

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doi = "10.1007/BF00685623",

language = "English",

volume = "37",

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T1 - Comparative pharmacodynamic analysis of TAT-59 and tamoxifen in rats bearing DMBA-induced mammary carcinoma

AU - Toko, Toshiyuki

AU - Shibata, Jiro

AU - Sugimoto, Yoshikazu

AU - Yamaya, Hidetoshi

AU - Yoshida, Masahiko

AU - Ogawa, Kazuo

AU - Matsushima, Eiji

PY - 1995/1/1

Y1 - 1995/1/1

N2 - 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.

AB - 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.

KW - Anti-estrogenic activity

KW - DMBA-induced mammary tumor

KW - Pharmacodynamics

KW - TAT-59

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ER -

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

Abstract

Keywords

ASJC Scopus subject areas

UN SDGs

Access to Document

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