Effects of CH4893237, a new orally active estrogen receptor downregulator, on breast cancer xenograft models with low serum estrogen levels

Oncology Reports

Volumn 21, Issue 3, 2009, Pages 747-755

  Yoneya, Takaaki ^a   Tsunenari, Toshiaki ^a   Taniguchi, Kenji ^a   Kanbe, Yoshitake ^a   Morikawa, Kazumi ^a   Yamada Okabe, Hisafumi ^a   Lee, Yeon Ho ^b   Lee, Mee Hyun ^b   Kwon, Lae Sung ^b  

^a CHUGAI PHARMACEUTICAL CO LTD   (Japan)

^b C and C Research Laboratories   (South Korea)

Author keywords

Aromatase inhibitor; Breast cancer; Orally active; Postmenopausal; Selective estrogen receptor downregulator; Tamoxifen

Indexed keywords

4 HYDROXYTAMOXIFEN; ANTIESTROGEN; CH 4893237; ESTROGEN; ESTROGEN RECEPTOR ALPHA; ESTROGEN RECEPTOR BETA; FULVESTRANT; TAMOXIFEN; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANTINEOPLASTIC ACTIVITY; ARTICLE; BREAST CANCER; CANCER CELL CULTURE; CANCER GROWTH; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; DRUG EFFICACY; DRUG POTENCY; DRUG RESPONSE; DRUG STRUCTURE; ESTROGEN BLOOD LEVEL; FEMALE; GROWTH INHIBITION; HUMAN; HUMAN CELL; HUMAN TISSUE; MOLECULAR MECHANICS; MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN DEGRADATION; STRUCTURE ACTIVITY RELATION; TUMOR VOLUME; TUMOR XENOGRAFT;

ANIMALS; ANTINEOPLASTIC AGENTS; BREAST NEOPLASMS; ESTRADIOL; ESTROGENS; FEMALE; HUMANS; MICE; MICE, NUDE; RECEPTORS, ESTROGEN; SELECTIVE ESTROGEN RECEPTOR MODULATORS; XENOGRAFT MODEL ANTITUMOR ASSAYS;

EID: 64849089624     PISSN: 1021335X     EISSN: 17912431     Source Type: Journal    
DOI: 10.3892/or_00000280     Document Type: Article

References (21)

1. Anderson WF, Chatterjee N, Ershler WB and Brawley OW: Estrogen receptor breast cancer phenotypes in the surveillance, epidemiology, and end results database. Breast Cancer Res Treat 76: 27-36, 2002.
2. Adamo V, Iorfida M, Montalto E, et al: Overview and new strategies in metastatic breast cancer (MBC) for treatment of tamoxifen-resistant patients. Ann Oncol 18 (Suppl 6): vi53-vi57, 2007.
3. Howell A: Pure oestrogen antagonists for the treatment of advanced breast cancer. Endocr Relat Cancer 13: 689-706, 2006.
4. Osborne CK, Pippen J, Jones SE, et al: Double-blind, randomized trial comparing the efficacy and tolerability of fulvestrant versus anastrozole in postmenopausal women with advanced breast cancer progressing on prior endocrine therapy: results of a North American trial. J Clin Oncol 20: 3386-3395, 2002.
5. Howell A, Robertson JFR, Quaresma Albano J, et al: Fulvestrant, formerly ICI 182,780, is as effective as anastrozole in postmenopausal women with advanced breast cancer progressing after prior endocrine treatment. J Clin Oncol 20: 3396-3403, 2002.
6. Howell A, Robertson JFR, 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 22: 1605-1613, 2004.
7. Robertson JFR: Fulvestrant (Faslodex)-How to make a good drug better. Oncologist 12: 774-784, 2007.
8. Vergote I, Amant F, Leunen K, Van Gorp T, Berteloot P and Neven P: Metastatic breast cancer: sequencing hormonal therapy and positioning of fulvestrant. Int J Gynecol Cancer 16 (Suppl 2): 524-526, 2006.
9. Hoffmann J, Bohlmann R, Heinrich N, et al: Characterization of new estrogen receptor destabilizing compounds: effects on estrogen-sensitive and tamoxifen-resistant breast cancer. J Natl Cancer Inst 96: 210-218, 2004.
10. Dardes RC, O'Regan RM, Gajdos C, et al: Effects of a new clinically relevant antiestrogen (GW5638) related to tamoxifen on breast and endometrial cancer growth in vivo. Clin Cancer Res 8: 1995-2001, 2002.
11. Wittmann BM, Sherk A and McDonnell DP: Definition of functionally important mechanistic differences among selective estrogen receptor down-regulators. Cancer Res 67: 9549-9560, 2007.
12. Yoneya T, Taniguchi K, Tsunenari T, et al: Identification of a novel, orally bioavailable estrogen receptor downregulator. Anticancer Drugs 16: 751-756, 2005.
13. Shim WS, Conaway M, Masamura S, et al: Estradiol hypersensitivity and mitogen-activated protein kinase expression in long-term estrogen deprived human breast cancer cells in vivo. Endocrinology 141: 396-405, 2000.
14. Berstein LM, Wang JP, Zheng H, Yue W, Conaway M and Santen RJ: Long-term exposure to tamoxifen induces hypersensitivity to estradiol. Clin Cancer Res 10: 1530-1534, 2004.
15. Odell WD: The menopause. In: Endocrinology. DeGroot LJ (ed). 2nd edition, WB Saunders Corp., Philadelphia, pp2009-2018, 1989.
16. Kraichely DM, Sun J, Katzenellenbogen JA and Katzenellenbogen BS: Conformational changes and coactivator recruitment by novel ligands for estrogen receptor-α and estrogen receptor-β: correlations with biological character and distinct differences among SRC coactivator family members. Endocrinology 141: 3534-3545, 2000.
17. Baumann CK and Castiglione-Gertsch M: Estrogen receptor modulators and down regulators. Optimal use in postmenopausal women with breast cancer. Drugs 67: 2335-2353, 2007.
18. Howell A, DeFriend DJ, Robertson JFR, et al: Pharmacokinetics, pharmacological and anti-tumor effects of the specific anti-oestrogen ICI 182780 in women with advanced breast cancer. Br J Cancer 74: 300-308, 1996.
19. Robertson JF, Nicholson RI, Bundred NJ, et al: Comparison of short-term biological effects of 7α-[9-(4,4,5,5,5-pentafluoropentylsulfinyl) -nonyl]estra-1,3,5, (10)-triene-3,17b-diol (faslodex) versus tamoxifen in postmenopausal women with primary breast cancer. Cancer Res 61: 6739-6749, 2001.
20. Kenny FS, Willsher PC, Gee JMW, et al: Change in expression of ER, bcl-2 and MIB1 on primary tamoxifen and relation to response in ER positive breast cancer. Breast Cancer Res Treat 65: 135-144, 2001.
21. Kanbe Y, Kim M-H, Nishimoto M, et al: Newly discovered orally active pure antiestrogens. Bioorg Med Chem Lett 16: 4959-4964, 2006.