Raloxifene: A review of its use in the prevention of invasive breast cancer

Drugs

Volumn 68, Issue 14, 2008, Pages 2059-2083

  Moen, Marit D ^a,b   Keating, Gillian M ^a,b  

^a ADIS INTERNATIONAL LIMITED   (New Zealand)

^b WOLTERS KLUWER HEALTH   (United States)

Author keywords

Adis drug profiles; Breast cancer, treatment; Raloxifene, general

Indexed keywords

AMOXICILLIN; AMPICILLIN; ANTACID AGENT; CORTICOSTEROID; DIGOXIN; HIGH DENSITY LIPOPROTEIN; LOW DENSITY LIPOPROTEIN; PLACEBO; RALOXIFENE; SEX HORMONE BINDING GLOBULIN; SIMVASTATIN; SOMATOMEDIN C; TAMOXIFEN; TRIACYLGLYCEROL; WARFARIN;

ALCOHOL CONSUMPTION; BONE DENSITY; BONE METABOLISM; BREAST CANCER; CANCER CELL; CANCER INVASION; CANCER PREVENTION; CANCER RISK; CARDIOVASCULAR DISEASE; CATARACT; CELL PROLIFERATION; CHEMOPROPHYLAXIS; CLINICAL TRIAL; DEEP VEIN THROMBOSIS; DISEASE COURSE; DISEASE SEVERITY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG EFFECT; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; DRUG TOLERABILITY; DRUG WITHDRAWAL; ENDOMETRIAL DISEASE; ENDOMETRIUM CANCER; ENDOMETRIUM HYPERPLASIA; FLU LIKE SYNDROME; FOLLOW UP; FRACTURE REDUCTION; GALLBLADDER DISEASE; HOT FLUSH; HUMAN; HYPERCHOLESTEROLEMIA; LEG CRAMP; LIPID BLOOD LEVEL; OSTEOPOROSIS; PERIPHERAL EDEMA; POSTMENOPAUSE; QUALITY OF LIFE; RECOMMENDED DRUG DOSE; REVIEW; RISK REDUCTION; STROKE; TREATMENT DURATION; TREATMENT INDICATION; TREATMENT OUTCOME; TREATMENT RESPONSE; VENOUS THROMBOEMBOLISM;

BREAST NEOPLASMS; FEMALE; HUMANS; MIDDLE AGED; NEOPLASM INVASIVENESS; OSTEOPOROSIS, POSTMENOPAUSAL; QUALITY OF LIFE; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATORS;

EID: 51449103629     PISSN: 00126667     EISSN: 00126667     Source Type: Journal    
DOI: 10.2165/00003495-200868140-00008     Document Type: Review

References (78)

1. American Cancer Society. Cancer facts and figures 2008 [online]. Available from URL: http://www.cancer.org/downloads/STT/2008CAFFfinalsecured.pdf [Accessed 2008 Aug 11]
2. breastcancer.org. Symptoms and diagnosis [online]. Available from URL: www.breastcancer.org/symptoms [Accessed 2008 May 30]
3. National Comprehensive Cancer Network (NCCN). Breast cancer risk reduction guidelines v.1.2008 [online]. Available from URL: http://www.nccn.org/ professionals/physician_gls/PDF/breast_risk.pdf [Accessed 2008 Apr 22]
4. Bao T, Prowell T, Stearns V. Chemoprevention of breast cancer: tamoxifen, raloxifene, and beyond. Am J Ther 2006 Jul-Aug; 13 (4): 337-48
5. Eli Lilly and Company. EVISTA (raloxifene hydrochloride): US prescribing information [online]. Available from URL: http://pi.lilly.com/us/evista-pi.pdf [Accessed 2008 Mar 12]
6. Balfour JA, Goa KL. Raloxifene. Drugs Aging 1998 Apr; 12 (4): 335-41; discussion 342
7. Clemett D, Spencer CM. Raloxifene: a review of its use in postmenopausal osteoporosis. Drugs 2000 Aug; 60 (2): 379-411
8. Cummings SR, Eckert S, Krueger KA, et al. The effect of raloxifene on risk of breast cancer in postmenopausal women: results from the MORE randomized trial. JAMA 1999 Jun 16; 281 (23): 2189-97
9. 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. Breast Cancer Res Treat 2001 Jan; 65 (2): 125-34
10. 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 2004 Dec 1; 96 (23): 1751-61
11. 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 Jun 21; 295 (23): 2727-41
12. Barrett-Connor E, Mosca L, Collins P, et al. Effects of raloxifene on cardiovascular events and breast cancer in postmenopausal women. N Engl J Med 2006 Jul 13; 355 (2): 125-37
13. Sporn MB, Dowsett SA, Mershon J, et al. Role of raloxifene in breast cancer prevention in postmenopausal women: clinical evidence and potential mechanisms of action. Clin Ther 2004 Jun; 26 (6): 830-40
14. Hochner-Celnikier D. Pharmacokinetics of raloxifene and its clinical application. Eur J Obstet Gynecol Reprod Biol 1999 Jul; 85 (1): 23-9
15. Escande A, Pillon A, Servant N, et al. Evaluation of ligand selectivity using reporter cell lines stably expressing estrogen receptor alpha or beta. Biochem Pharmacol 2006 May 14; 71 (10): 1459-69
16. Wolczynski S, Surazynski A, Swiatecka J, et al. Estrogenic and antiestrogenic effects of raloxifene on collagen metabolism in breast cancer MCF-7 cells. Gynecol Endocrinol 2001 Jun; 15 (3): 225-33
17. Glaeser M, Niederacher D, Djahansouzi S, et al. Effects of the antiestrogens tamoxifen and raloxifene on the estrogen receptor transactivation machinery. Anticancer Res 2006 Jan-Feb; 26 (1B): 735-44
18. Anzano MA, Peer CW, Smith JM, et al. Chemoprevention of mammary carcinogenesis in the rat: combined use of raloxifene and 9-cis-retinoic acid. J Natl Cancer Inst 1996 Jan 17; 88 (2): 123-5
19. Clemens JA, Bennett DR, Black LJ, et al. Effects of a new antiestrogen, keoxifene (LY156758), on growth of carcinogen-induced mammary tumors and on LH and prolactin levels. Life Sci 1983 Jun 20; 32 (25): 2869-75
20. Osborne CK, Hobbs K, Clark GM. Effect of estrogens and antiestrogens on growth of human breast cancer cells in athymic nude mice. Cancer Res 1985 Feb; 45 (2): 584-90
21. Dowsett M, Bundred NJ, Decensi A, et al. Effect of raloxifene on breast cancer cell Ki67 and apoptosis: a double-blind, placebo-controlled, randomized clinical trial in postmenopausal patients. Cancer Epidemiol Biomarkers Prev 2001 Sep; 10 (9): 961-6
22. Freedman M, San Martin J, O'Gorman J, et al. Digitized mammography: a clinical trial of postmenopausal women randomly assigned to receive raloxifene, estrogen, or placebo. J Natl Cancer Inst 2001 Jan 3; 93 (1): 51-6
23. Eilertsen AL, Karssemeijer N, Skaane P, et al. Differential impact of conventional and low-dose oral hormone therapy, tibolone and raloxifene on mammographic breast density, assessed by an automated quantitative method. BJOG 2008 May; 115 (6): 773-9
24. Christodoulakos GE, Lambrinoudaki IV, Vourtsi AD, et al. Mammographic changes associated with raloxifene and tibolone therapy in postmenopausal women: a prospective study. Menopause 2002 Mar-Apr; 9 (2): 110-6
25. Jackson VP, San Martin JA, Secrest RJ, et al. Comparison of the effect of raloxifene and continuous-combined hormone therapy on mammographic breast density and breast tenderness in postmenopausal women. Am J Obstet Gynecol 2003 Feb; 188 (2): 389-94
26. da Silva BB, Moita DS, Pires CG, et al. Evaluation of insulin-like growth factor-I in postmenopausal women with breast cancer treated with raloxifene. Int Semin Surg Oncol 2007; 4: 18
27. Torrisi R, Baglietto L, Johansson H, et al. Effect of raloxifene on IGF-I and IGFBP-3 in postmenopausal women with breast cancer. Br J Cancer 2001 Dec 14; 85 (12): 1838-41
28. Eng-Wong J, Hursting SD, Venzon D, et al. Effect of raloxifene on insulin-like growth factor-I, insulin-like growth factor binding protein-3, and leptin in premenopausal women at high risk for developing breast cancer. Cancer Epidemiol Biomarkers Prev 2003 Dec; 12 (12): 1468-73
29. Johansson H, Bonanni B, Mariette F, et al. Effects of raloxifene on sex steroid hormones and C-telopeptide in postmenopausal women with primary breast cancer. Breast Cancer Res Treat 2006 Jul; 98 (2): 167-72
30. 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 1997 Dec 4; 337 (23): 1641-7
31. Goldstein SR, Scheele WH, Rajagopalan SK, et al. A 12-month comparative study of raloxifene, estrogen, and placebo on the postmenopausal endometrium. Obstet Gynecol 2000 Jan; 95 (1): 95-103
32. Jolly EE, Bjarnason NH, Neven P, et al. Prevention of osteoporosis and uterine effects in postmenopausal women taking raloxifene for 5 years. Menopause 2003 Jul-Aug; 10 (4): 337-44
33. Martino S, Disch D, Dowsett SA, et al. Safety assessment of raloxifene over eight years in a clinical trial setting. Curr Med Res Opin 2005 Sep; 21 (9): 1441-52
34. Fisher B, Costantino JP, Wickerham DL, et al. Tamoxifen for prevention of breast cancer: report of the National Surgical Adjuvant Breast and Bowel Project P-1 Study. J Natl Cancer Inst 1998 Sep 16; 90 (18): 1371-88
35. Johnston Jr CC, Bjarnason NH, Cohen FJ, et al. Long-term effects of raloxifene on bone mineral density, bone turnover, and serum lipid levels in early postmenopausal women: three-year data from 2 double-blind, randomized, placebo-controlled trials. Arch Intern Med 2000 Dec 11-25; 160 (22): 3444-50
36. Reid IR, Eastell R, Fogelman I, et al. A comparison of the effects of raloxifene and conjugated equine estrogen on bone and lipids in healthy postmenopausal women. Arch Intern Med 2004 Apr 26; 164 (8): 871-9
37. Heaney RP, Draper MW. Raloxifene and estrogen: comparative bone-remodeling kinetics. J Clin Endocrinol Metab 1997 Oct; 82 (10): 3425-9
38. 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. Multiple Outcomes of Raloxifene Evaluation (MORE) Investigators. JAMA 1999 Aug 18; 282 (7): 637-45
39. 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 2000 Jun; 85 (6): 2197-202
40. Ott SM, Oleksik A, Lu Y, et al. Bone histomorphometric and biochemical marker results of a 2-year placebo-controlled trial of raloxifene in postmenopausal women. J Bone Miner Res 2002 Feb; 17 (2): 341-8
41. Barrett-Connor E, Grady D, Sashegyi A, et al. Raloxifene and cardiovascular events in osteoporotic postmenopausal women: four-year results from the MORE (Multiple Outcomes of Raloxifene Evaluation) randomized trial. JAMA 2002 Feb 20; 287 (7): 847-57
42. Walsh BW, Kuller LH, Wild RA, et al. Effects of raloxifene on serum lipids and coagulation factors in healthy postmenopausal women. JAMA 1998 May 13; 279 (18): 1445-51
43. Insull Jr W, Davidson MH, Kulkarni PM, et al. Effects of raloxifene and low-dose simvastatin coadministration on plasma lipids in postmenopausal women with primary hypercholesterolemia. Metabolism 2005 Jul; 54 (7): 939-46
44. Yaffe K, Krueger K, Sarkar S, et al. Cognitive function in postmenopausal women treated with raloxifene. N Engl J Med 2001 Apr 19; 344 (16): 1207-13
45. Yaffe K, Krueger K, Cummings SR, et al. Effect of raloxifene on prevention of dementia and cognitive impairment in older women: the Multiple Outcomes of Raloxifene Evaluation (MORE) randomized trial. Am J Psychiatry 2005 Apr; 162 (4): 683-90
46. Morello KC, Wurz GT, DeGregorio MW. Pharmacokinetics of selective estrogen receptor modulators. Clin Pharmacokinet 2003; 42 (4): 361-72
47. Czock D, Keller F, Heringa M, et al. Raloxifene pharmacokinetics in males with normal and impaired renal function. Br J Clin Pharmacol 2005 Apr; 59 (4): 479-82
48. Miller JW, Skerjanec A, Knadler MP, et al. Divergent effects of raloxifene HCI on the pharmacokinetics and pharmacodynamics of warfarin. Pharm Res 2001 Jul; 18 (7): 1024-8
49. Land SR, Wickerham DL, Costantino JP, et al. Patient-reported symptoms and quality of life during treatment with tamoxifen or raloxifene for breast cancer prevention: the NSABP Study of Tamoxifen and Raloxifene (STAR) P-2 trial. JAMA 2006 Jun 21; 295 (23): 2742-51
50. Costantino JP, Gail MH, Pee D, et al. Validation studies for models projecting the risk of invasive and total breast cancer incidence. J Natl Cancer Inst 1999 Sep 15; 91 (18): 1541-8
51. Lippman ME, Krueger KA, Eckert S, et al. Indicators of lifetime estrogen exposure: effect on breast cancer incidence and interaction with raloxifene therapy in the multiple outcomes of raloxifene evaluation study participants. J Clin Oncol 2001 Jun 15; 19 (12): 3111-6
52. Cummings SR, Duong T, Kenyon E, et al. Serum estradiol level and risk of breast cancer during treatment with raloxifene. JAMA 2002 Jan 9; 287 (2): 216-20
53. Johnell O, Cauley JA, Kulkarni PM, et al. Raloxifene reduces risk of vertebral fractures and breast cancer in postmenopausal women regardless of prior hormone therapy. J Fam Pract 2004; 53 (10): 789-96
54. Goldstein SR, Mershon J, Wong M, et al. Effects of raloxifene on the incidence of invasive breast cancer in postmenopausal women at low and high risk of breast cancer by the Gail model [abstract no. P-37]. 17th Annual Meeting of the North American Menopause Society; 2006 Oct 11-14; Nashville (TN)
55. Martino S, Powles T, Cauley J, et al. Effect of raloxifene on incidence of invasive breast cancer in postmenopausal women stratified by baseline serum estradiol: results of the Continuing Outcomes Relevant to Evista® (CORE) trial [abstract no. 22]. Breast Cancer Res Treat 2004; 88 Suppl. 1: S14
56. Lippman ME, Cummings SR, Disch DP, et al. Effect of raloxifene on the incidence of invasive breast cancer in postmenopausal women with osteoporosis categorized by breast cancer risk. Clin Cancer Res 2006 Sep 1; 12 (17): 5242-7
57. Burshell AL, Song J, Dowsett SA, et al. Relationship between bone mass, invasive breast cancer incidence and raloxifene therapy in postmenopausal women with low bone mass or osteoporosis. Curr Med Res Opin 2008; 24 (3): 807-13
58. Purdie D, Cauley J, Disch D, et al. Effect of raloxifene on incidence of invasive breast cancer in postmenopausal women having a history of prior hormone therapy use: results of the CORE trial [abstract no. 4IN]. Ann Oncol 2004; 15 Suppl. 3: iii2
59. Gail MH, Brinton LA, Byar DP, et al. Projecting individualized probabilities of developing breast cancer for white females who are being examined annually. J Natl Cancer Inst 1989 Dec 20; 81 (24): 1879-86
60. Grady D, Cauley JA, Geiger MJ, et al. Reduced incidence of invasive breast cancer with raloxifene among women at increased coronary risk. J Natl Cancer Inst 2008 Jun 18; 100 (12): 854-61
61. Gradishar WJ, Cella D. Selective estrogen receptor modulators and prevention of invasive breast cancer. JAMA 2006 Jun 21; 295 (23): 2784-6
62. Gail MH, Costantino JP. Validating and improving models for projecting the absolute risk of breast cancer. J Natl Cancer Inst 2001 Mar 7; 93 (5): 334-5
63. Bondy ML, Newman LA. Assessing breast cancer risk: evolution of the Gail Model. J Natl Cancer Inst 2006 Sep 6; 98 (17): 1172-3
64. National Surgical Adjuvant Breast and Bowel Project (NSABP). Calculate your breast cancer risk [online]. Available from URL: http://www. breastcancerprevention.org/raf_source.asp [Accessed 2008 Jul 1]
65. National Cancer Institute. Breast cancer risk assessment tool [online]. Available from URL: http://www.cancer.gov/bcrisktool/ [Accessed 2008 Jul 1]
66. AstraZeneca Pharmaceuticals. Nolvadex (tamoxifen citrate): US prescribing information [online]. Available from URL: http://www.drugs.com/pro/nolvadex. html [Accessed 2008 May 21]
67. Jordan VC. The rise of raloxifene and the fall of invasive breast cancer. J Natl Cancer Inst 2008 Jun 18; 100 (12): 831-3
68. Buzdar AU, Marcus C, Holmes F, et al. Phase II evaluation of Ly156758 in metastatic breast cancer. Oncology 1988; 45 (5): 344-5
69. Gradishar W, Glusman J, Lu Y, et al. Effects of high dose raloxifene in selected patients with advanced breast carcinoma. Cancer 2000 May 1; 88 (9): 2047-53
70. Bevers TB. Raloxifene and the prevention of breast cancer. Expert Opin Pharmacother 2006 Nov; 7 (16): 2301-7
71. Lee WL, Chao HT, Cheng MH, et al. Rationale for using raloxifene to prevent both osteoporosis and breast cancer in postmenopausal women. Maturitas 2008 Jun 20; 60 (2): 92-107
72. Gennari L, Merlotti D, Paola VD, et al. Raloxifene in breast cancer prevention. Expert Opin Drug Saf 2008 May; 7 (3): 259-70
73. Tjia J, Micco E, Armstrong K. Interest in breast cancer chemoprevention among older women. Breast Cancer Res Treat 2008 Apr; 108 (3): 435-53
74. Bastian LA, Lipkus IM, Kuchibhatla MN, et al. Women's interest in chemoprevention for breast cancer. Arch Intern Med 2001 Jul 9; 161 (13): 1639-44
75. Fabian CJ. The what, why and how of aromatase inhibitors: hormonal agents for treatment and prevention of breast cancer. Int J Clin Pract 2007; 61 (12): 2051-63
76. Savage L. NCI director opts against breast cancer prevention trial in favor of biomarkers. J Natl Cancer Inst 2007 Sep 5; 99 (17): 1282-3, 1289
77. Jordan VC. Beyond raloxifene for the prevention of osteoporosis and breast cancer. Br J Pharmacol 2007 Jan; 150 (1): 3-4
78. Deshmane V, Krishnamurthy S, Melemed AS, et al. Phase III double-blind trial of arzoxifene compared with tamoxifen for locally advanced or metastatic breast cancer. J Clin Oncol 2007 Nov 1; 25 (31): 4967-73