Although existing ER-α-targeted SERMs, such as tamoxifen, raloxifene, ICI 164,384 and ICI 182,780, have achieved evidenced therapeutic effects, the situation that SERMs are now mainly developed for osteoporosis treatment and have not yet been widely approved for breast cancer treatment [5] prompts researchers and clinicians to explore novel ER-α modulators. This evidence concerns the gene ESR1 and osteoporosis.