The future of antihormone therapy: Innovations based on an established principle

Journal of Cancer Research and Clinical Oncology

Volumn 122, Issue 7, 1996, Pages 383-396

  Parczyk, Karsten ^a   Schneider, Martin R ^a  

^a BAYER PHARMA AG   (Germany)

Author keywords

Antihormones; Differentiation Apoptosis; Ligand independent activation; Receptor gene amplification and mutation; Total receptor blockade

Indexed keywords

ANAPRISTONE; ANDROGEN RECEPTOR; ANTIANDROGEN; ANTIESTROGEN; CYPROTERONE ACETATE; DIETHYLSTILBESTROL; DOPA; EPIDERMAL GROWTH FACTOR; ESTRADIOL; ESTROGEN RECEPTOR; FIBROBLAST GROWTH FACTOR; FLUTAMIDE; FULVESTRANT; GONADORELIN DERIVATIVE; HYDROXYTAMOXIFEN; KERATINOCYTE GROWTH FACTOR; MEDROXYPROGESTERONE ACETATE; MEGESTROL ACETATE; METRIBOLONE; MIFEPRISTONE; NIFEPRISTONE; ONAPRISTONE; PROGESTERONE; SOMATOMEDIN B; SOMATOMEDIN C; TAMOXIFEN; UNCLASSIFIED DRUG; ZK 119010; ZM 164384;

APOPTOSIS; BREAST CANCER; CELL DIFFERENTIATION; FEMALE; HORMONAL THERAPY; HUMAN; MALE; PRIORITY JOURNAL; PROSTATE CANCER; REVIEW;

ANDROGEN ANTAGONISTS; ANIMALS; ANTINEOPLASTIC AGENTS, HORMONAL; ESTROGEN ANTAGONISTS; FEMALE; FORECASTING; HUMANS; MALE; NEOPLASMS; NEOPLASMS, HORMONE-DEPENDENT; ORCHIECTOMY; RECEPTORS, STEROID;

EID: 0029901148     PISSN: 01715216     EISSN: None     Source Type: Journal    
DOI: 10.1007/BF01212877     Document Type: Review

References (82)

1. Angerer E von, Biberger C, Leichtl S (1995) Studies on heterocycle based pure antagonists. Ann NY Acad Sci 761:176-191
2. Boring CC, Squires TS, Tong T (1993) Cancer statistics. CA 43:7-26
3. Brinkmann AO, Trapman J (1995) Mutant androgen receptors in endocrine-related cancer. Endocr Relat Cancer 2:203-214
4. Brooks JR, Berman C, Nguyen H, Prahalada S, Primka RL, Rasmusson GH, Slater EE (1991) Effect of castration, DES, flutamide, and the 5α-reductase inhibitor, MK-906, on the growth of the Dunning rat prostatic carcinoma, R-3327. Prostate 18:215-227
5. Colombel M, Symmans F, Gil S, O'Toole KM, Chopin D, Benson M, Olsson CA, Korsmeyer S, Buttyan R (1993) Detection of the apoptosis-suppressing oncoprotein bcl-2 in hormone-refractory human prostate cancers. Am J Pathol 143:390-400
6. Crawford E, Eisenberger MA, McLeod, DG, Spaulding JT, Benson R, Dorr FA, Blumenstein BA, Davis MA, Goodman PJ (1989) A controlled trial of leuprolide with and without flutamide in prostatic carcinoma. N Engl J Med 321:419-424
7. Culig Z, Hobisch A, Cronauer MV, Radmayr C, Trapman J, Hittmair A, Bartsch G, Klocker H (1994) Androgen receptor activation in prostatic tumor cell lines by insulin-like growth factor-I, keratinocyte growth factor, and epidermal growth factor. Cancer Res 54:5474-5478
8. Dæhlin L, Bergh A, Damber JE (1987) Direct effects of oestradiol on growth and morphology of the Dunning R3327H prostatic carcinoma. Urol Res 15:169-172
9. Dauvois S, Danielian PS, White R, Parker MG (1992) Antiestrogen ICI 164,384 reduces cellular estrogen receptor content by increasing its turnover. Proc Natl Acad Sci USA 89:4037-4041
10. Dauvois S, White R, Parker MG (1993) The antiestrogen ICI 182780 discrupts estrogen receptor nucleocytoplasmic shuttling. J Cell Sci 106:1377-1388
11. DeFriend DJ, Howell A (1994) Tamoxifen withdrawal responses - chance observations or clinical clues to antioestrogen resistance? Breast 3:199-201
12. Delabre K, Guiochon-Mantel A, Milgrom E (1993) In vivo evidence against the existence of antiprogestins disrupting receptor binding to DNA. Proc Natl Acad Sci USA 90:4421-4425
13. Dukes M, Chester R, Yarwood L, Wakeling AE (1994) Effects of a non-steroidal pure antioestrogen, ZM 189,154, on oestrogen target organs of the rat including bones. J Endocrinol 141:335-341
14. Dupont A, Gomez JL, Cusan L, Koutsilieris M, Labrie F (1993) Response to flutamide withdrawal in advanced prostate cancer in progression under combination therapy. J Urol 150:908
15. Eaton CL, Griffiths K (1990) The role of endocrine therapy in prostatic cancer. In: Shalet SM (ed) Clinical endocrinology and metabolism, vol 4. Baillière Tindall, London, pp 85-96
16. El Etreby MF, Habenicht UF, Louton T, Nishino Y, Schröder G (1987) Effect of cyproterone acetate in comparison to flutamide and megestrol acetate on the ventral prostate, seminal vesicle, and adrenal glands of adult male rats. Prostate 11:361-375
17. Forbes A, Wilkinson ML, Iqbal MJ, Johnson PJ, Williams R (1987) Response to cyproterone acetate treatment in primary hepatocellular carcinoma is related to fall in free 5α-dihydrotestosterone. Eur J Cancer Clin Oncol 23:1659-1664
18. Geller J (1993) Basis for hormonal management of advanced prostate cancer. Cancer 71:1039-1045
19. Gottardis MM, Jiang SY, Jeng MH, Jordan VC (1989) Inhibition of tamoxifen-stimulated growth of an MCF-7 tumor variant in athymic by novel steroidal antiestrogens. Cancer Res 49:4090-4093
20. Gronemeyer H, Benhamou B, Berry MT, Gofflo D, Garcia T, Lerone T, Metzger D, Meyer ME, Tora L, Vergezac A, Chambon D (1992) Mechanism of antihormone action. J Steroid Biochem Mol Biol 41:217-221
21. Haak HR, Keizer RJW de, Hagennouw-Taal JCW, Seters AP van, Vielvoye GJ, Dulken H van (1990) Successful mifepristone treatment of recurrent, inoperable meningioma. Lancet 336:124-125
22. Horn DW, Vollmer G, Deerberg F, Schneider MR (1993) The EnDA endometrial adenocarcinoma: an oestrogen-sensitive, metastasizing, in vivo tumor model of the rat. J Cancer Res Clin Oncol 119:450-456
23. Horn DW, Vollmer G, Angerer E von, Schneider MR (1994) Effect of the nonsteroidal antiestrogen ZK 119.010 on growth and metastasis of the EnDA endometrial carcinoma. Int J Cancer 58:426-429
24. Horvath G, Stendahl U, Kalling M, Fernüo M, Himmelmann A, Hajba A (1990) Antiestrogenic treatment of advanced and recurrent carcinoma corpus uteri - a phase-II study of toremifene. Anticancer Res 10:323-326
25. Horwitz KB (1992) The molecular biology of RU 486. Is there a role for antiprogestins in the treatment of breast cancer? Endocr Rev 13:1-17
26. Howell A, Dodwell DJ, Anderson H (1990) New endocrine approaches to breast cancer. In: Shalet SM (ed) Clinical endocrinology and metabolism, vol 4. Baillière Tindall, London, pp 67-84
27. Howell A, DeFriend D, Robertson J, Blarney R, Walton P (1995) Response to a specific antioestrogen (ICI 182780) in tamoxifen-resistant breast cancer. Lancet 345:29-30
28. Huisman TWA, Tanghe HLJ, Koper JW, Reubi JC, Foekens JA, Avezaat CJJ, Braakman R, Lamberts SWJ (1991) Progesterone, oestradiol, somatostatin and epidermal growth factor receptors on human meningiomas and their CT characteristics. Eur J Cancer 27:1453-1457
29. Ignar-Trowbridge DM, Nelson KG, Bidwell MC, Curtis SW, Washburn TF, McLachlan JA, Korach KS (1992) Coupling of dual signaling pathways: epidermal growth factor action involves the estrogen receptor. Proc Natl Acad Sci USA 89:4658-4662
30. Iveson TJ, Smith IE, Ahern J, Smithers DA, Trunet PF, Dowsett M (1993) Phase I study of the oral nonsteroidal aromatase inhibitor CGS 20267 in postmenopausal patients with advanced breast cancer. Cancer Res 63:266-270
31. Jordan VC (1993) A current view of tamoxifen for the treatment and prevention of breast cancer. Br J Pharmacol 110:507-517
32. Kiang DT, Kollander RE, Thomas T, Kennedy BJ (1989) Up-regulation of estrogen receptors by nonsteroidal antiestrogens in human breast cancer. Cancer Res 49:5312-5316
33. Labrie F, Belanger A, Dupont A, Luu-The V, Simard J, Labrie C (1993) Science behind total androgen blockade: from gene to combination therapy. Clin Invest Med 16:475-492
34. Li M, Spitzer E, Zschiesche W, Binas B, Parczyk K, Grosse R (1995). Antiprogestins inhibit growth and stimulate differentiation in the normal mammary gland. J Cell Physiol 164:1-8
35. Maasberg M, Rotsch M, Jaques G, Enderle-Schmidt U, Weehle R, Havemann K (1989) Androgen receptors, androgen-dependent proliferation, and 5α-reductase activity of small-cell lung cancer cell lines. Int J Cancer 43:685-691
36. Madjno R, Parczyk K, Michna H, Schneider MR (1995) The impact of tamoxifen and the pure antiestrogen ZM 182780 on the estrogen and progesterone receptor levels in rat mammary carcinoma and uterine tissue. In: 12th International Symposium of the Journal of Biochemistry and Molecular Biology, 21-24 May 1995, Berlin
37. McDonnell DP, Goldman ME (1994) RU486 exerts antiestrogenic activities through a novel progesterone receptor A form-mediated mechanism. J Biol Chem 269:11 945-11 949
38. McDonnell DP, Vegeto E, O'Malley BW (1992) Identification of a negative regulatory function for steroid receptors. Proc Natl Acad Sci USA 89:10 563-10 567
39. McDonnell TJ, Troncoso P, Brisbay SM, Logothetis C, Chung LWK, Hsieh JT, Tu SM, Campbell ML (1992) Expression of the protooncogene bcl-2 in the prostate and its association with emergence of androgen-independent prostate cancer. Cancer Res 52:6940-6944
40. Michna H, Schneider MR, Nishino Y, El Etreby MF (1989) The antitumor mechanism of progesterone antagonists is a receptor mediated antiproliferative effect by induction of terminal cell death. J Steroid Biochem 34:447-453
41. Michna H, Fritzemeier KH, Parczyk K, Nishino Y, Schneider MR (1996) Antiprogestin-progesterone interactions. In: Lippmann ME, Dickson RB (eds) Breast cancer: cellular and molecular biology
42. Mobbs BG, Johnson IE, Liu Y (1990) Quantitation of cytosolic and nuclear estrogen and progesterone receptor in benign, untreated, and treated malignant human prostatic tissue by radioligand binding and enzyme-immunoassays. Prostate 16:235-244
43. Muss HB (1992) Endocrine therapy for advanced breast cancer: a review. Breast Cancer Res Treat 21:15-26
44. Neumann F (1983) Pharmacological basis for clinical use of antiandrogens. J Steroid Biochem 19:391-402
45. Nicholson RI, Francis AB, McClelland RA, Manning DL, Gee JMW (1994) Pure anti-oestrogens (ICI 164384 and ICI 182780) and breast cancer: is the attainment of complete oestrogen withdrawal worthwile? Endocr Relat Cancer 1:5-17
46. Nieh PT (1995) Withdrawal phenomenon with the antiandrogen casodex. J Urol 153:1070-1073
47. Nishino Y, Schneider MR, Michna H (1994) Enhancement of the antitumor efficacy of the antiprogestin, onapristone, by combination with the antiestrogen, ICI 164384. J Cancer Res Clin Oncol 120:298-302
48. Osborne CK, Ester B, Coronado-Heinsohn, Susan G, Hilsenbeck, Bryant L, McCue, Wakeling AE, Richard A, McClelland, Manning DL, Nicholson RI (1995) Comparison of the effects of a pure steroidal antiestrogen with those of tamoxifen in a model of human breast cancer. J Natl Cancer Inst 87:746-750
49. Parczyk K, Madjno R, Angerer E von, Schneider MR (1995) Various pure antiestrogens downregulated the ER while partial agonists do not. In: 12th International Symposium of the Journal of Steroid Biochemistry and Molecular Biology, 21-24 May 1995, Berlin
50. Parczyk K, Michna H (1996) Androgen withdrawal reduces androgen receptor immunoreactivity in rat prostate carcinoma in contrast to androgen receptor antagonists. J Steroid Biochem Mol Biol
51. Park R, Grigsby PW, Muss H, Norris HJ (1992) Corpus: epithelial tumors. In: Hoskins W, Perez C, Young R (eds) Principles and practice of gynaecologic oncology. Lippincott, Philadelphia, pp 663-693
52. Patterson JS (1981) Clinical aspects and development of anti-oestrogen therapy: a review of the endocrine effects of tamoxifen in animals and man. J Endocrinol 89:67P-75P
53. Petrow V (1986) The dihydrotestosterone (DHT) hypothesis of prostate cancer and its therapeutic implications. Prostate 9:343-361
54. Pham TA, Elliston JF, Nawaz Z, McDonnell DP, Tsai MJ, O'Malley BW (1991) Antiestrogen can establish nonproductive receptor complexes and alter chromatin structure at target enhances. Proc Natl Acad Sci USA 88:3125-3129
55. Raghaven D (1988) Non-hormone chemotherapy for prostate cancer: principles of treatment and application to the testing of new drugs. Semin Oncol 15:371-389
56. Reed JC (1994) Bcl-2 and the regulation of programmed cell death. J Cell Biol 124:1-6
57. Ruizeveld de Winter JA, Janssen PJ, Sleddens HM, Verleun-Mooijman MC, Trapman J, Brinkmann AO, Santerse AB, Schroder FH, van derKwast TH (1994) Androgen receptor status in localized and locally progressive hormone refractory human. Am J Pathol 144:735-46
58. Santen RJ, Manni A, Harvey H, Redmond C (1990) Endocrine treatment of breast cancer in women. Endocr Rev 11:221-265
59. Savouret JF, Bailly A, Misrahi M, Rauch C, Redeuilh G, Chauchereau A, Milgrom E (1991) Characterization of the hormone responsive element involved in the regulation of the progesterone receptor gene. EMBO J 10:1875-1883
60. Scher HI, Kelly WK (1993) The flutamide withdrawal syndrome: Its impact on clinical trials in hormone-refractory prostatic cancer. J Clin Oncol 11:1566-1572
61. Schieweck K, Bhatnagar AS, Batzl CH, Lang M (1993) Anti-tumor and endocrine effects of non-steroidal aromatase inhibitors on estrogen-dependent rat mammary tumors. J Steroid Biochem Mol Biol 44:633-636
62. Schneider MR (1993) Antihormone: Von der Entdeckung der Steroid-hormone zu spezifischen Krebstherapeutika. Arch Pharm (Weinheim) 326:769-784
63. Schneider MR, Michna H, Nishino Y, El Etreby MF (1989) Antitumor activity of the progesterone antagonists ZK 98299 and RU486 in the hormone-dependent MXT mammary tumor model of the mouse and the DMBA- and MNU-induced mammary tumor model of the rat. Eur J Cancer Clin Oncol 25:691-701
64. Schneider MR, Humm A, Graf AH (1990a) The tumor-inhibiting effect of diethylstilbestrol and its diphosphate on the Nb-H and Nb-R prostatic carcinomas of the rat. J Cancer Res Clin Oncol 116:159-167
65. Schneider MR, Michna H, Nishino Y, El Etreby MF (1990b) Antitumor activity and mechanism of action of different antiprogestins in experimental breast cancer models. J Steroid Biochem Mol Biol 37:783-787
66. Schneider MR, Michna H, Nishino Y, Henderson D (1991) Antitumor activity and mechanism of action of progesterone antagonists in experimental breast cancer. In: Masobrio M, Menalo G, Cassoni P, Simonetta M (eds) Attualita endocrine in oncologia ginecologica e in medicina del riproduzione. Monduzzi, Bologna, pp 99-105
67. Schneider MR, Michna H, Habenicht UF, Nishino Y, Grill HJ, Pollow K (1992) The tumor-inhibiting potential of the progesterone antagonist onapristone in the human mammary carcinoma T61 in nude mice. J Cancer Res Clin Oncol 118:187-189
68. Smith CL, Conneely OM, O'Malley BW (1993) Modulation of the ligand-independent activation of the human estrogen receptor by hormone and antihormone. Proc Natl Acad Sci USA 90:6120-6124
69. Steinberg GD, Isaacs JT (1993) Pharmacological approaches to the management of metastatic prostatic cancer. In: Hickman JA, Tritton TR (eds) Cancer chemotherapy. Blackwell, London, pp 322-343
70. Steiner JF (1993) Finasteride: a 5α-reductase inhibitor. Clin Pharm 12:15-23
71. Taplin ML, Bubley GJ, Shuster TD, Frantz ME, Spooner AE, Ogata GK, Keer HN, Balk SP (1995) Mutation of the androgen-receptor gene in metastatic androgen-independent prostate cancer. N Engl J Med 332:1393-1398
72. Truss M, Bartsch J, Beato M (1994) Antiprogestins prevent progesterone receptor binding to hormone responsive elements in vivo. Proc Natl Acad Sci USA 91:11 333-11 337
73. Tucker H (1990) Non-steroidal anti-androgens in the treatment of prostate cancer. Drug Future 15:255-265
74. Van de Velde P, Nique F, Bouchoux F, Brémaud J, Hameau M-C, Lucas D, Moratille C, Viet S, Philibert D, Teutsch G (1994) RU 58 668, a new pure antiestrogen inducing a regression of human mammary carcinoma implanted in nude mice. J Steroid Biochem Mol Biol 48:187-196
75. Visakorpi T, Hyytinen E, Koivisto P, Tanner M, Keinänen R, Palmberg C, Palotie A, Tammela T, Isola J, Kallioniemi OP (1995) In vivo amplification of the androgen receptor gene and progression of human prostate cancer. Nat Genet 9:401-406
76. Vollmer G, Schneider MR (1996) The rat endometrial adenocarcinoma cell line Ruca-I: a novel hormone-responsive in vivo/in vitro tumor model. J Steroid Biochem Mol Biol
77. Voogt HJ de (1992) The position of cyproterone acetate (CPA), a steroidal anti-androgen, in the treatment of prostate cancer. Prostate 4:91-95
78. Wakeling AE (1985) Chemical structure and pharmacology of anti-oestrogens. History, current trends and future prospects. In: Pannuti F (ed) Anti-oestrogens in oncology. Past, present and prospects. Excerpta Medica, Amsterdam Geneva Hong Kong, pp 43-53
79. Wakeling AE (1989) Comparative studies on the effects of steroidal and nonsteroidal oestrogen antagonists on the proliferation of human breast cancer cells. J Steroid Biochem 34:183-188
80. Wakeling AE, Bowler J (1987) Steroidal pure antiestrogens. J Endocrinol 112:R7-R10
81. Wakeling AG, Dukes M, Bowler J (1991) A potent specific pure antiestrogen with clinical potential. Cancer Res 51:3867-3873
82. Weinbauer GF, Nieschlag E (1992) LH-RH antagonists: state of the art and future perspectives. Recent Results Cancer Res 124:113-136