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

References

• Sambrook P, Cooper C. Osteoporosis. Lancet367, 2010–2018 (2006).
   PubMed Web of Science ®Google Scholar
• Poole KES, Compston JE. Osteoporosis and its management. BMJ333, 1251–1256 (2006).
   PubMed Web of Science ®Google Scholar
• NIH Consensus Development Panel on Osteoporosis Prevention, Diagnosis, and Therapy. Osteoporosis Prevention, Diagnosis, and Therapy Consensus Statement 2000. JAMA285, 785–795 (2001).
   PubMed Web of Science ®Google Scholar
• Reginster JY, Burlet N. Osteoporosis: a still increasing prevalence. Bone38(2 Suppl. 1), S4–S9 (2006).
   Web of Science ®Google Scholar
• Cummings SR, Melton LJ 3rd. Epidemiology and outcomes of osteoporotic fractures. Lancet359, 1761–1767 (2002).
   PubMed Web of Science ®Google Scholar
• Johnell O, Kanis JA. An estimate of the worldwide prevalence and disability associated with osteoporotic fractures. Osteoporos. Int.17, 1726–1733 (2006).
   PubMed Web of Science ®Google Scholar
• Ross PD. Osteoporosis. Frequency, consequences, and risk factors. Arch. Intern. Med.156, 1399–1411 (1996).
   PubMed Web of Science ®Google Scholar
• Chrischilles EA, Butler CD, Davis CS, Wallace RB. A model of lifetime osteoporosis impact. Arch. Intern. Med.151, 2026–2032 (1991).
   PubMed Web of Science ®Google Scholar
• Black DM, Cummings SR, Genant HK, Nevitt MC, Palermo L, Browner W. Axial and appendicular bone density predict fractures in older women. J. Bone Miner. Res.7, 633–638 (1992).
   PubMed Web of Science ®Google Scholar
• Cummings SR, Black DM, Nevitt MC et al. Bone density at various sites for prediction of hip fractures. Lancet341, 72–75 (1993).
   PubMed Web of Science ®Google Scholar
• Hui SL, Slemenda CW, Carey MA, Johnston CC. Choosing between predictors of fractures. J. Bone Miner. Res.10, 1816–1822 (1995).
   PubMed Web of Science ®Google Scholar
• Seeman E, Delmas PD. Bone quality – the material and structural basis of bone strength and fragility. N. Engl. J. Med.354, 2250–2261 (2006).
   PubMed Web of Science ®Google Scholar
• Raisz LG. Pathogenesis of osteoporosis: concepts, conflicts and prospects. J. Clin. Invest.115, 3318–3325 (2005).
   PubMed Web of Science ®Google Scholar
• Riggs BL, Khosla S, Melton LJ 3rd. Sex steroids and the construction and conservation of the adult skeleton. Endo. Rev.23, 279–302 (2002).
   PubMed Web of Science ®Google Scholar
• Syed F, Khosla S. Mechanisms of sex steroid effects on bone. Biochem. Biophys. Res. Commun.328, 688–696 (2005).
   PubMed Web of Science ®Google Scholar
• Grodstein F, Manson JE, Colditz GA et al. A prospective, observational study of postmenopausal hormone therapy and primary prevention of cardiovascular disease. Ann. Intern. Med.133, 933–941 (2000).
   PubMed Web of Science ®Google Scholar
• Manson JE, Hsia J, Johnson KC et al.; Women’s Health Initiative Investigators. Estrogen plus progestin and the risk of coronary heart disease. N. Engl. J. Med.349, 523–534 (2003).
   PubMed Web of Science ®Google Scholar
• Rossouw JE, Prentice RL, Manson JE et al. Postmenopausal hormone therapy and risk of cardiovascular disease by age and years since menopause. JAMA297, 1465–1477 (2007).
   PubMed Web of Science ®Google Scholar
• Vassilopoulou-Sellin R. Breast cancer and hormonal replacement therapy. Ann. NY Acad. Sci.997, 341–350 (2003).
   PubMed Web of Science ®Google Scholar
• HRT: what are women (and their doctors) to do? Lancet364, 2069–2070 (2004).
   PubMed Web of Science ®Google Scholar
• Bilezikian JP, Matsumoto T, Bellido T et al. Targeting bone remodeling for the treatment of osteoporosis: summary of the proceedings of an ASBMR workshop. J. Bone Miner. Res.24, 373–385 (2009).
   PubMed Web of Science ®Google Scholar
• Pleiner-Duxneuner J, Zwettler E, Paschalis E, Roschger P, Nell-Duxneuner V, Klaushofer K. Treatment of osteoporosis with parathyroid hormone and teriparatide. Calcif. Tissue Int.84, 159–170 (2009).
   PubMed Web of Science ®Google Scholar
• Tournis S, Economopoulos D, Lyritis GP. Strontium ranelate: a novel treatment in postmenopausal osteoporosis. Ann. NY Acad. Sci.1092, 403–407 (2006).
   PubMed Web of Science ®Google Scholar
• Blake GM, Compston JE, Fogelman I. Could strontium ranelate have a synergistic role in the treatment of osteoporosis? J. Bone Miner. Res.24, 1354–1357 (2009).
   PubMed Web of Science ®Google Scholar
• Bilezikian JP. Efficacy of bisphosphonates in reducing fracture risk in postmenopausal osteoporosis. Am. J. Med.122(2 Suppl.), S14–S21 (2009).
   Web of Science ®Google Scholar
• Rabenda V, Mertens R, Fabri V et al. Adherence to bisphosphonates therapy and hip fracture risk in osteoporotic women. Osteoporos. Int.19, 811–818 (2008).
   PubMed Web of Science ®Google Scholar
• Cramer JA, Amonkar MM, Hebborn A et al. Compliance and persistence with bisphosphonate dosing regimens among women with postmenopausal osteoporosis. Curr. Med. Res. Opin.21, 1453–1460 (2005).
   PubMed Web of Science ®Google Scholar
• Cho CH, Nuttall ME. Therapeutic potential of oestrogen receptor ligands in development for osteoporosis. Emerging Drugs6, 137–154 (2001).
   PubMedGoogle Scholar
• Nilsson S, Koehler KF. Oestrogen receptors and selective oestrogen receptor modulators: molecular and cellular pharmacology. Basic Clin. Pharmacol. Toxicol.96, 15–25 (2005).
   PubMed Web of Science ®Google Scholar
• Riggs BL, Hartmann LC. Selective estrogen-receptor modulators-mechanisms of action and application to clinical practice. N. Engl. J. Med.348, 618–629 (2003).
   PubMed Web of Science ®Google Scholar
• Gennari L, Merlotti D, De Paola V, Nuti R. Raloxifene in breast cancer prevention. Expert. Opin. Drug. Saf.7, 259–270 (2008).
   PubMed Web of Science ®Google Scholar
• Gennari L, Merlotti D, Valleggi F, Martini G, Nuti R. Selective estrogen receptor modulators for postmenopausal osteoporosis: current state of development. Drugs Aging24, 361–379 (2007).
   PubMed Web of Science ®Google Scholar
• Prestwood KM, Gunness M, Muchmore DB et al. A comparison of the effects of raloxifene and estrogen on bone in postmenopausal women. J. Clin. Endocrinol. Metab.85, 2197–2202 (2000).
   PubMed Web of Science ®Google Scholar
• Weinstein RS, Parfitt AM, Marcus R et al. Effects of raloxifene, hormone replacement therapy, and placebo on bone turnover in postmenopausal women. Osteoporos. Int.14, 814–822 (2003).
   PubMed Web of Science ®Google Scholar
• Rosati RL, Da Silva Jardine P, Cameron KO. Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene. J. Med. Chem.41, 2928–2931 (1998).
   PubMed Web of Science ®Google Scholar
• Ke HZ, Paralkar VM, Grasser WA. Effects of CP-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus and body composition in rat models. Endocrinology139, 2068–2076 (1998).
   PubMed Web of Science ®Google Scholar
• Gennari L, Merlotti D, Martini G, Nuti R. Lasofoxifene: a third-generation selective estrogen receptor modulator for the prevention and treatment of osteoporosis. Expert. Opin. Investig. Drugs15, 1091–1103 (2006).
   PubMed Web of Science ®Google Scholar
• Ke HZ, Qi H, Chidsey-Frink KL et al. Effects of different dose regimens of lasofoxifene (CP-336,156) in preventing bone loss in ovariectomized rats. J. Bone Miner. Res.15, S1–S310 (2000).
   Google Scholar
• Ke HZ, Foley GL, Simmons HA et al. Long-term treatment of lasofoxifene preserves bone mass and bone strength and does not adversely affect the uterus in ovariectomized rats. Endocrinology145, 1996–2005 (2004).
   PubMed Web of Science ®Google Scholar
• Cohen LA, Pittman B, Wang CX et al. LAS, a novel selective estrogen receptor modulator with chemopreventive and therapeutic activity in the N-nitroso-N-methylurea-induced rat mammary tumor model. Cancer Res.61, 8683–8688 (2001).
   PubMed Web of Science ®Google Scholar
• Gennari L. Lasofoxifene: a new type of selective estrogen receptor modulator for the treatment of osteoporosis. Drugs Today (Barc.)42, 355–367 (2006).
   PubMed Web of Science ®Google Scholar
• Gardner M, Nishizawa Y, Wei G et al. A single-dose pharmacokinetic study of lasofoxifene in japanese and caucasian postmenopausal women. J. Bone Miner. Res.19, (2004) Abstract M469.
   Google Scholar
• Gardner M, Taylor A, Wei G et al. Clinical pharmacology of multiple doses of lasofoxifene in postmenopausal women. J. Clin. Pharmacol.46, 52–58 (2006).
   PubMed Web of Science ®Google Scholar
• Fountaine RJ, Nishizawa Y, Wei G, Dogolo L, Calcagni A, Gardner MJ. Clinical pharmacology of lasofoxifene in Japanese and white postmenopausal women. J. Clin. Pharmacol.46, 693–699 (2006).
   PubMed Web of Science ®Google Scholar
• Morello KC, Wurz GT, DeGregorio MW. Pharmacokinetics of selective estrogen receptor modulators. Clin. Pharmacokinet.42, 361–372 (2003).
   PubMed Web of Science ®Google Scholar
• Hochner-Celnikier D. Pharmacokinetics of raloxifene and its clinical application. Eur. J. Obstet. Gynecol. Reprod. Biol.85, 23–29 (1999).
   PubMed Web of Science ®Google Scholar
• Katzenellenbogen JA. D-1,2-dyaril-3,4-dihydronaphthalenes: photofluorogenic ligands for the estrogen receptor. J. Steroid. Biochem.23, 929–937 (1985).
   PubMedGoogle Scholar
• Moller R, Fisher J, Taylor A, Kolluri S, Gardner M. Effect of food on the pharmacokinetics of lasofoxifene, in healthy postmenopausal women. J. Bone Miner. Res.19(Suppl. 1) (2004) (Abstract SU487).
   PubMed Web of Science ®Google Scholar
• Jhonson KA, Gardner MJ, Prakash C. In vivo and in vitro metabolites of a next-generation selective estrogen receptor modulator, lasofoxifene, in humans. Drug. Metab. Rev.36, 246 (2004).
   Web of Science ®Google Scholar
• Roman D, Bramson C, Ouellet D et al. Effect of lasofoxifene on the pharmacokinetics of digoxin in healthy postmenopausal women. J. Clin. Pharmacol.45, 1407–1412 (2005).
   PubMed Web of Science ®Google Scholar
• Moller RA, Fisher JM, Taylor AE et al. Effects of steady-state lasofoxifene on CYP2D6- and CYP2E1-mediated metabolism. Ann. Pharmacother.40, 32–37 (2006).
   PubMed Web of Science ®Google Scholar
• Bramson C, Ouellet D, Roman D et al. A single-dose pharmacokinetic study of lasofoxifene in healthy volunteers and subjects with mild and moderate hepatic impairment. J. Clin. Pharmacol.46, 29–36 (2006).
   PubMed Web of Science ®Google Scholar
• Ouellet D, Bramson C, Carvajal-Gonzalez S et al. Effects of lasofoxifene on the pharmacokinetics and pharmacodynamics of single-dose warfarin. Br. J. Clin. Pharmacol.61, 741–745 (2006).
   PubMed Web of Science ®Google Scholar
• Lee A, Radecki D, Wolter K et al. Lasofoxifene Phase 2 and Phase 3 clinical trial design and strategy. J. Bone Miner. Res.20 (2005) (Abstract M384).
   Google Scholar
• Day W, Martel J, Lee A. Lasofoxifene Phase 2 dose response analysis in postmenopausal women. J. Bone Miner. Res.20 (2005) (Abstract M385).
   Google Scholar
• Portman DJ, Moffett AH, Bachman GA et al. Lasofoxifene, a selective estrogen receptor modulator, improves objective measures of vaginal atrophy. Obstet. Gynecol.103, S25–S26 (2004).
   Web of Science ®Google Scholar
• McClung MR, Siris E, Cummings S et al. Prevention of bone loss in postmenopausal women treated with lasofoxifene compared with raloxifene. Menopause13, 377–386 (2006).
   PubMed Web of Science ®Google Scholar
• McClung M, Omizo M, Weiss S et al. Comparison of lasofoxifene and raloxifene for the prevention of bone loss in postmenopausal women. J. Bone Miner. Res.19 (2004) (Abstract SA424).
   PubMed Web of Science ®Google Scholar
• McClung M, Portman D, Emkey R et al. Comparison of the extraskeletal effects of lasofoxifene and raloxifene. J. Bone Miner. Res.19 (2004) (Abstract SA423).
   PubMed Web of Science ®Google Scholar
• McClung M, Siris E, Cummings S et al. Lasofoxifene increased BMD of the spine and hip and decreased bone turnover markers in postmenopausal women with low or normal BMD. J. Bone Miner. Res.20 (2005) (Abstract F429).
   Google Scholar
• Davidson M, Moffett A, Welty F et al. Extraskeletal effects of lasofoxifene on postmenopausal women. J. Bone Miner. Res.20 (2005) (Abstract SA428).
   Google Scholar
• Eastell R, Reid DM, Vukicevic S et al. The effects of lasofoxifene on bone turnover markers: the PEARL trial. J. Bone Miner. Res.23 (2008) (Abstract 1287).
   Web of Science ®Google Scholar
• Glover SJ, Rogers A, Gossiel F, Eastell R. A randomized double blinded controlled trial of individual response in biochemical markers of bone turnover to lasofoxifene therapy.J. Bone Miner. Res.23 (2008) (Abstract M507).
   Google Scholar
• Cummings SR, Eastell R, Ensrud K et al. The effects of lasofoxifene on fractures and breast cancer: 3-year results from the PEARL trial. J. Bone Miner. Res.23 (2008) (Abstract 1288).
   Google Scholar
• Goldstein SR. Not all selective estrogen response modulators are created equal: update on lasofoxifene. Int. J. Gynecol. Cancer16(Suppl. 2), 504 (2006).
   PubMedGoogle Scholar
• Wang XN, Simmons HA, Salatto CT, Cosgrove PG, Thompson DD. Lasofoxifene enhances vaginal mucus formation without causing hypertrophy and increases estrogen receptor b and androgen receptor in rats. Menopause13, 609–620 (2006).
   PubMed Web of Science ®Google Scholar
• Moffett AH, Ettinger M, Bolognese M et al. Lasofoxifene, a next generation SERM, is effective in preventing loss of BMD and reducing LDL-C in postmenopausal women. J. Bone Miner. Res.19 (2004) (Abstract SA426).
   PubMedGoogle Scholar
• EMEA. European Medicines Agency, Pre-Authorisation Evaluation of Medicines for Human Use. Committee for Medicinal Products for Human Use summary of positive opinion for Fablyn. Document reference: EMEA/CHMP/609979/2008. European Medicines Agency, London, UK (2008).
   Google Scholar
• Bryant HU, Glasebrook AL, Yang NN, Sato M. A pharmacological review of raloxifene. J. Bone Miner. Metab.14, 1–9 (1996).
   Google Scholar
• Delmas PD, Bjarnason NH, Mitlak BH et al. Effects of raloxifene on bone mineral density, serum cholesterol concentrations, and uterine endometrium in postmenopausal women. N. Engl. J. Med.337, 1641–1647 (1997).
   PubMed Web of Science ®Google Scholar
• Lufkin EG, Whitaker MD, Nickelsen T et al. Treatment of established postmenopausal osteoporosis with raloxifene: a randomized trial. J. Bone Miner. Res.13, 1747–1754 (1998).
   PubMed Web of Science ®Google Scholar
• Ettinger B, Black DM, Mitlak BH et al.; Multiple Outcomes of Raloxifene Evaluation (MORE) Investigators. Reduction of vertebral fracture risk in postmenopausal women with osteoporosis treated with raloxifene: results from a 3-year randomized clinical trial. JAMA282, 637–645 (1999); erratum: JAMA282, 2124 (1999).
   PubMed Web of Science ®Google Scholar
• Cauley JA, Norton L, Lippman ME et al. Continued breast cancer risk reduction in postmenopausal women treated with raloxifene: 4-year results from the MORE trial. Multiple Outcomes of Raloxifene Evaluation. Breast Cancer Res. Treat.65, 125–134 (2001); correction: Breast Cancer Res. Treat.67 (2001).
   PubMed Web of Science ®Google Scholar
• Martino S, Cauley JA, Barrett-Connor E et al. Continuing outcomes relevant to Evista: breast cancer incidence in postmenopausal osteoporotic women in a randomized trial of raloxifene. J. Natl. Cancer. Inst.96, 1751–1761 (2004).
   PubMed Web of Science ®Google Scholar