Bazedoxifene Acetate

Bazedoxifene acetate is a third-generation SERM. In in vitro studies bazedoxifene competitively inhibited 17y0-estradiol binding to both ERa (Ki = 0.1 nM) and ER/3 (Ki = 0.03 nM). Bazedoxifene s ability to competitively bind to ERs... 

Bodine, P.V.N., Harris, H.A., Miller, C.P. and Lyttle, C.R. (2005) Bazedoxifene acetate a selective estrogen receptor modulator with improved selectivity. Endocrinology, 146, 3999-4008. 

Constantine, G. and Pickar, J.H. (2005) Endometrial effects of bazedoxifene acetate, a novel selective estrogen receptor modulator, in postmenopausal women. Obstetrics and Gynecology, 105,1397-1404. 

A Bischler-Mohlau indole synthesis was also pivotal in constructing the indole ring of bazedoxifene acetate (Viviant), Wyeth s novel and highly selective indole estrogen. It is a selective estrogen receptor modulator (SERM) for the treatment of and prevention of osteoporosis. It was found... 

Ethun KF, Wood CE, Cline JM, Register TC, Appt SE, Clarkson TB. Endometrial profile of bazedoxifene acetate alone and in combination with conjugated equine estrogens in a primate model. Menopause 2013 20(7) 777-84. 

---