Arzoxifene is a selective estrogen receptor modulator. It 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 third-generation SERM currently in Phase III clinical trials for the treatm ent of ER-positive recurrent/metastatic breast cancer. Similar to raloxifene, it is an ER antagonist in both breast and uterine tissues and an ER agonist on bone and the cardiovascular system. Arzoxifene is able to both preserve and build bone mineral density, which makes it a viable candidate for the treatment of osteoporosis. Ample evidence from early clinical trials indicates that arzoxifene also can be utilized as a chemopreventive agent against breast cancer.
Adverse effects include hot flashes (major) and headache, nausea, vomiting, and constipation (minor).
