Lasofoxifene is a third-generation, non-steroidal selective estrogen receptor modulator (SERM). It selectively binds to human ERα with an IC50 value of 1.5 nM and inhibits bone loss in ovariectomized rats.{28785} In clinical studies of postmenopausal osteoporosis, 0.5 mg/day lasofoxifene was associated with reduced risks of nonvertebral and vertebral fractures, ER-positive breast cancer, coronary heart disease, and stroke but an increased risk of venous thromboembolic events.{28786,28787} Lasofoxifene has also been shown to act as an inverse agonist at the CB2 cannabinoid receptor, indicating its potential to be repurposed as a therapeutic for indications wherein CB2 is a target.{28788}
产品描述
A third-generation SERM that selectively binds to human ERα (IC50 = 1.5 nM) and inhibits bone loss in ovariectomized rats; used in the treatment of postmenopausal osteoporosis and ER-positive breast cancer; also acts as an inverse agonist at the CB2 cannabinoid receptor
