Selective estrogen receptor modulator (SERM) for the treatment of osteoporosis in postmenopausal women: focus on lasofoxifene

References

• Osteoporosis Prevention, Diagnosis, and Therapy Consensus Statement 2000JAMA200128578579511176917
   PubMed Web of Science ®Google Scholar
• SambrookPCooperCOsteoporosisLancet20063672010201816782492
   PubMed Web of Science ®Google Scholar
• ReginsterJYBurletNOsteoporosis: a still increasing prevalenceBone200638S4S916455317
   PubMed Web of Science ®Google Scholar
• CummingsSRMeltonLJEpidemiology and outcomes of osteoporotic fracturesLancet20023591761176712049882
   PubMed Web of Science ®Google Scholar
• JohnellOKanisJAAn estimate of the worldwide prevalence and disability associated with osteoporotic fracturesOsteoporos Int2006171726173316983459
   PubMed Web of Science ®Google Scholar
• RossPDOsteoporosis. Frequency, consequences, and risk factorsArch Intern Med1996156139914118678708
   PubMed Web of Science ®Google Scholar
• DennisonEMohamedMACooperCEpidemiology of osteoporosisRheum Dis Clin North Am20063261762917288968
   PubMed Web of Science ®Google Scholar
• RaiszLGPathogenesis of osteoporosis: concepts, conflicts and prospectsJ Clin Invest20051153318332516322775
   PubMed Web of Science ®Google Scholar
• LindsayRHartDMForrestCBairdCPrevention of spinal osteoporosis in oophorectomised womenLancet198028205115111546107766
   PubMed Web of Science ®Google Scholar
• CummingsSRBlackDMNevittMCBone density at various sites for prediction of hip fracturesLancet199334172758093403
   PubMed Web of Science ®Google Scholar
• HuiSLSlemendaCWCareyMAJohnstonCCChoosing between predictors of fracturesJ Bone Miner Res199510181618228592960
   PubMed Web of Science ®Google Scholar
• SeemanEDelmasPDBone quality-the material and structural basis of bone strength and fragilityN Engl J Med20063542250226116723616
   PubMed Web of Science ®Google Scholar
• MartinTJSeemanEBone remodeling: its local regulation and the emergence of bone fragilityBest Pract Res Clin Endo Endocrinol Metab200822701722
   PubMed Web of Science ®Google Scholar
• RiggsBLKhoslaSMeltonLJIIISex steroids and the construction and conservation of the adult skeletonEndo Rev200223279302
   PubMed Web of Science ®Google Scholar
• SyedFKhoslaSMechanisms of sex steroid effects on boneBiochem Biophys Res Commun200532868869615694402
   PubMed Web of Science ®Google Scholar
• PacificiRBilezikianJPRaiszLGMartinTJMechanisms of estrogen action in bonePrinciples of Bone Biology3rd edUSAElsevier Inc2008921933
   Google Scholar
• BushTLWellsHBJamesMKEffects of hormone therapy on bone mineral density–results from the postmenopausal estrogen/progestin interventions (PEPI) trialJAMA1996276138913968892713
   PubMed Web of Science ®Google Scholar
• RossouwJEPrenticeRLMansonJEPostmenopausal hormone therapy and risk of cardiovascular disease by age and years since menopauseJAMA20072971465147717405972
   PubMed Web of Science ®Google Scholar
• JacksonRDShidhamSThe role of hormone therapy and calcium plus vitamin D for reduction of bone loss and risk for fractures: lessons learned from the Women’s Health InitiativeCurrent Osteoporosis Reports20075415315918430389
   PubMedGoogle Scholar
• GrodsteinFMansonJEColditzGAA prospective, observational study of postmenopausal hormone therapy and primary prevention of cardiovascular diseaseAnn Intern Med200013393394111119394
   PubMed Web of Science ®Google Scholar
• MansonJEHsiaJJohnsonKCWomen’s Health Initiative InvestigatorsEstrogen plus progestin and the risk of coronary heart diseaseN Engl J Med200334952353412904517
   PubMed Web of Science ®Google Scholar
• The Writing Group for the PEPI TrialEffects of estrogen or estrogen/progestin regimens on heart disease risk factors in postmenopausal women: the Postmenopausal Estrogen/Progestin Interventions (PEPI) TrialJAMA19952731992087807658
   PubMed Web of Science ®Google Scholar
• Vassilopoulou-SellinRBreast cancer and hormonal replacement therapyAnn N Y Acad Sci200399734135014644841
   PubMed Web of Science ®Google Scholar
• The North American Menopause SocietyEstrogen and progestogen use in postmenopausal women: July 2008 position statement of The North American menopause societyMenopause200815458460218580541
   PubMed Web of Science ®Google Scholar
• ChoCHNuttallMETherapeutic potential of oestrogen receptor ligands in development for osteoporosisExpert Opin Emerg Drugs2001613715415989501
   PubMedGoogle Scholar
• JordanVCChemosuppression of breast cancer with tamoxifen-laboratory evidence and future clinical investigationsCancer Investigation198865895953063338
   PubMed Web of Science ®Google Scholar
• LernerLJJordanVCDevelopment of antiestrogens and their use in breast cancer (Eighth Cain Memorial award lecture)Cancer Res199050417741892194650
   PubMed Web of Science ®Google Scholar
• AvioliLVSERM Drugs for the prevention of osteoporosisTrends Endocrinol Metab19991031731910481162
   PubMed Web of Science ®Google Scholar
• RiggsLHartmannLCSelective Estrogen-Receptor Modulators- Mechanisms of Action and Application to Clinical PracticeN Engl J Med200334861862912584371
   PubMed Web of Science ®Google Scholar
• BrzozowskiAMPikeACDauterZMolecular basis of agonism and antagonism in the oestrogen receptorNature19973897537589338790
   PubMed Web of Science ®Google Scholar
• ShiauAKBarstadDLoriaPMThe structural basis of estrogen receptor/coactivator recognition and the antagonism of this interaction by tamoxifenCell1998959279379875847
   PubMed Web of Science ®Google Scholar
• PaigeLAChristensenDJGrønHEstrogen receptor (ER) modulators each induce distinct conformational changes in ERa and ERbProc Natl Acad Sci U S A1999963999400410097152
   PubMed Web of Science ®Google Scholar
• NilssonSKoehlerKFOestrogen receptors and selective oestrogen receptor modulators: molecular and cellular pharmacologyBasic Clin Pharmacol Toxicol200596152515667591
   PubMed Web of Science ®Google Scholar
• GennariLMerlottiDValleggiFMartiniGNutiRSelective estrogen receptor modulators for postmenopausal osteoporosis: current state of developmentDrugs Aging20072436137917503894
   PubMed Web of Science ®Google Scholar
• GennariLMerlottiDDe PaolaVMartiniGNutiRBazedoxifene for the prevention of postmenopausal osteoporosisTher Clin Risk Manag2008a461229124219337430
   PubMedGoogle Scholar
• DelmasPDBjarnasonNHMitlakBHEffects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal womenN Engl J Med1997337164116479385122
   PubMed Web of Science ®Google Scholar
• LufkinEGWhitakerMDNickelsenTTreatment of established postmenopausal osteoporosis with raloxifene: a randomized trialJ Bone Miner Res199813174717549797484
   PubMed Web of Science ®Google Scholar
• EttingerBBlackDMMitlakBHReduction of vertebral fracture risk in postmenopausal women with osteoporosis treated with raloxifene: results from a 3-year randomized clinical trial. Multiple Outcomes of Raloxifene Evaluation (MORE) InvestigatorsJAMA1999282763764510517716
   PubMed Web of Science ®Google Scholar
• JordanVCPhelpsELindgrenJUEffects of anti-estrogens on bone in castrated and intact female ratsBreast Cancer Res Treat19871031353689979
   PubMed Web of Science ®Google Scholar
• LoveRRBardenHSMazessRBEffect of tamoxifen on lumbar spine bone mineral density in postmenopausal women after 5 yearsArch Intern Med1994154258525887979855
   PubMed Web of Science ®Google Scholar
• PrestwoodKMGunnessMMuchmoreDBA comparison of the effects of raloxifene and estrogen on bone in postmenopausal womenJ Clin Endocrinol Metab2000852197220210852452
   PubMed Web of Science ®Google Scholar
• WeinsteinRSParfittAMMarcusREffects of raloxifene, hormone replacement therapy, and placebo on bone turnover in postmenopausal womenOsteoporos Int20031481482214610642
   PubMed Web of Science ®Google Scholar
• GennariLMerlottiDDe PaolaVNutiRRaloxifene in breast cancer preventionExpert Opin Drug Saf2008b725927018462184
   PubMed Web of Science ®Google Scholar
• GennariLMerlottiDValleggiFNutiROspemifene use in postmenopausal womenExpert Opin Investig Drugs2009186839849
   PubMed Web of Science ®Google Scholar
• RosatiRLDa Silva JardinePCameronKODiscovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthaleneJ Med Chem199841292829319685230
   PubMed Web of Science ®Google Scholar
• KeHZParalkarVMGrasserWAEffects of CP-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus and body composition in rat modelsEndocrinology1998139206820769528995
   PubMed Web of Science ®Google Scholar
• GennariLMerlottiDMartiniGNutiRLasofoxifene: a thirdgeneration selective estrogen receptor modulator for the prevention and treatment of osteoporosisExpert Opin Investig Drugs2006a1510911103
   PubMed Web of Science ®Google Scholar
• MorelloKCWurzGTDeGregorioMWPharmacokinetics of selective estrogen receptor modulatorsClin Pharmacokinet20034236137212648026
   PubMed Web of Science ®Google Scholar
• GennariLLasofoxifene: a new type of selective estrogen receptor modulator for the treatment of osteoporosisDrugs Today (Barc)2006b4235536716845439
   PubMed Web of Science ®Google Scholar
• MollerRFisherJTaylorAEffect of Food on the Pharmacokinetics of Lasofoxifene, in Healthy Postmenopausal WomenJ Bone Miner Res200419 Abstract SU487
   PubMed Web of Science ®Google Scholar
• GardnerMNishizawaYWeiGA Single-Dose Pharmacokinetic Study of Lasofoxifene in Japanese and Caucasian Postmenopausal WomenJ Bone Miner Res200419 Abstract M469
   Web of Science ®Google Scholar
• GardnerMTaylorAWeiGClinical pharmacology of multiple doses of lasofoxifene in postmenopausal womenJ Clin Pharmacol200646525816397284
   PubMed Web of Science ®Google Scholar
• FountaineRJNishizawaYWeiGDogoloLCalcagniAGardnerMJClinical pharmacology of lasofoxifene in Japanese and white postmenopausal womenJ Clin Pharmacol20064669369916707415
   PubMed Web of Science ®Google Scholar
• KatzenellenbogenJAD-1,2-Dyaril-3,4-dihydronaphthalenes: photofluorogenic ligands for the estrogen receptorJ Steroid Biochem1985239299374094420
   PubMedGoogle Scholar
• JhonsonKAGardnerMJPrakashCIn vivo and in vitro metabolites of a next-generation selective estrogen receptor modulator, lasofoxifene, in humansDrug Metab Rev200436246
   Web of Science ®Google Scholar
• RomanDBramsonCOuelletDEffect of lasofoxifene on the pharmacokinetics of digoxin in healthy postmenopausal womenJ Clin Pharmacol2005451407141216291716
   PubMed Web of Science ®Google Scholar
• MollerRAFisherJMTaylorAEEffects of Steady-State Lasofoxifene on CYP2D6- and CYP2E1-Mediated MetabolismAnn Pharmacother200640323716368922
   PubMed Web of Science ®Google Scholar
• BramsonCOuelletDRomanDA single-dose pharmacokinetic study of lasofoxifene in healthy volunteers and subjects with mild and moderate hepatic impairmentJ Clin Pharmacol200646293616397281
   PubMed Web of Science ®Google Scholar
• OuelletDBramsonCCarvajal-GonzalezSRomanDRandinitisERemmersAEffects of lasofoxifene on the pharmacokinetics and pharmacodynamics of single-dose warfarinBr J Clin Pharmacol20066174174516722839
   PubMed Web of Science ®Google Scholar
• KeHZQiHChidsey-FrinkKLEffects of different dose regimens of lasofoxifene (CP-336,156) in preventing bone loss in ovariectomized ratsJ Bone Miner Res2000a15S1S310
   Web of Science ®Google Scholar
• KeHZFoleyGLSimmonsHAShenVThompsonDDLong-term treatment of lasofoxifene preserves bone mass and bone strength and does not adversely affect the uterus in ovariectomized ratsEndocrinology20041451996200514726439
   PubMed Web of Science ®Google Scholar
• KeHZQiHCrawfordDTLasofoxifene (CP-336-156), a selective estrogen receptor modulator, prevents bone loss induced by aging and orchidectomy in the adult ratEndocrinology2000b1411338134410746637
   PubMed Web of Science ®Google Scholar
• KeHZOiHChidsey-FrinkKLLasofoxifene (CP-336-156) protects against the age-related changes in bone mass, bone strength, and total serum cholesterol in intact aged male ratsJ Bone Miner Res20011676577311316005
   PubMed Web of Science ®Google Scholar
• KharodeYPGreenPDMarzolfJTComparison of the effects of bazedoxifene, raloxifene, lasofoxifene and risedronate, co-treatment on h-PTH-induced reversal of established osteopenia in ovariectomized ratsJ Bone Miner Res200318S273
   Web of Science ®Google Scholar
• CohenLAPittmanBWangCXLAS, a novel selective estrogen receptor modulator with chemopreventive and therapeutic activity in the N-nitroso-N-methylurea-induced rat mammary tumor modelCancer Res2001618683868811751385
   PubMed Web of Science ®Google Scholar
• GennariLMerlottiDDe PaolaVNutiRLasofoxifene: the evidence of its therapeutic value in osteoporosisCore Evidence20094113129
   Google Scholar
• ChesworthRZawistoskiMPLefkerBATetrahydroisoquinolines as subtype selective estrogen agonists/antagonistsBioorganic and Medicinal Chemistry Letters2004142729273315125923
   PubMed Web of Science ®Google Scholar
• LeeARadeckiDWolterKLasofoxifene Phase 2 and Phase 3 Clinical Trial Design and StrategyJ Bone Miner Res200520 Abstract M384
   Web of Science ®Google Scholar
• DayWMartelJLeeALasofoxifene phase 2 dose response analysis in postmenopausal womenJ Bone Miner Res200520 Abstract M385
   Web of Science ®Google Scholar
• MoffettAHEttingerMBologneseMLasofoxifene, a Next Generation SERM, is Effective in Preventing Loss of BMD and Reducing LDL-C in Postmenopausal WomenJ Bone Miner Res200419 Abstract SA426
   PubMed Web of Science ®Google Scholar
• PortmanDJMoffettAHBachmanGAWestCSymonsJLasofoxifene, a selective estrogen receptor modulator, improves objective measures of vaginal atrophyObstetrics and Gynecology200410325S26S
   Web of Science ®Google Scholar
• EttingerMSchwartzEEmkeyRLasofoxifene: a next generation selective estrogen receptor modulator (SERM) in the prevention of bone loss in postmenopausal women86th Annual Meeting of the Endocrine Society2004 June 16–19New Orleans, LA
   Google Scholar
• Lingand pharmaceutical Internetional IncAnnual Report 2000 Available from http//investors.ligand.com
   Google Scholar
• McClungMPortmanDEmkeyRComparison of the extraskeletal effects of lasofoxifene and raloxifeneJ Bone Miner Res200419 Abstract SA423
   PubMed Web of Science ®Google Scholar
• McClungMRSirisECummingsSPrevention of bone loss in postmenopausal women treated with lasofoxifene compared with raloxifeneMenopause20061337738616735934
   PubMed Web of Science ®Google Scholar
• McClungMSirisECummingsSLasofoxifene Increased BMD of the Spine and Hip and Decreased Bone Turnover Markers in Postmenopausal Women with Low or Normal BMDJ Bone Miner Res200520 Abstract F429
   Web of Science ®Google Scholar
• DavidsonMMoffettAWeltyFExtraskeletal Effects of Lasofoxifene on Postmenopausal WomenJ Bone Miner Res200520 Abstract SA428
   Web of Science ®Google Scholar
• EastellRReidDMVukicevicSThe Effects of Lasofoxifene on Bone Turnover Markers: the PEARL TrialJ Bone Miner Res200823 Abstract 1287
   Web of Science ®Google Scholar
• GloverSJRogersAGossielFEastellRA randomized double blinded controlled trial of individual response in biochemical markers of bone turnover to lasofoxifene therapyJ Bone Miner Res200823 Abstract M507
   Web of Science ®Google Scholar
• CummingsSREastellREnsrudKThe effects of lasofoxifene on fractures and breast cancer: 3-year results from the PEARL TrialJ Bone Miner Res200823 Abstract 1288
   Web of Science ®Google Scholar
• European Medicines Agency, Pre-Authorisation Evaluation of Medicines for Human UseCommittee for Medicinal Products for Human Use summary of positive opinion for FablynLondon2008 December 18 Doc Ref EMEA/CHMP/609979/2008
   Google Scholar
• StevensonNJonesMLDe NigrisEBrewerNDavisSOakleyJA systematic review and economic evaluation of alendronate, etidronate, risedronate, raloxifene and teriparatide for the prevention and treatment of postmenopausal osteoporosisHealth Technol Assess20059116015929857
   PubMed Web of Science ®Google Scholar