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OBJECTIVE: To review literature evaluating the pharmacology, pharmacokinetics, clinical efficacy, and adverse effects of lasofoxifene (CP-336156), a selective estrogen receptor modulator (SERM) that is not approved for use in the US. DATA SOURCES: Literature was accessed through the MEDLINE and EMBASE databases (1985-June 2010) using the terms lasofoxifene and selective estrogen receptor modulators. Reference lists from retrieved articles were also manually reviewed. The Food and Drug Administration and Pfizer provided additional information. STUDY SELECTION AND DATA EXTRACTION: All clinical trials evaluating lasofoxifene were included in this review. In addition, all articles evaluating the pharmacology, pharmacokinetics, and safety of lasofoxifene in humans were reviewed. DATA SYNTHESIS: Lasofoxifene is a third-generation SERM with markedly higher in vitro and in vivo potency and oral bioavailability than other SERMs. The drug has produced significant improvements in bone density and biochemical markers of bone turnover in preclinical studies and in Phase 2 and 3 clinical trials. In these trials, lasofoxifene has shown a favorable safety profile, with adverse events including hot flushes, leg cramps, and increased vaginal moisture. One 2-year major comparative study in postmenopausal women determined that lasofoxifene and raloxifene were equally effective at increasing total hip bone mineral density (BMD), while lasofoxifene had a significantly greater effect on lumbar spine BMD. CONCLUSIONS: Osteoporosis is a significant health problem. While the results of further clinical trials are needed to define the risks and benefits of treatment, particularly relating to fractures, lasofoxifene may prove to be an effective and well-tolerated therapeutic option for the prevention of bone loss in postmenopausal women.

Item Type:	Refereed Article
Keywords:	lasofoxifene; osteoporosis; selective estrogen receptor modulator
Research Division:	Biomedical and Clinical Sciences
Research Group:	Pharmacology and pharmaceutical sciences
Research Field:	Clinical pharmacology and therapeutics
Objective Division:	Health
Objective Group:	Clinical health
Objective Field:	Clinical health not elsewhere classified
UTAS Author:	Peterson, GM (Professor Gregory Peterson)
ID Code:	78043
Year Published:	2011
Web of Science® Times Cited:	9
Deposited By:	Pharmacy
Deposited On:	2012-06-13
Last Modified:	2017-11-02
Downloads:	1 View Download Statistics