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The Sound of Evolution
Raloxifene
雷洛昔芬
Mechanism of action:
Raloxifene 是一種選擇性雌激素受體調節劑（selective estrogen receptor modulator），屬於苯並噻吩類（benzothiophene）衍生物。Raloxifene 可與雌激素受體（estrogen receptor） ERα 與 ERβ 結合，但會誘導受體產生與雌二醇不同的構形變化，而在不同組織產生不同效果。比如抑制破骨細胞（osteoclast）活性，減少骨吸收，增加骨密度；抑制雌激素受體介導的細胞增殖，降低雌激素受體陽性乳癌風險；抑制子宮內膜增生等。
Reference(s):
1. Heringa M et al. (2003). Review on raloxifene: profile of a selective estrogen receptor modulator. Int J Clin Pharmacol Ther.
2. Cummings SR et al. (1999). The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. JAMA.
3. Bryant HU et al. (1999). An estrogen receptor basis for raloxifene action in bone. J Steroid Biochem Mol Biol.
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