75
Views
21
CrossRef citations to date
0
Altmetric
Drug Evaluation

Arzoxifene: the development and clinical outcome of an ideal SERM

Pages 317-326 | Published online: 27 Feb 2006

Bibliography

  • JEMAL A, MURRAY T, WARD E et al.: Cancer statistics, 2005. CA Cancer J. Clin. (2005) 55(1):10-30.
  • WU AH, PIKE MC, STRAM DO: Meta-analysis: dietary fat intake, serum estrogen levels, and the risk of breast cancer. J. Natl. Cancer Inst. (1999) 91(6):529-534.
  • UNITED KINGDOM NATIONALCASE-CONTROL STUDY GROUP: Breast feeding and risk of breast cancer in young women. Br. Med. J. (1993) 307(6895):17-20.
  • KALACHE A, MAGUIRE A, THOMPSON SG: Age at last full-term pregnancy and risk of breast cancer. Lancet (1993) 341(8836):33-36.
  • VATTEN LJ, KVINNSLAND S: Pregnancy-related factors and risk of breast cancer in a prospective study of 29,981 Norwegian women. Eur. J. Cancer (1992) 28A(6-7):1148-1153.
  • CHLEBOWSKI RT, HENDRIX SL, LANGER RD et al.: Influence of estrogen plus progestin on breast cancer and mammography in healthy postmenopausal women: the Women’s Health Initiative Randomized Trial. J. Am. Med. Assoc. (2003) 289(24):3243-3253.
  • EARLY BREAST CANCER TRIALISTS’COLLABORATIVE GROUP: Ovarian ablation in early breast cancer: overview of the randomised trials. Lancet (1996) 348(9036):1189-1196.
  • EARLY BREAST CANCER TRIALISTS’COLLABORATIVE GROUP: Tamoxifen for early breast cancer: an overview of the randomised trials. Lancet (1998) 351(9114):1451-1467.
  • EARLY BREAST CANCER TRIALISTS’COLLABORATIVE GROUP: Effects of chemotherapy and hormonal therapy for early breast cancer on recurrence and 15-year survival: an overview of the randomised trials. Lancet (2005) 365(9472):1687-1717.
  • DODGE JA, LUGAR CW, CHO S et al.: Evaluation of the major metabolites of raloxifene as modulators of tissue selectivity. J. Steroid Biochem. Mol. Biol. (1997) 61(1-2):97-106.
  • FUCHS-YOUNG R, GLASEBROOK AL, SHORT LL et al.: Raloxifene is a tissue-selective agonist/antagonist that functions through the estrogen receptor. Ann. NY Acad. Sci. (1995) 761:355-360.
  • GRESE TA, SLUKA JP, BRYANT HU et al.: Molecular determinants of tissue selectivity in estrogen receptor modulators. Proc. Natl. Acad. Sci. USA (1997) 94(25):14105-14110.
  • SHANG Y, BROWN M: Molecular determinants for the tissue specificity of SERMs. Science (2002) 295(5564):2465-2468.
  • PALKOWITZ AD, GLASEBROOK AL, THRASHER KJ et al.: Discovery and synthesis of [6-hydroxy-3-[4-[2-(1-piperidinyl)ethoxy] phenoxy]-2-(4-hydroxyphenyl)]b enzo[b]thiophene: a novel, highly potent, selective estrogen receptor modulator. J. Med. Chem. (1997) 40(10):1407-1416.
  • SATO M, ZENG GQ, ROWLEY E, TURNER CH: LY353381.HCl: an improved benzothiophene analog with bone efficacy complementary to parathyroid hormone-(1-34). Endocrinology (1998) 139(11):4642-4651.
  • SATO M, TURNER CH, WANG T, ADRIAN MD, ROWLEY E, BRYANT HU: LY353381.HCl: a novel raloxifene analog with improved SERM potency and efficacy in vivo. J. Pharmacol. Exp. Ther. (1998) 287(1):1-7.
  • SCHAFER JM, LEE ES, DARDES RC et al.: Analysis of cross-resistance of the selective estrogen receptor modulators arzoxifene (LY353381) and LY117018 in tamoxifen-stimulated breast cancer xenografts. Clin. Cancer Res. (2001) 7(8):2505-2512.
  • FREDDIE CT, LARSEN SS, BARTHOLOMAEUSSEN M, LYKKESFELDT AE: The effect of the new SERM arzoxifene on growth and gene expression in MCF-7 breast cancer cells. Mol. Cell. Endocrinol. (2004) 219(1-2):27-36.
  • DARDES RC, BENTREM D, O’REGAN RM, SCHAFER JM, JORDAN VC: Effects of the new selective estrogen receptor modulator LY353381.HCl (arzoxifene) on human endometrial cancer growth in athymic mice. Clin. Cancer Res. (2001) 7(12):4149-4155.
  • DETRE S, RIDDLER S, SALTER J, A’HERN R, DOWSETT M, JOHNSTON SR: Comparison of the selective estrogen receptor modulator arzoxifene (LY353381) with tamoxifen on tumor growth and biomarker expression in an MCF-7 human breast cancer xenograft model. Cancer Res. (2003) 63(19):6516-6522.
  • LICUN W, TANNOCK IF: Selective estrogen receptor modulators as inhibitors of repopulation of human breast cancer cell lines after chemotherapy. Clin. Cancer Res. (2003) 9(12):4614-4618.
  • MUNSTER PN, BUZDAR A, DHINGRA K et al.: Phase I study of a third-generation selective estrogen receptor modulator, LY353381.HCl, in metastatic breast cancer. J. Clin. Oncol. (2001) 19(7):2002-2009.
  • 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(9):1383-1390.
  • BUZDAR A, O’SHAUGHNESSY 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(6):1007-1014.
  • McMEEKIN DS, GORDON A, FOWLER J et al.: A Phase II trial of arzoxifene, a selective estrogen response modulator, in patients with recurrent or advanced endometrial cancer. Gynecol. Oncol. (2003) 90(1):64-69.
  • JEMAL A, TIWARI RC, MURRAY T et al.: Cancer statistics, 2004. CA Cancer J. Clin. (2004) 54(1):8-29.
  • GORLA SR, HOU N, ACHARYA S et al.: A predictive model for the development of hormone-responsive breast cancer. Ann. Surg. Oncol. (2005) 12(1):48-56.
  • MANSON JE, HSIA J, JOHNSON KC et al.: Estrogen plus progestin and the risk of coronary heart disease. N. Engl. J. Med. (2003) 349(6):523-534.
  • ANDERSON GL, LIMACHER M, ASSAF AR et al.: Effects of conjugated equine estrogen in postmenopausal women with hysterectomy: the Women’s Health Initiative Randomized Controlled Trial. J. Am. Med. Assoc. (2004) 291(14):1701-1712.
  • STEPHENSON J: FDA orders estrogen safety warnings: agency offers guidance for HRT use. J. Am. Med. Assoc. (2003) 289(5):537-538.
  • LEVENSON AS, SVOBODA KM, PEASE KM et al.: Gene expression profiles with activation of the estrogen receptor alpha-selective estrogen receptor modulator complex in breast cancer cells expressing wild-type estrogen receptor. Cancer Res. (2002) 62(15):4419-4426.
  • LONARD DM, SMITH CL: Molecular perspectives on selective estrogen receptor modulators (SERMs): progress in understanding their tissue-specific agonist and antagonist actions. Steroids (2002) 67(1):15-24.
  • KODAMA M, KODAMA T: The nature of tamoxifen action in the control of female breast cancer. In Vivo (2001) 15(4):319-325.
  • KUIPER GG, CARLSSON B, GRANDIEN K et al.: Comparison of the ligand binding specificity and transcript tissue distribution of estrogen receptors alpha and beta. Endocrinology (1997) 138(3):863-870.
  • JORDAN VC, ROBINSON SP: Species-specific pharmacology of antiestrogens: role of metabolism. Fed. Proc. (1987) 46(5):1870-1874.
  • BONNETERRE J, BUZDAR A, NABHOLTZ JM et al.: Anastrozole is superior to tamoxifen as first-line therapy in hormone receptor positive advanced breast carcinoma. Cancer (2001) 92(9):2247-2258.
  • MOURIDSEN H, GERSHANOVICH M, SUN Y et al.: Superior efficacy of letrozole versus tamoxifen as first-line therapy for postmenopausal women with advanced breast cancer: results of a Phase III study of the International Letrozole Breast Cancer Group. J. Clin. Oncol. (2001) 19(10):2596-2606.
  • COOMBES RC, HALL E, GIBSON LJ et al.: A randomized trial of exemestane after two to three years of tamoxifen therapy in postmenopausal women with primary breast cancer. N. Engl. J. Med. (2004) 350(11):1081-1092.
  • GOSS PE, INGLE JN, MARTINO S et al.: Randomized trial of letrozole following tamoxifen as extended adjuvant therapy in receptor-positive breast cancer: updated findings from NCIC CTG MA.17. J. Natl. Cancer Inst. (2005) 97(17):1262-1271.
  • BAUM M, BUDZAR AU, CUZICK J et al.: Anastrozole alone or in combination with tamoxifen versus tamoxifen alone for adjuvant treatment of postmenopausal women with early breast cancer: first results of the ATAC randomised trial. Lancet (2002) 359(9324):2131-2139.
  • 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(18):1371-1388.
  • POWLES T, EELES R, ASHLEY S et al.: Interim analysis of the incidence of breast cancer in the Royal Marsden Hospital tamoxifen randomised chemoprevention trial. Lancet (1998) 352(9122):98-101.
  • FISHER B: Commentary on endometrial cancer deaths in tamoxifen-treated breast cancer patients. J. Clin. Oncol. (1996) 14(3):1027-1039.
  • FISHER B, COSTANTINO JP, REDMOND CK, FISHER ER, WICKERHAM DL, CRONIN WM: Endometrial cancer in tamoxifen-treated breast cancer patients: findings from the National Surgical Adjuvant Breast and Bowel Project (NSABP) B-14. J. Natl. Cancer Inst. (1994) 86(7):527-537.
  • FALLOWFIELD LJ, LEAITY SK, HOWELL A, BENSON S, CELLA D: Assessment of quality of life in women undergoing hormonal therapy for breast cancer: validation of an endocrine symptom subscale for the FACT-B. Breast Cancer Res. Treat. (1999) 55(2):189-199.
  • GOTTARDIS MM, JIANG SY, JENG MH, JORDAN VC: Inhibition of tamoxifen-stimulated growth of an MCF-7 tumor variant in athymic mice by novel steroidal antiestrogens. Cancer Res. (1989) 49(15):4090-4093.
  • GOTTARDIS MM, JORDAN VC: Development of tamoxifen-stimulated growth of MCF-7 tumors in athymic mice after long-term antiestrogen administration. Cancer Res. (1988) 48(18):5183-5187.
  • OSIPO C, GAJDOS C, CHENG D, JORDAN VC: Reversal of tamoxifen resistant breast cancer by low dose estrogen therapy. J. Steroid Biochem. Mol. Biol. (2005) 93(2-5):249-256.
  • FISHER B, DIGNAM J, BRYANT J et al.: Five versus more than five years of tamoxifen therapy for breast cancer patients with negative lymph nodes and estrogen receptor-positive tumors. J. Natl. Cancer Inst. (1996) 88(21):1529-1542.
  • BLACK LJ, GOODE RL: Evidence for biological action of the antiestrogens LY117018 and tamoxifen by different mechanisms. Endocrinology (1981) 109(3):987-989.
  • BLACK LJ, GOODE RL: Uterine bioassay of tamoxifen, trioxifene and a new estrogen antagonist (LY117018) in rats and mice. Life Sci. (1980) 26(17):1453-1458.
  • SCHOLL SM, HUFF KK, LIPPMAN ME: Antiestrogenic effects of LY 117018 in MCF-7 cells. Endocrinology (1983) 113(2):611-617.
  • WESTLEY BR, HOLZEL F, MAY FE: Effects of oestrogen and the antioestrogens, tamoxifen and LY117018, on four oestrogen-regulated RNAs in the EFM-19 breast cancer cell line. J. Steroid Biochem. (1989) 32(3):365-372.
  • BUZDAR AU, MARCUS C, HOLMES F, HUG V, HORTOBAGYI G: Phase II evaluation of Ly156758 in metastatic breast cancer. Oncology (1988) 45(5):344-345.
  • GRADISHAR W, GLUSMAN J, LU Y, VOGEL C, COHEN FJ, SLEDGE GW Jr: Effects of high dose raloxifene in selected patients with advanced breast carcinoma. Cancer (2000) 88(9):2047-2053.
  • 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) 10(9):961-966.
  • 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. J. Am. Med. Assoc. (1999) 282(7):637-645.
  • 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(23):2189-2197.
  • SNYDER KR, SPARANO N, MALINOWSKI JM: Raloxifene hydrochloride. Am. J. Health Syst. Pharm. (2000) 57(18):1669-1675 (Quiz 1676-1668).
  • BRYANT HU, GLASEBROOK AL, YANG NN, SATO M: An estrogen receptor basis for raloxifene action in bone. J. Steroid Biochem. Mol. Biol. (1999) 69(1-6):37-44.
  • GRESE TA, CHO S, FINLEY DR et al.: Structure-activity relationships of selective estrogen receptor modulators: modifications to the 2-arylbenzothiophene core of raloxifene. J. Med. Chem. (1997) 40(2):146-167.
  • GRESE TA, PENNINGTON LD, SLUKA JP et al.: Synthesis and pharmacology of conformationally restricted raloxifene analogues: highly potent selective estrogen receptor modulators. J. Med. Chem. (1998) 41(8):1272-1283.
  • LIU H, LIU J, VAN BREEMEN RB, THATCHER GR, BOLTON JL: Bioactivation of the selective estrogen receptor modulator desmethylated arzoxifene to quinoids: 4′-fluoro substitution prevents quinoid formation. Chem. Res. Toxicol. (2005) 18(2):162-173.
  • FREDDIE CT, CHRISTENSEN GL, LYKKESFELDT AE: A new MCF-7 breast cancer cell line resistant to the arzoxifene metabolite desmethylarzoxifene. Mol. Cell. Endocrinol. (2004) 220(1-2):97-107.
  • YAO K, LEE ES, BENTREM DJ et al.: Antitumor action of physiological estradiol on tamoxifen-stimulated breast tumors grown in athymic mice. Clin. Cancer Res. (2000) 6(5):2028-2036.
  • SCHAFER JM, LEE ES, O’REGAN RM, YAO K, JORDAN VC: Rapid development of tamoxifen-stimulated mutant p53 breast tumors (T47D) in athymic mice. Clin. Cancer Res. (2000) 6(11):4373-4380.
  • MADSEN MW, REITER BE, LYKKESFELDT AE: Differential expression of estrogen receptor mRNA splice variants in the tamoxifen resistant human breast cancer cell line, MCF-7/TAMR-1 compared to the parental MCF-7 cell line. Mol. Cell. Endocrinol. (1995) 109(2):197-207.
  • LYKKESFELDT AE, MADSEN MW, BRIAND P: Altered expression of estrogen-regulated genes in a tamoxifen-resistant and ICI 164,384 and ICI 182,780 sensitive human breast cancer cell line, MCF-7/TAMR-1. Cancer Res. (1994) 54(6):1587-1595.
  • 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(23):8412-8415.
  • 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(12):2256-2264.
  • 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(16):5403-5417.
  • HOWELL A, ROBERTSON JF, ABRAM P et al.: 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.
  • BONNETERRE J, THURLIMANN B, ROBERTSON JF et al.: Anastrozole versus tamoxifen as first-line therapy for advanced breast cancer in 668 postmenopausal women: results of the Tamoxifen or Arimidex Randomized Group Efficacy and Tolerability study. J. Clin. Oncol. (2000) 18(22):3748-3757.
  • NABHOLTZ JM, BUZDAR A, POLLAK M et al.: Anastrozole is superior to tamoxifen as first-line therapy for advanced breast cancer in postmenopausal women: results of a North American multicenter randomized trial. Arimidex Study Group. J. Clin. Oncol. (2000) 18(22):3758-3767.
  • PARIDAENS R, DIRIX L, LOHRISCH C et al.: Mature results of a randomized Phase II multicenter study of exemestane versus tamoxifen as first-line hormone therapy for postmenopausal women with metastatic breast cancer. Ann. Oncol. (2003) 14(9):1391-1398.
  • PARIDAENS R, THERASSE P, DIRIX L et al.: First line hormonal treatment (HT) for metastatic breast cancer (MBC) with exemestane (E) or tamoxifen (T) in postmenopausal patients (pts) – a randomized Phase III trial of the EORTC Breast Group. J. Clin. Oncol., 2004 ASCO Annual Meeting Proceedings (2004) 22(14S):A515.
  • THURLIMANN B, ROBERTSON JF, NABHOLTZ JM, BUZDAR A, BONNETERRE J: Efficacy of tamoxifen following anastrozole (‘Arimidex’) compared with anastrozole following tamoxifen as first-line treatment for advanced breast cancer in postmenopausal women. Eur. J. Cancer (2003) 39(16):2310-2317.
  • NABHOLTZ JM, BONNETERRE J, BUZDAR A, ROBERTSON JF, THURLIMANN B: Anastrozole (Arimidex) versus tamoxifen as first-line therapy for advanced breast cancer in postmenopausal women: survival analysis and updated safety results. Eur. J. Cancer (2003) 39(12):1684-1689.

Wesbites

  • http://www.clinicaltrials.gov/ct/show/NCT00003906 Website for the STAR study.
  • http://www.clinicaltrials.gov/ct/show/NCT00034125 Phase III study of LY-353381 versus tamoxifen in women with locally advanced or metastatic breast cancer.
  • http://www.clinicaltrials.gov/ct/show/NCT00088010?order=1 Effects of arzoxifene on bone fractures and incidence of breast cancer.
  • http://www.clinicaltrials.gov/ct/show/NCT00085956?order=1 Effects of arzoxifene on bone mass and the uterus.

Reprints and Corporate Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

To request a reprint or corporate permissions for this article, please click on the relevant link below:

Academic Permissions

Please note: Selecting permissions does not provide access to the full text of the article, please see our help page How do I view content?

Obtain permissions instantly via Rightslink by clicking on the button below:

If you are unable to obtain permissions via Rightslink, please complete and submit this Permissions form. For more information, please visit our Permissions help page.