Treatment with Bazedoxifene, a Selective Estrogen Receptor Modulator, Causes Regression of Endometriosis in a Mouse Model

Jaime Kulak, Catha Fischer, Barry Komm, Barry S. Komm, Hugh S Taylor
Endocrinology · 2011 · vol. 152(8) , pp. 3226–3232 · doi:10.1210/en.2010-1010 · PMID:21586552 · W2152300718
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Bazedoxifene treatment significantly reduced endometriosis implant size in mice by decreasing estrogen-mediated cell proliferation, without adverse ovarian effects.

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Abstract

Endometriosis is a common estrogen-dependent disorder. Medical treatments currently consist of progestins or GnRH agonists; however, neither is fully effective and both entail significant side effects. Selective estrogen receptor (ER) modulators (SERM) have tissue-selective actions, acting as an ER agonist in some tissues and ER antagonist in others. The SERM bazedoxifene (BZA) effectively antagonizes estrogen-induced uterine endometrial stimulation without countering estrogenic effects in bone or central nervous system. These properties make it an attractive candidate for use in the treatment of endometriosis. Experimental endometriosis was created in reproductive-age CD-1 mice. After 8 wk, 10 animals received i.p. injections of BZA (3 mg/kg·d) for 8 wk, whereas 10 received vehicle control. Mice were killed, and implant size was assessed. The mean size of the implants after treatment was 60 mm(2) in the control group and 21 mm(2) in the BZA treatment group (P = 0.03). Quantitative PCR and immunohistochemical analysis were used to determine the effect on endometrial gene expression. PCNA, ERα, and LIF mRNA and protein expression were significantly decreased in endometrium of the treated group. Caspase 3 mRNA expression was increased. Expression of PR and Hoxa10 were not significantly altered by treatment. There was no evidence of ovarian enlargement or cyst formation. Decreased PCNA and ER expression demonstrated that the regression of endometriosis likely involved decreased estrogen-mediated cell proliferation. BZA may be an effective novel agent for the treatment of endometriosis due to greater endometrial-specific estrogen antagonism compared with other SERM.
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SELEKTİF ESTROJEN RESEPTÖR MODÜLATÖRÜ OLAN BAZEDOKSİFENİN RAT MODELİNDE OLUŞTURULAN ENDOMETRİOZİS TEDAVİSİNDEKİ ROLÜ Öz Anahtar Kelimeler Kaynakça - Sidell N, Han SW, Parthasarathy S. Regulation and modulation of abnormal immune responses in endometriosis. Ann N Y Acad Sci 2002;955:159–73. 2. Wheeler JM, Malinak LR. Recurrent endometriosis: incidence, management, and prognosis. Am J Obstet Gynecol 1983; 146(3):247-53. - Taylor E, Williams C. Surgical treatment of endometriosis: location and patterns of disease at reoperation. Fertil Steril 2010; 93:57-61. - Kulak J Jr, Fischer C, Komm B, Taylor HS. Treatment with bazedoxifene, a selective estrogen receptor modulator, causes regression of endometriosis in a mouse model. Endocrinology 152(8):3226-32. 2011doi: 10.1210/en.2010-1010. Epub 2011 May 17. - Komm BS, Kharode YP, Modine PV, Harris HA, Miller CP, Lyttle CR. Bazedoxifene acetate: a selective estrogen receptor modulator with improved selectivity. Endocrinology 2005;146:3999-4008. - Ronkin S, Northington R, Baracat E, et al. Endometrial effects of bazedoxifene acetate, a novel selective estrogen receptor modulator, in postmenopausal women. Obstet Gynecol 2005;105(6):1397-404. - Morello KC, Wurz GT, DeGregorio MW. Pharmacokinetics of selective estrogen receptor modulators. Clin Pharmacokinet 2003;42:361-72. - Chris P. Spencer, MD, Edward P. Morris and Janice M. Selective estrogen receptor modulators: Women’s panacea for the next millennium? Am J Obstet Gynecol 1999; 180: 763-70. - Maeda K, Ohkura S, Tsukamura H. Physiology of the reproduction. In: Krinke GJ, editor. The laboratory rat (Handbook of experimental animals) London:Academic Press; 2000.p.148-149 Ayrıntılar Birincil Dil Türkçe Konular - Bölüm - Yazarlar Senem Mine Keskin Bu kişi benim Hacer Cavidan Gülerman Bu kişi benim Özlem Uzunlar Bu kişi benim Şebnem Özyer Bu kişi benim Ayla Aktulay Bu kişi benim Muzaffer Çaydere Bu kişi benim Yayımlanma Tarihi 1 Temmuz 2013 Gönderilme Tarihi - Kabul Tarihi - Yayımlandığı Sayı Yıl 2013 Cilt: 10 Sayı: 39

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Condition tags

mesh:D004715endometriosis

MeSH descriptors

Endometriosis Indoles Selective Estrogen Receptor Modulators Animals Caspase 3 Caspase 3 Disease Models, Animal Endometriosis Female Indoles Indoles Mice Proliferating Cell Nuclear Antigen Proliferating Cell Nuclear Antigen Receptors, Estrogen Receptors, Estrogen Selective Estrogen Receptor Modulators

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