Lasofoxifene (LASO), A Next Generation Selective Estrogen Response Modulator (SERM) Improves Dyspareunia in Postmenopausal Women with Vaginal Atrophy (VA)

Nuclear Receptors and Their Selective Pharmacologic Modulators

“…It is thought that these effects are likely due to the ability of lasofoxifene to increase the expression levels of ERb and AR in vaginal tissues, which other SERMs do not . Clinical data support the use of lasofoxifene in the prevention and treatment of osteoporosis and treatment of vaginal atrophy in postmenopausal women without an increased risk of endometrial cancer but with an increased risk of venous thromboembolic events (Bachmann et al, 2005;McClung et al, 2006b;Taylor, 2009;Cummings et al, 2010;Gennari et al, 2010). From a structural perspective, much like tamoxifen and raloxifene, lasofoxifene displaces helix 12 in the LBD from the agonist position to block the AF-2 coregulator-binding surface (Vajdos et al, 2007).…”

Not all selective estrogen response modulators are created equal: update on lasofoxifene

“…This is in keeping with findings of several other trials that looked at the effects of lasofoxifene on vaginal atrophy and the dyspareunia associated with it. Lasofoxifene, when compared to placebo, improves dyspareunia in postmenopausal women with vaginal atrophy (14,15) . Furthermore, lasofoxifene resulted in decrease symptoms associated with vaginal atrophy (16) as well clinical signs associated with it (17) .…”

Clinical effects of selective estrogen receptor modulators on vulvar and vaginal atrophy

“…92 Significantly more women receiving lasofoxifene (all doses, PG 0.001 vs placebo) reported improvement in vaginal dryness/ soreness compared with placebo. At all doses, lasofoxifene significantly reduced symptoms associated with sexual intercourse (P G 0.01 for all doses vs placebo for improved discomfort during and after sexual intercourse; P G 0.05 for all doses vs placebo for bleeding during/after sexual intercourse).…”