lasofoxifene

Lasofoxifene is a non-steroidal, third-generation selective estrogen receptor modulator (SERM) that selectively binds with high affinity to both estrogen receptor alpha (ERα) and beta (ERβ). It acts as an agonist on bone tissue, mimicking the positive effects of estrogen to reduce osteoclast activity and stimulate osteoblasts, thereby increasing bone mineral density and reducing fracture risk. In other tissues such as the uterus and mammary glands, it functions as an antagonist by suppressing estrogen signaling in oncogenic pathways. Lasofoxifene also exhibits potential inverse agonist activity at the cannabinoid receptor 2 (CB2), which may contribute to its antiresorptive effects on bone. The drug was initially developed for prevention and treatment of osteoporosis and vaginal atrophy in postmenopausal women. It has demonstrated efficacy in reducing vertebral and nonvertebral fractures, improving symptoms of vulvovaginal atrophy, and decreasing the risk of ER-positive breast cancer. Lasofoxifene is being further investigated for use in hormone receptor-positive advanced or metastatic breast cancer—including cases with ESR1 mutations resistant to other endocrine therapies[1][3][5][6].

Brand names

FablynOporia

Other names

lasofoxifene tartrate