Lasofoxifene: a new-generation SERM for the treatment of postmenopausal osteoporosis

Lasofoxifene is a new-generation selective estrogen receptor modulator that completed the Phase III development program for the prevention and treatment of osteoporosis in postmenopausal women. This compound has a remarkably improved oral bioavailability with respect to other selective estrogen receptor modulators owing to its increased resistance to intestinal wall glucuronidation. In both preclinical and short-term Phase II clinical studies, lasofoxifene showed a favorable safety profile and demonstrated a proven efficacy in preventing bone loss and lowering cholesterol levels. The recent results from Phase III clinical trials demonstrated the clinical efficacy of this drug in the prevention of vertebral and nonvertebral fractures. The purpose of this article is to review the clinical evidence for the use of lasofoxifene in women after menopause and to discuss how it will fit into the treatment of postmenopausal osteoporosis. © 2009, Expert Reviews Ltd. All rights reserved.