Arzoxifene: A promising new selective estrogen receptor modulator for clinical chemoprevention of breast cancer

Clinical Cancer Research

Volumn 10, Issue 16, 2004, Pages 5313-5315

  Sporn, Michael B ^a  

^a DARTMOUTH MEDICAL SCHOOL   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ARZOXIFENE; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; NEW DRUG; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TAMOXIFEN;

ANTINEOPLASTIC ACTIVITY; BREAST CANCER; CANCER PREVENTION; CLINICAL TRIAL; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; GENE EXPRESSION; HUMAN; NONHUMAN; NOTE; PHARMACODYNAMICS; POSTMENOPAUSE; PRIORITY JOURNAL; SIDE EFFECT; STRUCTURE ACTIVITY RELATION;

ANTICARCINOGENIC AGENTS; BREAST NEOPLASMS; FEMALE; HUMANS; MOLECULAR STRUCTURE; NEOPLASM STAGING; PIPERIDINES; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATORS; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES;

EID: 4143071454     PISSN: 10780432     EISSN: None     Source Type: Journal    
DOI: 10.1158/1078-0432.CCR-04-1377     Document Type: Note

References (25)

1. 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;90:1371-88.
2. 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. Multiple outcomes of raloxifene evaluation. J Am Med Assoc 1999;281:2189-97.
3. 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 2001;65:125-34.
4. Katzenellenbogen BS, Katzenellenbogen JA. Defining the "S" in SERMs. Science 2002;295:2380-1.
5. Turgeon JL, McDonnell DP, Martin KA, Wise PM. Hormone therapy: physiological complexity belies therapeutic simplicity. Science 2004;304:1269-73.
6. Smith CL, O'Malley BW. Coregulator function: a key to understanding tissue specificity of selective receptor modulators. Endocr Rev 2004;25:45-71.
7. Shang Y, Brown M. Molecular determinants for the tissue specificity of SERMs. Science 2002;495:2465-8.
8. Bergman L, Beelen ML, Gallee MP, Hollema H, Benraadt J, van Leeuwen FE. Risk and prognosis of endometrial cancer after tamoxifen for breast cancer. Comprehensive Cancer Centres' ALERT Group. Assessment of liver and endometrial cancer risk following tamoxifen Lancet 2000;356:881-7.
9. Fabian CJ, Kimler BF, Anderson J, et al. Breast cancer chemoprevention Phase I evaluation of biomarker modulation by arzoxifene, a third generation selective estrogen receptor modulator. Clin Cancer Res 2004;10:5403-17.
10. Baselga J, Llombart-Cussac A, Bellet M, et al. Randomized, double-blind, multicenter trial comparing two doses of arzoxifene (LY353381) in hormone-sensitive advanced or metastatic breast cancer patients. Ann Oncol 2003;14:1383-90.
11. Buzdar A, O'Shaughnessey JA, Booser DJ, et al. Phase II, randomized, double-blind study of two dose levels of arzoxifene in patients with locally advanced or metastatic breast cancer. J Clin Oncol 2003;21: 1007-14.
12. Suh N, Glasebrook AL, Palkowitz AD, et al. Arzoxifene, a new selective estrogen receptor modulator for chemoprevention of experimental breast cancer. Cancer Res 2001;61:8412-5.
13. Ma YL, Bryant HU, Zeng Q, et al. Long-term dosing of arzoxifene lowers cholesterol, reduces bone turnover, and preserves bone quality in ovariectomized rats. J Bone Miner Res 2002;17:2256-64.
14. Rendi MH, Suh N, Lamph WW, et al. The selective estrogen receptor modulator arzoxifene and the rexinoid LG1002688 cooperate to promote transforimg growth factor-β-dependent apoptosis in breast cancer. Cancer Res 2004;64:3566-71.
15. Wakefield LM, Roberts AB. TGF-β signaling: positive and negative effects on tumorigenesis. Curr Opin Genes Dev 2002;12:22-9.
16. Pollak MN, Schernhammer ES, Hankinson SE. Insulin-like growth factors and neoplasia. Nat Rev Cancer 2004;4:505-18.
17. Renehan AG, Zwahlen M, Minder C, O-Dwyer ST, Shalet SM, Egger M. Insulin-like growth factor (IGF)-1, IGF binding protein-3, and cancer risk: systematic review and meta-regression analysis. Lancet 2004;363:13346-53.
18. Luo S, Labrie C, Bélanger A, Candas B, Labrie F. Prevention of development of dimethylbenz(a)anthracene (DMBA)-induced mammary tumors in the rat by the new nonsteroidal antiestrogen EM-800 (SCH57050). Breast Cancer Res Treat 1998;49:1-11.
19. Labrie F, Champagne P, Labrie C, et al. Activity and safety of the antiestrogen EM-800, the orally active precursor of acolbifene, in tamoxifen-resistant breast cancer. J Clin Oncol 2004;22:864-71.
20. Cohen LA, Pittman B, Wang C-X, Aliaga C, Yu L, Moyer JD. 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 2001;61:8683-8.
21. Ke HZ, Foley GL, Simmons HA, Shen V, Thompson DD. Long-term treatment of lasofoxifene preserves bone mass and bone strength and does not adversely affect the uterus in ovariectomized rats. Endocrinology 2004;145:1996-2005.
22. Petricoin EF, Zoon KC, Kohn EC, Barrett JC, Liotta LA. Clinical proteomics: translating benchside promise into bedside reality. Nat Rev Drug Discov 2002;1:683-95.
23. Wulfkuhle JD, Liotta LA, Petricoin EF. Proteomic applications for the early detection of cancer. Nat Rev Cancer 2003;3:267-75.
24. Suh N, Lamph WW, Glasebrook AL, et al. Prevention and treatment of experimental breast cancer with the combination of a new selective estrogen receptor modulator, arzoxifene, and a new rexinoid, LG 100268. Clin Cancer Res 2002;8:3270-5.
25. Spom MB. Hobson's choice and the need for combinations of new agents for the prevention and treatment of breast cancer. J Natl Cancer Inst 2002;94:242-3.