Non-steroidal anti-estrogens in the treatment of breast cancer

Current Opinion in Investigational Drugs

Volumn 7, Issue 12, 2006, Pages 1085-1091

  Barker, Stewart ^a  

^a QUEEN MARY UNIVERSITY OF LONDON   (United Kingdom)

Author keywords

Anastrozole; ER ; ER ; Selective estrogen receptor downregulator; Selective estrogen receptor modulator; Tamoxifen

Indexed keywords

2 (3 FLUORO 4 HYDROXYPHENYL) 7 VINYL 5 BENZOXAZOLOL; 2,3 BIS(4 HYDROXYPHENYL)DIARYLPROPIONITRILE; 4 (1,2 DIPHENYL 1 BUTENYL)CINNAMIC ACID; 4 [4 METHYL 2 [4 [2 (1 PIPERIDINYL)ETHOXY]PHENYL] 7 PIVALOYLOXY 2H 1 BENZOPYRAN 3 YLPHENYL] PIVALATE; ACOLBIFENE; ANASTROZOLE; ANTIESTROGEN; AROMATASE INHIBITOR; ARZOXIFENE; BAZEDOXIFENE; DROLOXIFENE; ESTROGEN RECEPTOR ALPHA ANTAGONIST; ESTROGEN RECEPTOR ANTAGONIST; ESTROGEN RECEPTOR BETA AGONIST; FULVESTRANT; GW 7604; HORMONE RECEPTOR BLOCKING AGENT; HORMONE RECEPTOR STIMULATING AGENT; IDOXIFENE; LASOFOXIFENE; LETROZOLE; METHYLPIPERIDINOPYRAZOLE; NONSTEROID ANTIESTROGEN; PIPENDOXIFENE; PRINABEREL; RALOXIFENE; SELECTIVE ESTROGEN RECEPTOR MODULATOR; TAMOXIFEN; TOREMIFENE; TRILOSTANE; UNINDEXED DRUG;

ALKALINE PHOSPHATASE BLOOD LEVEL; ANTINEOPLASTIC ACTIVITY; ARM FRACTURE; BREAST CANCER; CANCER HORMONE THERAPY; CANCER RESISTANCE; CANCER RISK; CANCER SURVIVAL; CARDIOVASCULAR DISEASE; CELL SURVIVAL; CEREBROVASCULAR ACCIDENT; CEREBROVASCULAR DISEASE; CLINICAL TRIAL; COLORECTAL CANCER; COMBINATION CHEMOTHERAPY; DEEP VEIN THROMBOSIS; DNA MICROARRAY; DRUG APPROVAL; DRUG CHOICE; DRUG EFFICACY; DRUG INDUCED CANCER; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG RESEARCH; DRUG SELECTIVITY; DRUG STRUCTURE; ENDOMETRIAL DISEASE; ENDOMETRIUM CANCER; GYNECOLOGIC CANCER; HEAD AND NECK CANCER; HIGH RISK POPULATION; HUMAN; HYPERCALCEMIA; HYPERCHOLESTEROLEMIA; LEG FRACTURE; LONG TERM CARE; LUNG CANCER; LUNG EMBOLISM; LYMPHOMA; MEDICAL DECISION MAKING; MONOTHERAPY; NONHUMAN; OSTEOPOROSIS; POSTMENOPAUSE; PROGNOSIS; REVIEW; SIDE EFFECT; SPINE FRACTURE; STRUCTURE ACTIVITY RELATION; THROMBOEMBOLISM; THROMBOSIS; TISSUE SPECIFICITY; TREATMENT PLANNING; UNSPECIFIED SIDE EFFECT; VASCULAR DISEASE; VEIN THROMBOSIS; VENOUS THROMBOEMBOLISM; WRIST FRACTURE;

ANIMALS; ANTINEOPLASTIC AGENTS; BREAST NEOPLASMS; CLINICAL TRIALS; ESTROGEN ANTAGONISTS; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; FEMALE; HUMANS; SELECTIVE ESTROGEN RECEPTOR MODULATORS;

EID: 33845637854     PISSN: 14724472     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Review

References (68)

1. Bonneterre J, Buzdar A, Nabholtz J-M, Robertson JF, Thurliman B, von Euler M, Sahmoud T, Webster A, Steinberg M: Anastrozole is superior to tamoxifen as first-line therapy in hormone receptor positive advanced breast carcinoma: Results of two randomized designed for combined analysis. Cancer (2001) 92(9):2247-2258.
2. Barker S: Anti-estrogena in the treatment of breast cancer: Current status and future directions. Curr Opin Investig Drugs (2003) 4(6):652-657.
3. Stasi R, Thornton H: Questions about anastrozole for early breast cancer. Lancet (2002) 360(9348):1890-1891.
4. Buzdar A, Howell A, Cuzick J, Wale C, Distler W, Hoctin-Boes G, Houghton J, Locker GY, Nabhoitz M: Comprehensive profile of anastrozole and tamoxifen as adjuvant treatment for early-stage breast cancer Long-term safety analysis of the ATAC trial. Lancet Oncol (2006) 7(8):633-643.
5. Mokbel R, Karat I, Mokbel K: Adjuvant endocrine therapy for postmenopausal breast cancer in the era of aromatase inhibitors: An update. Int Semin Surg Oncol (2006) 3:31-34.
6. Spicar J, Ellis P: Towards optimal endocrine therapy for hormone-inhibition. Cancer Lett (2006):doi:10.16/j.canlet.2006.07.002.
7. Pemberton KD, Melissari E, Kakkar W: The influence of tamoxifen in vivo on the main natural anticoagulants and fibrinolysis. Blood Coagul Fibrinolysis (1993) 4(6):935-942.
8. Bushnell CD, Goldstein LB: Risk of ischemic stroke with tamoxifen treatment for breast cancer: A meta-analysis. Neurology (2004) 63(7):1230-1233.
9. Vogel VG, Costantino JP, Wickerham DL, Cronin WM, Cecchini RS, Atkins JN, Bevers TB, Fehrenbacher L, Pajon ER, Wade JL, Robidoux A et at. Effects of tamoxifen vs raloxifene on the risk of developing invasive breast cancer and other disease outcomes. J Am Med Assoc (2006) 295(23):2727-2741.
10. Vitseva O, Flockhart DA, Jin Y, Varghese S, Freedman JE: The effects of tamoxifen and its metabolites on platelet function and release of reactive oxygen intermediates. J Pharmacol Exp Ther (2005) 312(3):1144-1150.
11. Cosman F, Baz-Hecht M, Cushman M, Vardy MD, Cruz JD, Nieves JW, Zion M, Lindsay R: Short-term effects of estrogon, tamoxifen and raloxifene on hemostasis: A rendomised-controlled study and review of the literature. Thromb Res (2005) 116(1): 1-13.
12. Ozeren M, Karahan SO, Ozgur M, Eminagaoglu S, Unsal M, Baytan S, Bozkaya H: The effects of short-term reloxifene therapy on fibrinolysis markers: TAFI, tPA, and PAI-1. Acta Obstet Gynecol Scand (2005) 84(10):987-991.
13. Goldstein SR: Controversy about uterine effects and safety of SERMs: The saga continues. Menopause (2002) 9(5):381-384.
14. Sherwin BB: Estrogen and cognitive aging in women. Trends Phermacol Sci (2002) 23(11):527-534.
15. Hosoda T, Nakajima H, Honjo H: Estrogen protects neuronal cells from amyloid β-induced apoptotic cell death. Neuroreport 12(9): 1965-1970.
16. Yaffe K: Estrogens, selective estrogen receptor modulators, and dementia: What is the evidence? Ann NY Acad Sci (2001) 949:215-222.
17. Yaffe K, Krueger K, Cummings SR, Blackwell T, Henderson VW, Sarkar S, Ensrud K, Gardy D: Effect of reloxifene on prevention of dementia and cognitive impairment in older women: The Multiple Outcomes of Raloxifene Evaluation (MORE) randomised trial. Am J Psychiatr (2005) 162(4):683-690.
18. Brinton RD: Requirements of a brain selective estrogen: Advances and remaining challenges for developing a neuroSERM. J Alzheimers Dis (2004) 6(6 Suppl):S27-S35.
19. Spore MB: Arzoxifene: A promising new selective estrogen receptor modulator for chemoprevention of breast cancer. Olin Cancer Res (2004) 10(16):5313-5315.
20. Ariazi EA, Ariazi JL, Cordera F, Jordan VC: Estrogen receptors as therapeutic targets in breast cancer. Curr Top Med Chem (2006) 6(3):181-202.
21. McDonnell DP: The molecular determinants of estrogen receptor pharmacology. Maturitas (2004) 48(Suppl 1):S7-S12.
22. Harvey HA, Kimura M, Hajba A: Toremifene: An evaluation of its safety profile. Breast (2006) 15(2):142-157.
23. Buzdar A, Hayes D, El-Khoudary S, Yan S, Lanning P, Lichinitser M, Gopal R, Falkson G, Pritchard K, Lipton A, Walter K et al: Phase III randomised trial of droloxifene and tamoxifen as first-line endocrine treatment of ER/PgR-positive advanced breast cancer. Breast Cancer Res Treat (2002) 73(2): 161-175.
24. Dardes RC, O'Regan RM, Gajdos C, Robinson SP, Bentrem D, De Los Reyes A, Jordan VC: Effects of a new clinically relevant antiestrogen (GW5638) related to tamoxifen on breast and endometrial cancer growth in vivo. Clin Cancer Res (2002) 8(6):1995-2001.
25. Wu Y-L, Yang X, Ran Z, McDonnell DP, Norris JD, Willson TM, Greene GL: Structural basis for an unexpected mode of SERM-mediated ER antagonism. Mol Cell (2005) 18(4):413-424.
26. Bentrem DJ, Dardes RC, Liu H, MacGregor-Schafar J, Zapf JW, Jordan VC: Molecular mechanism of action at estrogen receptor α of a new clinically relevant antiestrogen (GW7604) related to tamoxifen. Endocrinology (2001) 142(2):838-846.
27. Connor CE, Norris JD, Broadwater G, Willson TM, Gottardis MM, Dewhirst MW, McDonnell DP: Circumventing tamoxifen resistance in breast cancers using antiestrogens that induce unique conformational changes in the estrogen receptor. Cancer Res (2001) 61(7):2917-2922.
28. Iannone MA, Simmons CA, Kadwell SH, Svoboda DL, Vanderwall DE, Dang S-J, Consler TG, Shearin J, Gray JG, Pearce KH: Correlation between in vitro peptide binding profiles and cellular activities for estrogen receptor-modulating compounds. Mol Endocrinol 18(5):1064-1081.
29. Girault I, Bièche I, Lidereau R: Role of estrogen receptor α transcriptional coregulators in tamoxifen resistance in breast cancer. Maturitas (2006) 54(4):342-351.
30. Howell A, Robertson JFR, Abram P. Lichinister MR, Elledge R, Bajetta E, Watanabe T, Morris C, Webster A, Dimery I, Osborne CK: Comparison of fulvestrant versus tamoxifen for the treatment of advanced breast cancer in postmenopausal women previously untreated with endocrine therapy: A multinational, double-blind, randomized trial. J Clin Oncol (2004) 22(9):1605-1613.
31. Howell A: Pure oestrogen antagonists for the treatment of advanced breast cancer. Endocr Rel Cancer (2006) 13(3):689-706.
32. Hoffmann J, Bohlmann R, Heinrich N, Hofmeister H, Kroll J, Kunzer H, Lichtner RB, Nishimo Y, Parczyk K, Sauer G, Gieschen H et al: Characterization of new estrogen receptor destabilizing compounds: Effects on estrogen-sensitive and tamoxifen-resistant breast cancer. J Natl Cancer Inst (2004) 96(3):210-218.
33. Fabian CJ, Kimler BF, Anderson J, Tawfik OW, Mayo MS, Burak WE Jr, O'Shaughnessy JA, Albain KS, Hyams DM, Budd GT, Gan PA et al: Breast cancer chemoprevention phase I evaluation of blomarker modulation by arzoxifene, a third generation selective estrogen receptor modulator. Clin Cancer Res (2004) 10(16):5403-5417.
34. Komm BS, Kharode YP, Bedine PVN, Harris HA, Miller CP, Lyttle CR: Bazedoxifene acetate: Selective estrogen receptor modulator with improved selectivity. Endocrinology (2005) 146(9):3999-4008.
35. Labrie F, Champagne P, Labrie C, Roy J, Laverdière J, Provencher L, Potvin M, Drolet Y, Pellak M, Panasci L, L'Esperance B et al: Activity and safety of the antiestrogen EM-800, the orally active precursor of acolfifene, in tamoxifen-resistant breast cancer. J Clin Oncol (2004) 22(5):864-871.
36. Gutman M, Couillard S, Roy J, Labrie F, Candas B, Labrie C: Comparison of the effects of EM-632 (SCH57068), tamoxifen, toremifene, droloxifene, GW-5638 and raloxifene on the growth of human ZR-75-1 breast tumors in nude mice. Int J Cancer (2002) 99(2):273-278.
37. Smith CL O'Malley BW: Coregulator function: A key to understanding tissue specificity of selective receptor modulators. Endocr Rev (2004) 25(1):45-71.
38. Veeneman GH: Non-steroidal subtype selective estrogens. Curr Med Chem (2005) 12(9):1077-1136.
39. Harrington WR, Sheng S, Barnett DH, Petz LN, Katzenellenbogen JA, Katzenellenbogen BS: Activities of estrogen receptor α- and β-selective ligands at diverse estrogen responsive gene sites mediating transactivation or transrepression. Mol Cell Endocrinol (2003) 206(1-2):13-22.
40. Murphy LC, Watson PH: Is oestrogen receptor-β a predictor of endocrine therapy responsiveness in human breast cancer? Endocr Relat Cancer (2006) 13(2):327-334.
41. Lindberg MK, Movérare S, Skrtic S, Gao H, Dahlman K, Gustafsson J-A, Ohisson C: Estrogen receptor (ER)-β reduces ERα-regulated gene transcription, supporting a 'ying yang' relationship between ERα and ERβ in mice. Mol Endocrinol (2003) 17(2):203-208.
42. Maruyama S, Fujimoto N, Asano K, Ito A: Suppression by estrogen receptor β of AP-1 mediated transactivation through estrogen receptor α. J Steroid Biochem Mol Biol (2001) 78(2):177-184.
43. Bardin A, Boulle N, Lazennec G, Vignon F, Pujol P: Loss of ERβ expression as a common step in estrogen-dependent tumor progression. Endocr Relat Cancer (2004) 11(3):537-551.
44. Nakopoulou L, Lazaris AC, Panayotopoulou EG, Giannopoulou I, Givalas N, Markaki S, Keramopoulos A: The favourable prognostic value of estrogen receptor β immunohistochemical expression in breast cancer. J Clin Pathol (2004) 57(5):523-528.
45. Shaaban JAM O'Neill PA, Davies MP, Sibson R, West CR, Smith PH, Foster CS: Declining estrogen receptor-β expression defines malignant progression of human breast neoplasia. Am J Surg Pathol (2003) 27(12):1502-1512.
46. Gustafsson JA: What pharmacologists can learn from recent advances in estrogen signalling. Trends Pharmacol Sci (2003) 24(9):479-485.
47. Hopp TA, Weiss HL, Parra IS, Cui Y, Osborne CK, Fuqua SAW: Low levels of estrogen receptor β protein predict resistance to tamoxifen therapy in breast cancer. Clin Cancer Res (2004) 10(22):7490-7499.
48. Esslimani-Sahia M, Simony-Lafontaine J, Kramar A, Lavaill R., Mollevi C, Warner M, Gustafsson, Rochefort H: Estrogen receptor β (ERβ) level but not its ERβcx variant helps to predict tamoxifen resistance in breast cancer. Clin Cancer Res (2004) 10(17):5769-5776.
49. Sun J, Baudry J, Katzenellenbogen JA, Katzenellenbogen BS: Molecular basis for the subtype discrimination of the estrogen receptor-β-selective ligand, diarylproprionitrile. Mol Endocrinol (2003) 17(2):247-258.
50. Harris HA, Albert LM, Leathurby Y, Malamas MS, Mewshaw RE, Miller CP, Kharode YP, Marzolf J, Komm BS, Winneker RC, Frail DE et al: Evaluation of an estrogen receptor-β agonist in animal models of human disease. Endocrinology (2003) 144(10):4241-4249.
51. McPherson SJ, Ellem SJ, Simpson ER, Patchev V, Fritzemeier K-H, Risbridger GP: Essential role for estrogen receptor β in stromal-epithelial regulation of prostatic hyperplasia. Endocrinology (2006):doi:10.1210/en.2006-0906.
52. Puddefoot JR, Barker S, Vinson GP: Triilostane in advanced breast cancer. Expert Opin Pharmacother (2006) 7(17):2413-2419.
53. Barker S, Malouitre SDM, Glover HR, Puddefoot JR, Vinson GP: Comparison of effects of 4-hydroxy-tamoxifen and trilostane on oestrogen-regulated gene expression in MCF-7 cells: Up-regulation of oestrogen receptor β. J Steroid Biochem Mol Biol (2006) 100(4-5):141-151.
54. Nicholson RI, Staka C, Boyns F, Hutcheson IR, Gee JMW: Growth factor-driven mechanisms associated with resistance to estrogen deprivation in breast cancer: New opportunities for therapy. Endocr Rel Cancer (2004) 11(4):623-641.
55. Glaros S, Atanaskova N, Zhao C, Skafar DF, Reddy KB: Activation function-1 domain of estrogen receptor regulates the agonist and antagonistic actions of tamoxifen. Mol Endocrinol (2006) 20(5):996-1008.
56. Normanno N, Di Maio M, De Maio E, De Luca A, de Matteis A, Giordano A, Perrone F: Mechanisms of endocrine resistance and novel therapeutic strategies in breast cancer. Endocr Relat Cancer (2005) 12(4):721-747.
57. Johnston SR, Dowsett M: Aromatase inhibitors for breast cancer: Lessons from the laboratory. Nat Rev Cancer (2003) 3(11):821-831.
58. Santen RJ, Song RX, Zhang Z, Yue W, Kumar R: Adaptive hypersensitivity to estrogen: Mechanism for sequential responses to hormonal therapy in breast cancer. Clin Cancer Res (2004) 10(1 Pt 2):337S-345S.
59. Geisler J, Haynes B, Anker G, Dowsett M, Lonning PE: Influence of letrozole and anastrozole on total body aromatization and plasma estrogen levels in postmenopausal breast cancer patients evaluated in a randomized, cross-over study. J Clin Oncol (2002) 20(3):751-757.
60. Gee JMW, Howell A, Gullick WJ, Benz CC, Sutherland RL, Santen RJ, Martin L-A, Ciardello F, Miller WR, Dowsett M, Barratt-Lee P et al: Consensus statement. Therapeutic resistance in breast cancer: impact of growth factor signalling pathways and implications for future treatment. Endocr Rel Cancer (2005) 12(Suppl):S1-S7.
61. Hiscox S, Morgan L, Barrow D, Dutkowskil C, Wakeling a, Nicholson RI: Tamoxifen resistance in breast cancer cells is accompanied by an enhanced motile and invasive phenotype: inhibition by gefitinib ('Iressa', ZD1839). Clin Exp Metastasis (2004) 21(3):201-212.
62. Lipton A, Leitzel K, Suhail A: Predicting response to herceptin therapy. Clin Cancer Res (2004) 10(5):1559-1560.
63. Chu I, Blackwell K, Chen S, Slingerland J: The dual ErbB1/ErbB2 inhibitor, lapatinib (GW672016), cooperates with tamoxifen to inhibit both cell proliferation- and estrogen-dependent gene expression in antiestrogen-resistant breast cancer. Cancer Res (2005) 65(1):18-25.
64. Breman DJ, O'Brien SL, Fagan A, Culhane AC, Higgins DG, Duffy MJ, Gallagher WM: Application of DNA microarray technology in determining breast cancer prognosis and therapeutic response. Expert Opin Biol Ther (2005) 5(8):1069-1083.
65. Sodie T, Wang Y, Xiao C, Johnsen H, Naume B, Samaha RR, Borresen-Dale AL: Distinct molecular mechanisms underlying clinically relevant subtypes of breast cancer: Gene expression analyses across three different platforms. BMC Genomics (2006) 7:127.
66. Kirkegaard T, Witton CJ, McGlynn LM, Tovey SM, Dunne B, Lyon A, Bartlett JM: Akt activation predicts outcome in breast cancer patients treated with tamoxifen. J Pathol(2005) 207(2):139-146.
67. Tovey S, Dunne B, Witton CJ, Forsyth A, Cooke TG, Bartlett JM: Can molecular markers predict when to implement treatment with aromatase inhibitors. Clin Cancer Res (2005) 11(13):4835-4842.
68. Lipton A, Leitzel K, Ali SM, Demers L, Harvey HA, Chaudri-Ross HA, Evans D, Hackl W, Hamer P, Carney W: Serum HER-2/neu conversion to positive at the time of disease progression in patients with breast carcinoma. Cancer (2005) 104(2):257-263.