Lasofoxifene: Selective estrogen receptor modulator for the prevention and treatment of postmenopausal osteoporosis;Lasofoxifeno: SERM para la prevención y tratamiento de osteoporosis posmenopáusica

Annals of Pharmacotherapy

Volumn 45, Issue 4, 2011, Pages 499-509

  Peterson, Gregory M ^a   Naunton, Mark ^b   Tichelaar, Lisette K ^c   Gennari, Luigi ^d  

^a UNIVERSITY OF TASMANIA   (Australia)

^b CHARLES DARWIN UNIVERSITY   (Australia)

^c UNIVERSITY OF GRONINGEN   (Netherlands)

^d UNIVERSITY OF SIENA   (Italy)

Author keywords

Lasofoxifene; Osteoporosis; Selective estrogen receptor modulator

Indexed keywords

ALKALINE PHOSPHATASE BONE ISOENZYME; AMINO TERMINAL TELOPEPTIDE; BAZEDOXIFENE; CALCIUM; CONJUGATED ESTROGEN; DEOXYPYRIDINOLINE; ESTRADIOL; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; LASOFOXIFENE; OSPEMIFENE; OSTEOCALCIN; PLACEBO; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TAMOXIFEN; TOREMIFENE; VITAMIN D;

AREA UNDER THE CURVE; ARTICLE; BONE DENSITY; BONE TURNOVER; CANDIDIASIS; DIET SUPPLEMENTATION; DOSE RESPONSE; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG EFFICACY; DRUG ELIMINATION; DRUG FECES LEVEL; DRUG HALF LIFE; DRUG INDUCED CANCER; DRUG METABOLISM; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG URINE LEVEL; ENDOMETRIUM CANCER; ENDOMETRIUM HYPERPLASIA; ENDOMETRIUM POLYP; ESTROGEN THERAPY; HIP; HOT FLUSH; HUMAN; IN VITRO STUDY; IN VIVO STUDY; LEG CRAMP; LOADING DRUG DOSE; LUMBAR SPINE; NONHUMAN; PELVIC ORGAN PROLAPSE; POSTMENOPAUSE; POSTMENOPAUSE OSTEOPOROSIS; PRIORITY JOURNAL; SIDE EFFECT; URINE INCONTINENCE; UTERUS MYOMA; VAGINA BLEEDING; VENOUS THROMBOEMBOLISM;

CLINICAL TRIALS AS TOPIC; FEMALE; HUMANS; OSTEOPOROSIS, POSTMENOPAUSAL; PYRROLIDINES; SELECTIVE ESTROGEN RECEPTOR MODULATORS; TETRAHYDRONAPHTHALENES; UNITED STATES; UNITED STATES FOOD AND DRUG ADMINISTRATION;

EID: 79955625121     PISSN: 10600280     EISSN: None     Source Type: Journal    
DOI: 10.1345/aph.1P604     Document Type: Article

References (60)

1. Sambrook P, Cooper C. Osteoporosis. Lancet 2006;367:2010-8.
2. Poole KES, Compston JE. Osteoporosis and its management. BMJ 2006;333:1251-6.
3. Mulder JE, Kolatkar NS, LeBoff MS. Drug insight: existing and emerging therapies for osteoporosis. Nature Clin Pract Endocrinol Metab 2006;2:670-80.
4. Eichner SF, Lloyd KB, Timpe EM. Comparing therapies for postmenopausal osteoporosis prevention and treatment. Ann Pharmacother 2003;37:711-24. DOI 10.1345/aph.1C246
5. Department of Health and Human Services. Bone health and osteoporosis: a report of the Surgeon General. Rockville, MD: US Department of Health and Human Services, Office of the Surgeon General, 2004.
6. Cummings S, Melton L. Epidemiology and outcomes of osteoporotic fractures. Lancet 2002;359:1761-7.
7. Hogson S, Watts N, Bilezikian J, Clark B, Gray T, Harris D. American Association of Clinical Endocrinologists 2001 Medical Guidelines for Clinical Practice for the Prevention and Management of Postmenopausal Osteoporosis. Endocr Pract 2001;7:294-312.
8. Gold D, Lee L, Tresolini C. Working with patients to prevent, treat, and manage osteoporosis: a curriculum guide for the health professions. 3rd ed. Durham, NC: Center for the Study of Aging and Human Development, Duke University Medical Center, 2001.
9. Gennari L. Lasofoxifene (Pfizer). Curr Opin Invest Drugs 2005;6:1067-78.
10. Herrington D. Effects of estrogen replacement on the progression of coronary-artery atherosclerosis. N Engl J Med 2000;343:522-9.
11. Manson JE, Hsia J, Johnson KC, et al. Estrogen plus progestin and the risk of coronary heart disease. N Engl J Med 2003;349:523-34.
12. Hulley S. Randomized trial of estrogen plus progestin for secondary prevention of coronary heart disease in postmenopausal women. JAMA 1998;290:605-13.
13. HRT: what are women (and their doctors) to do? Lancet 2004;364:2069-70.
14. Vassilopoulou-Sellin R. Breast cancer and hormonal replacement therapy. Ann N Y Acad Sci 2003;997:341-50.
15. Dull P. Hormone replacement therapy. Prim Care 2006;33:953-63.
16. Close P, Neuprez A, Reginster JY. Developments in the pharmacotherapeutic management of osteoporosis. Exp Opin Pharmacother 2006;7:1603-15.
17. Deal C. Osteoporosis therapies: bisphosphonates, SERMs, PTH, and new therapies. Clin Rev Bone Min Metab 2005;3:125-41.
18. Chapurlat R, Delmas PD. New treatments of osteoporosis. Revue de Med Intern 2004;25(suppl 5):S573-9.
19. Scottish Intercollegiate Guidelines Network (SIGN). Management of osteoporosis. A clinical guideline. National Guideline Clearinghouse, June 2003.
20. Gennari L. Lasofoxifene: a new type of selective estrogen receptor modulator for the treatment of osteoporosis. Drugs Today 2006;42:355-67.
21. Chaki O. [Next generation selective estrogen receptor modulators]. Clin Calcium 2006;16:145-52.
22. Petersen NM, Briggs AL. Selective estrogen receptor modulators. Clin Rev Bone Min Metab 2005;3:19-30.
23. Riggs BL, Hartmann LC. Selective estrogen-receptor modulators-mechanisms of action and application to clinical practice. N Engl J Med 2003;348:618-29.
24. Vogelvang TE, Van Der Mooren MJ, Mijatovic V, Kenemans P. Emerging selective estrogen receptor modulators: special focus on effects on coronary heart disease in postmenopausal women. Drugs 2006;66:191-221.
25. McClung M, Siris E, Cummings S. Lasofoxifene increased BMD of the spine and hip and decreased bone turnover markers in postmenopausal women with low or normal BMD. J Bone Min Res 2005;20:F429.
26. Davidson M, Moffett A, Welty F, et al. Extraskeletal effects of lasofoxifene on postmenopausal women. J Bone Min Res 2005;20:S173.
27. McClung MR, Siris E, Cummings S, et al. Prevention of bone loss in postmenopausal women treated with lasofoxifene compared with raloxifene. Menopause 2006;13:377-86.
28. Cummings SR, Eastell R, Ensrud K. The effects of lasofoxifene on fractures and breast cancer: 3 year results from the PEARL trial. J Bone Miner Res 2008;23:s81.
29. Cummings SR, Ensrud K, Delmas PD, et al. Lasofoxifene in postmenopausal women with osteoporosis. N Engl J Med 2010;362:686-96.
30. DeMichele A. Impact of raloxifene or tamoxifene use on endometrial cancer risk: a population-based case-control study. J Clin Oncol 2008;26: 415-9.
31. Ettinger B, Black DM, Mitlak BH, et al. Reduction of vertebral fracture risk in postmenopausal women with osteoporosis treated with raloxifene: results from a 3-year randomized clinical trial. JAMA 1999;282:637-45.
32. Siris ES, Harris ST, Eastell R, et al. Skeletal effects of raloxifene after 8 years: results from the continuing outcomes relevant to Evista (CORE) study. J Bone Mine Res 2005;20:1514-24.
33. Goldstein SR. Not all SERMs are created equal. Menopause 2006;13: 325-7.
34. Kelly J. FDA turns down lasofoxifene for osteoporosis. Medscape September 15, 2005. http://www.medscape.com/viewarticle/538340 (accessed July 1, 2010).
35. New Drugs Online Report for lasofoxifene. UK Medicines Information New Drugs Online. http://www.ukmi.nhs.uk/applications/ndo/record_view_open.asp?newDrugID=3 184 (accessed July 1, 2010).
36. Pfizer receives FDA complete response letter for lasofoxifene. January 2009. http://www.medicalnewstoday.com/articles/135923.php (accessed July 1, 2010).
37. Gennari L, Merlotti D, Martini G, Nuti R. Lasofoxifene: a third-generation selective estrogen receptor modulator for the prevention and treatment of osteoporosis. Exp Opin Invest Drugs 2006;15:1091-103.
38. Hochner-Celnikier D. Pharmacokinetics of raloxifene and its clinical application. Eur J Obstet Gynecol Reprod Biol 1999;85:23-9.
39. 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 2006;46:693-9.
40. Morello KC, Wurz GT, DeGregorio MW. Pharmacokinetics of selective estrogen receptor modulators. Clin Pharmacokinet 2003;42:361-72.
41. Rosati RL, Da Silva Jardine P, Cameron KO, et al. Discovery and preclinical pharmacology of a novel, potent, nonsteroidal estrogen receptor agonist/antagonist, CP-336156, a diaryltetrahydronaphthalene. J Med Chem 1998;41:2928-31.
42. Moller R, Fisher JM, Taylor A, Kolluri S, Gardner M. Effect of food on the pharmacokinetics of lasofoxifene, in healthy postmenopausal women. J Bone Miner Res 2004;19(SI):SU487.
43. Gardner M, Taylor A, Wei G, Calcagni A Jr, Duncan B, Milton A. Clinical pharmacology of multiple doses of lasofoxifene in postmenopausal women. J Clin Pharmacol 2006;46:52-8.
44. Johnson K, Gardner M, Prakash C. In vivo and in vitro metabolism of a next-generation selective estrogen receptor modulator, lasofoxifene, in humans. Drug Metab Rev 2004;36(suppl 1):246.
45. 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 2006;61:741-5.
46. Bramson C, Ouellet D, Roman D, Randinitis E, Gardner MJ. A singledose pharmacokinetic study of lasofoxifene in healthy volunteers and subjects with mild and moderate hepatic impairment. J Clin Pharmacol 2006;46:29-36.
47. Roman D, Bramson C, Ouellet D, Randinitis E, Gardner M. Effect of lasofoxifene on the pharmacokinetics of digoxin in healthy postmenopausal women. J Clin Pharmacol 2005;45:1407-12.
48. Moller RA, Fisher JM, Taylor AE, et al. Effects of steady-state lasofoxifene on CYP2D6-and CYP2E1-mediated metabolism. Ann Pharmacother 2006;40:32-7. DOI 10.1345/aph.1G347
49. Tukey RH, Strassburg CP. Human UDP-glucuronosyltransferases: metabolism, expression, and disease. Annu Rev Pharmacol Toxicol 2000;40:581-616.
50. Prakash C, Johnson KA, Gardner MJ. Disposition of lasofoxifene, a next-generation selective estrogen receptor modulator, in healthy male subjects. Drug Metab Dispos 2008;36:1218-26.
51. Goldstein SR. Not all selective estrogen response modulators are created equal: update on lasofoxifene. Int J Gynecol Cancer 2006;16(suppl 2):504.
52. Ke HZ, Paralkar VM, Grasser WA, et al. Effects of CP-336,156, a new, nonsteroidal estrogen agonist/antagonist, on bone, serum cholesterol, uterus and body composition in rat models. Endocrinology 1998;139:2068-76.
53. Ke Hua HZ, Brown TA, Thompson DD. Lasofoxifene (CP-336,156), a novel selective estrogen receptor modulator, in preclinical studies. J Am Aging Assoc 2002;25:87-99.
54. Moffett AH, Ettinger M, Bolognese M, et al. Lasofoxifene, next generation SERM, is effective in preventing loss of BMD and reducing LDL-C in postmenopausal women. J Bone Min Res 2004;19:S96.
55. Lee A, Radecki D, Wolter K. Lasofoxifene Phase II and Phase III clinical trial design and strategy. J Bone Min Res 2005;20:M384.
56. Wang XN, Simmons HA, Salatto CT, Cosgrove PG, Thompson DD. Lasofoxifene enhances vaginal mucus formation without causing hypertrophy and increases estrogen receptor (beta) and androgen receptor in rats. Menopause 2006;13:609-20.
57. Goldstein SR, Neven P, Cummings S, et al. Postmenopausal Evaluation and Risk Reduction with Lasofoxifene (PERARL) trial: 5-year gynecological outcomes. Menopause 2011;18:17-22. DOI 10.1097/gme.0b013e3181e84bb4
58. Delmanto A, Nahas-Neto J, Nahas EA, de Oliveira ML, Fernandes CE, Traiman P. Effect of raloxifene on the vaginal epithelium of postmenopausal women. Eur J Obstet Gynecol Reprod Biol 2008;139:187-92.
59. Vogel VG, Costantino JP, Wickerham DL, et al. Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial. JAMA 2006;295:2727-41.
60. Vogel VG, Costantino JP, Wickerham DL, et al. Update of the National Surgical Adjuvant Breast and Bowel Project Study of Tamoxifen and Raloxifene (STAR) P-2 Trial: preventing breast cancer. Cancer Prev Res (Phil) 2010;3:696-706.