Lasofoxifene, a new selective estrogen receptor modulator for the treatment of osteoporosis and vaginal atrophy

摘要: Selective estrogen receptor modulators (SERMs) represent a class with growing number of compounds that act as either (ER) agonists or antagonists in tissue-specific manner. The purpose this article is to review the effects lasofoxifene, new-generation SERM has completed Phase III development program for prevention and treatment osteoporosis vaginal atrophy postmenopausal women. This compound selectively binds both ERs high affinity. Lasofoxifene also remarkably improved oral bioavailability respect other SERMs such raloxifene tamoxifen, owing increased resistance intestinal wall glucuronidation. In preclinical short-term clinical studies, showed favorable safety profile demonstrated proven efficacy preventing bone loss lowering cholesterol levels. More recently, trials have confirmed new vertebral nonvertebral fractures. Moreover, women osteoporosis, lasofoxifene reduced ER positive breast cancer risk occurrence atrophy. With its potency on fractures vagina, may an alternative therapy