Development of aromatase inhibitors and their pharmacologic profile

American Journal of Clinical Oncology: Cancer Clinical Trials

Volumn 26, Issue 4 SUPPL. 1, 2003, Pages

  Lønning, Per Eystein ^a   Geisler, Jürgen ^a   Bhatnager, Ajay ^b  

^a UNIVERSITY OF BERGEN   (Norway)

^b NOVARTIS PHARMA AG   (Switzerland)

Author keywords

Aromatase inhibitors; Breast cancer; Estrogen; Estrogen synthesis inhibition

Indexed keywords

AMINOGLUTETHIMIDE; ANASTROZOLE; ANDROGEN; ANTIESTROGEN; AROMATASE INHIBITOR; ESTROGEN; EXEMESTANE; FADROZOLE; FORMESTANE; LETROZOLE; PYRIDOGLUTETHIMIDE; TAMOXIFEN;

ADRENALECTOMY; BREAST CANCER; CANCER GROWTH; CLINICAL TRIAL; DRUG EFFICACY; ENZYME INHIBITION; HUMAN; HYPOPHYSECTOMY; OVARIECTOMY; POSTMENOPAUSE; REVIEW;

ANTINEOPLASTIC AGENTS; AROMATASE INHIBITORS; BREAST NEOPLASMS; ENZYME INHIBITORS; ESTROGEN ANTAGONISTS; FEMALE; HUMANS; NEOPLASMS, HORMONE-DEPENDENT; NITRILES; TRIAZOLES;

EID: 0042591541     PISSN: 02773732     EISSN: None     Source Type: Journal    
DOI: 10.1097/00000421-200308001-00002     Document Type: Review

References (30)

1. Beatson G. On the treatment of inoperable cases of carcinoma of the mamma: suggestions for a new method of treatment with illustrative cases. Lancet 1896;2:104-7.
2. Cash R, Brough AJ, Cohen MN, et al. Aminoglutethimide (Elipten-Ciba) as an inhibitor of adrenal steroidogenesis: mechanism of action and therapeutic trial. J Clin Endocrinol Metab 1967;27:1239-48.
3. Santen RJ, Santner S, Davis B, et al. Aminoglutethimide inhibits extraglandular estrogen production in postmenopausal women with breast carcinoma. J Clin Endocrinol Metab 1978;47:1257-65.
4. Santen RJ, Worgul TJ, Samojlik E, et al. A randomized trial comparing surgical adrenalectomy with aminoglutethimide plus hydrocortisone in women with advanced breast cancer. N Engl J Med 1981;305:545-51.
5. Dickson RB, Lippman ME. Growth factors in breast cancer. Endocrin Rev 1995;16:559-89.
6. Hemsell DL, Grodin JM, Brenner PF, et al. Plasma precursors of estrogen. II. Correlation of the extent of conversion of plasma androstenedione to estrone with age. J Clin Endocrinol Metab 1974;38:476-9.
7. Grodin J, Siiteri P, MacDonald P. Source of estrogen production in the postmenopausal woman. J Clin Endocrinol Metab 1973;36: 207-14.
8. O'Regan RM, Gradishar WJ. Selective estrogen-receptor modulators in 2001. Oncology (Huntingt) 2001;15:1177-85, 89-90; discussion 90-4.
9. Port ER, Montgomery LL, Heerdt AS, et al. Patient reluctance toward tamoxifen use for breast cancer primary prevention. Ann Surg Oncol 2001;8:580-5.
10. Dombernowsky P, Smith I, Falkson G, et al. Letrozole, a new oral aromatase inhibitor for advanced breast cancer: double-blind randomized trial showing a dose effect and improved efficacy and tolerability compared with megestrol acetate. J Clin Oncol 1998; 16:453-61.
11. Buzdar AU, Jonat W, Howell A, et al. Anastrozole versus megestrol acetate in the treatment of postmenopausal women with advanced breast carcinoma: results of a survival update based on a combined analysis of data from two mature phase III trials. Arimidex Study Group. Cancer 1998;83:1142-52.
12. Gershanovich M, Chaudri HA, Campos D, et al. Letrozole, a new oral aromatase inhibitor: randomised trial comparing 2.5 mg daily, 0.5 mg daily and aminoglutethimide in postmenopausal women with advanced breast cancer. Letrozole International Trial Group (AR/BC3). Ann Oncol 1998;9:639-45.
13. 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;92:2247-58.
14. 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;19:2596-606.
15. Kaufmann M, Bajetta E, Dirix LY, et al. Exemestane is superior to megestrol acetate after tamoxifen failure in postmenopausal women with advanced breast cancer: results of a phase III randomized double-blind trial. The Exemestane Study Group. J Clin Oncol 2000;18:1399-411.
16. Dirix LY, Piccart MJ, Lohrisch C, et al. Efficacy of and tolerance to exemestane (E) versus tamoxifen (T) in 1st line hormone therapy (HT) of postmenopausal metastatic breast cancer (MBC) patients (pts): a European Organisation for the Research and Treatment of Cancer (EORTC Breast Group) Phase II trial with Pharmacia and Upjohn [Abstract 114]. Proc Am Soc Clin Oncol 2001;20:29a.
17. Murphy MJ Jr. Molecular action and clinical relevance of aromatase inhibitors. Oncologist 1998;3:129-30.
18. Masamura S, Santner SJ, Heitjan DF, et al. Estrogen deprivation causes estradiol hypersensitivity in human breast cancer cells. J Clin Endocrinol Metab 1995;80:2918-25.
19. Bhatnagar AS, Brodie AM, Long BJ, et al. Intracellular aromatase and its relevance to the pharmacological efficacy of aromatase inhibitors. J Steroid Biochem Mol Biol 2001;76:199-202.
20. Bhatnagar AS, Batel C, Häusler A, et al. Pharmacology of non-steroidal aromatase inhibitors in hormone-dependent cancer. (Pasqualini JR, Valzenellenbogen BS, Eds), 1996 New York, Marcel Dekker pp 155-168.
21. Bhatnagar AS, Hausler A, Schieweck K, et al. Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor. J Steroid Biochem Mol Biol 1990; 37:1021-7.
22. Pfister CU, Martoni A, Zamagni C, et al. Effect of age and single versus multiple dose pharmacokinetics of letrozole (Femara) in breast cancer patients. Biopharm Drug Dispos 2001;22:191-7.
23. Miller WR, Dixon JM. Local endocrine effects of aromatase inhibitors within the breast. J Steroid Biochem Mol Biol 2001;79: 93-102.
24. Geisler J, King N, Dowsett M, et al. Influence of anastrozole (Arimidex), a selective, non-steroidal aromatase inhibitor, on in vivo aromatisation and plasma oestrogen levels in postmenopausal women with breast cancer. Br J Cancer 1996;74:1286-91.
25. Dowsett M, Jones A, Johnston SR, et al. In vivo measurement of aromatase inhibition by letrozole (CGS 20267) in postmenopausal patients with breast cancer. Clin Cancer Res 1995;1:1511-5.
26. Geisler J, King N, Anker G, et al. In vivo inhibition of aromatization by exemestane, a novel irreversible aromatase inhibitor, in postmenopausal breast cancer patients. Clin Cancer Res 1998;4: 2089-93.
27. Lonning PE. Aromatase inhibition for breast cancer treatment. Acta Oncol 1996;35(suppl 5):38-43.
28. Geisler J, Haynes B, Anker G, et al. 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;20:751-7.
29. Rose C, Vtoraya O, Pluzanska A, et al. Letrozole (Femara) vs. anastrozole (Arimidex): second-line treatment in postmenopausal women with advanced breast cancer [Abstract 131]. Proc Am Soc Clin Oncol 2002;21:34A.
30. Geisler J, Dowsett M, Lønning PE. Letrozole is more effective than anastrozole in suppressing total body aromatization and plasma estrogens levels in postmenopausal breast cancer patients. Am J Oncol Rev 2002;1:99-102.