Arzoxifene, a new selective estrogen receptor modulator for chemoprevention of experimental breast cancer.

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Suh N, Glasebrook AL, Palkowitz AD, Bryant HU, Burris LL, Starling JJ, Pearce HL, Williams C, Peer C, Wang Y, Sporn MB

Arzoxifene, a new selective estrogen receptor modulator for chemoprevention of experimental breast cancer.

Cancer Res. 2001 Dec 1;61(23):8412-5.

PubMed ID
11731420 [ View in PubMed
]
Abstract

Arzoxifene ([6-hydroxy-3-[4-[2-(1-piperidinyl)-ethoxy]phenoxy]-2-(4-methoxyphenyl)]benzo[b]t hiophene) is a selective estrogen receptor modulator (SERM) that is a potent estrogen antagonist in mammary and uterine tissue while acting as an estrogen agonist to maintain bone density and lower serum cholesterol. Arzoxifene is a highly effective agent for prevention of mammary cancer induced in the rat by the carcinogen nitrosomethylurea and is significantly more potent than raloxifene in this regard. Arzoxifene is devoid of the uterotrophic effects of tamoxifen, suggesting that, in contrast to tamoxifen, it is unlikely that the clinical use of arzoxifene will increase the risk of developing endometrial carcinoma.

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