Lasofoxifene: Selective estrogen receptor modulator for the prevention and treatment of postmenopausal osteoporosis [Lasofoxifeno: SERM para la prevencion y tratamiento de osteoporosis posmenopausica]

Gregory Peterson, Mark Naunton, Lisette Tichelaar, Luigi Gennari

Research output: Contribution to journalArticle

7 Citations (Scopus)

Abstract

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 (his 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 (lushes, 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 toss in postmenopausal women.
Original languageEnglish
Pages (from-to)499-509
Number of pages11
JournalAnnals of Pharmacotherapy
Volume45
Issue number4
DOIs
Publication statusPublished - 1 Apr 2011

Fingerprint

Selective Estrogen Receptor Modulators
Postmenopausal Osteoporosis
Osteoporosis
Bone Density
Therapeutics
Pharmacokinetics
Lasofoxifene
Clinical Trials
Pelvic Bones
Pharmacology
Safety
Muscle Cramp
Phase III Clinical Trials
Bone Remodeling
Information Storage and Retrieval
United States Food and Drug Administration
MEDLINE
Biological Availability
Leg
Spine

Cite this

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title = "Lasofoxifene: Selective estrogen receptor modulator for the prevention and treatment of postmenopausal osteoporosis [Lasofoxifeno: SERM para la prevencion y tratamiento de osteoporosis posmenopausica]",
abstract = "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 (his 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 (lushes, 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 toss in postmenopausal women.",
keywords = "Lasofoxifene, Osteoporosis, Selective estrogen receptor modulator",
author = "Gregory Peterson and Mark Naunton and Lisette Tichelaar and Luigi Gennari",
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language = "English",
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pages = "499--509",
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TY - JOUR

T1 - Lasofoxifene: Selective estrogen receptor modulator for the prevention and treatment of postmenopausal osteoporosis [Lasofoxifeno: SERM para la prevencion y tratamiento de osteoporosis posmenopausica]

AU - Peterson, Gregory

AU - Naunton, Mark

AU - Tichelaar, Lisette

AU - Gennari, Luigi

PY - 2011/4/1

Y1 - 2011/4/1

N2 - 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 (his 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 (lushes, 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 toss in postmenopausal women.

AB - 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 (his 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 (lushes, 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 toss in postmenopausal women.

KW - Lasofoxifene

KW - Osteoporosis

KW - Selective estrogen receptor modulator

U2 - 10.1345/APH.1P604

DO - 10.1345/APH.1P604

M3 - Article

VL - 45

SP - 499

EP - 509

JO - DICP, Annals of Pharmacotherapy

JF - DICP, Annals of Pharmacotherapy

SN - 1060-0280

IS - 4

ER -