Exemestane: Treatment of breast cancer with selective inactivation of aromatase

American Journal of Health-System Pharmacy

Volumn 59, Issue 22, 2002, Pages 2194-2204

  Higa, Gerald M ^a  

^a WEST VIRGINIA UNIVERSITY   (United States)

Author keywords

Antineoplastic agents; Breast neoplasms; Exemestane; Mechanism of action; Neoplasm metastasis; Toxicity

Indexed keywords

AMINOGLUTETHIMIDE; ANASTROZOLE; AROMATASE; AROMATASE INHIBITOR; CYTOCHROME P450; ESTROGEN; ESTROGEN RECEPTOR; EXEMESTANE; FADROZOLE; FORMESTANE; GLUCOCORTICOID; LETROZOLE; MEGESTROL ACETATE; SEX HORMONE BINDING GLOBULIN; TAMOXIFEN;

ABDOMINAL PAIN; ACNE; ADDISON DISEASE; ALOPECIA; ANOREXIA; BREAST CANCER; CANCER HORMONE THERAPY; CANCER SURVIVAL; CLINICAL TRIAL; CONSTIPATION; COST EFFECTIVENESS ANALYSIS; CROSS RESISTANCE; DEPRESSION; DIARRHEA; DOSE RESPONSE; DRUG COST; DRUG EFFICACY; DRUG INDICATION; DRUG MECHANISM; DRUG SAFETY; DRUG TOLERABILITY; DYSPNEA; ENZYME INACTIVATION; ESTROGEN SYNTHESIS; FATIGUE; FOOD DRUG INTERACTION; HAIR LOSS; HEADACHE; HOARSENESS; HOT FLUSH; HUMAN; HYPERHIDROSIS; HYPERTRICHOSIS; INCREASED APPETITE; INSOMNIA; LIVER DISEASE; METASTASIS; NAUSEA; PAIN; PARESTHESIA; PERIPHERAL EDEMA; POSTMENOPAUSE; PRIORITY JOURNAL; RASH; REVIEW; SIDE EFFECT; VERTIGO; VOMITING;

EID: 0037111583     PISSN: 10792082     EISSN: None     Source Type: Journal    
DOI: 10.1093/ajhp/59.22.2194     Document Type: Review

References (64)

1. Pike MC, Krailo MD, Henderson BE et al. 'Hormonal' risk factors, 'breast tissue age' and the age-incidence of breast cancer. Nature. 1983; 303:767-70.
2. Pujol P, Hilsenbeck SG, Chamness GC et al. Rising levels of estrogen receptor in breast cancer over 2 decades. Cancer. 1994; 74:1601-6.
3. Miller WR. Estrogens and endocrine therapy for breast cancer. In: WR Miller, ed. Estrogen and Breast Cancer. Austin, TX: Landes; 1996:125-50.
4. Glick JH, Creech RH, Torri S et al. Tamoxifen plus sequential CMF chemotherapy versus tamoxifen alone in postmenopausal patients with advanced breast cancer: A randomized trial. Cancer. 1980; 45:735-41.
5. Bezwoda WR, Derman D, MeMoor NG et al. Treatment of metastatic breast cancer in estrogen receptor-positive patients: A randomized trial comparing tamoxifen alone versus tamoxifen plus CMF. Cancer. 1982; 50:2747-50.
6. Esteban JM, Ahn C, Battifora H et al. Biological significance of quantitative estrogen receptor immuno-histochemical assay by image analysis in breast cancer patients. Am J Clin Pathol. 1994; 102:158-62.
7. Horwitz KB. Mechanisms of hormone resistance in breast cancer. Breast Cancer Res Treat. 1993; 26:119-30.
8. Osborne CK, Coronado E, Allred DC et al. Acquired tamoxifen resistance: Correlation with reduced breast tumor levels of tamoxifen and isomerization of trans-4-hydroxytamoxifen. J Natl Cancer Inst. 1991; 83:1477-82.
9. Fuqua SAW, Allred DC, Auchus RJ. Expression of estrogen receptor variants. J Cell Biochem. 1993; 17G:194-7.
10. Johnston SR, Saccani-Jotti G, Smith IE et al. Changes in estrogen receptor, progesterone receptor, and pS2 expression in tamoxifen-resistant human breast cancer. Cancer Res. 1995; 55:3331-8.
11. McClelland RA, Barrow D, Madden TA et al. Enhanced epidermal growth factor receptor signaling in MCF7 breast cancer cells after long-term culture in the presence of the pure antiestrogen ICI 182,780 (Faslodex). Endocrinology. 2001; 142:2776-88.
12. Cole PA, Robinson CH. Mechanism and inhibition of cytochrome P-450 aromatase. J Med Chem. 1990; 33:2933-42.
13. Thompson EA, Siiteri PK. Utilization of oxygen and reduced nicotinamide adenine dinucleotide phosphate by human placental microsomes during aromatization of androstenedione. J Biol Chem. 1974; 249:5364-72.
14. Grodin JM, Siiteri PK, MacDonald PC. Source of estrogen production in postmenopausal women. J Clin Endocrinol Metab. 1973; 36:207-14.
15. Bulun SE, Simpson ER. Regulation of aromatase expression in human tissues. Breast Cancer Res Treat. 1994; 30:19-29.
16. Di Salle E, Giudici D, Briatico G et al. Novel irreversible aromatase inhibitors. Ann N Y Acad Sci. 1990; 595:357-67.
17. Cocconi G. First generation aromatase inhibitors - Aminoglutethimide and testololactone. Breast Cancer Res Treat. 1994; 30:57-80.
18. Lonning PE, Kvinnsland S. Mechanisms of action of aminoglutethimide as endocrine therapy of breast cancer. Drugs. 1988; 35:685-710.
19. Bajetta E, Celio L, Buzzoni R et al. Novel non-steroidal aromatase inhibitors: Are there new perspectives in the treatment of breast cancer? Tumori. 1996; 82:417-22.
20. Shetty G, Krishnamurthy H, Krishnamurthy HN et al. Effect of estrogen deprivation on the reproductive physiology of male and female primates. J Steroid Biochem Mol Biol. 1997; 61:157-66.
21. Giudici D, Ornati G, Briatico G et al. 6-Methyleneandrosta-1,4-diene-3,17-dione (FCE 24304): A new irreversible, aromatase inhibitor. J Steroid Biochem. 1988; 30:391-4.
22. Evans TR, Di Salle E, Ornati G et al. Phase I and endocrine study of exemestane (FCE 24304), a new aromatase inhibitor, in postmenopausal women. Cancer Res. 1992; 52:5933-9.
23. Jannuzzo MG, Spinelli R, Poggesi I et al. Inhibition of CYP3A4 does not influence Aromasin (exemestane, EXE) pharmacokinetics (PK) in healthy postmenopausal volunteers (HPV). Eur J Cancer. 1999; 35 (suppl 4):S295. Abstract.
24. Cocchiara G, Allievi C, Berardi A et al. Urinary metabolism of exemestane, a new aromatase inhibitor, in rat, dog, monkey and human volunteers. J Endocrinol Invest. 1994; 17:78.
25. Buzzetti F, Di Salle E, Longo A et al. Synthesis and aromatase inhibition by potential metabolites of exemestane (6-methyleneandrosta-1,4-diene-3,17-dione). Steroids. 1993; 58:527-32.
26. In-House Aromasin Data. Kalamazoo, MI: Pharmacia Corporation; 1999.
27. Thurlimann B, Paridaens R, Serin D et al. Third-line hormonal treatment with exemestane in postmenopausal patients with advanced breast cancer progressing on aminoglutethimide: A Phase II multicentre multinational study. Exemestane Study Group. Eur J Cancer. 1997; 33:1767-73.
28. Johannessen DC, Engan T, di Salle E et al. Endocrine and clinical effects of exemestane (PNU 155971), a novel steroidal aromatase inhibitor, in postmenopausal breast cancer patients: A Phase I study. Clin Cancer Res. 1997; 3:1101-8.
29. 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.
30. 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.
31. Jones AL, MacNeill F, Jacobs S et al. The influence of intramuscular 4-hydroxyandrostenedione on peripheral aromatisation in breast cancer patients. Eur J Cancer. 1992; 10:1712-6.
32. Geisler J, King N, Dowsett M et al. Influence of anastrozole (Arimidex), a selective, nonsteroidal aromatase inhibitor, on in vivo aromatisation and plasma oestrogen levels in postmenopausal women with breast cancer. Br J Cancer. 1996; 74:1286-91.
33. Santen RJ, Demers LM, Lynch J et al. Specificity of low dose fadrozole hydrochloride (CGS 16949A) as an aromatase inhibitor. J Clin Endocrinol Metab. 1991; 73:99-106.
34. 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.
35. Di Salle E, Ornati G, Giudici D et al. Exemestane (FCE 24304), a new steroidal aromatase inhibitor. J Steroid Biochem Mol Biol. 1992; 43:137-43.
36. Bajetta E, Zilembo N, Noberasco C et al. The minimal effective exemestane dose for endocrine activity in advanced breast cancer. Eur J Cancer. 1997; 33:587-91.
37. Zilembo N, Noberasco C, Bajetta E et al. Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor. Br J Cancer. 1995; 72:1007-12.
38. Di Salle E, Briatico G, Giudici D et al. Novel aromatase and 5 alpha-reductase inhibitors. J Steroid Biochem Mol Biol. 1994; 49:289-94.
39. Jones S, Vogel C, Arkhipov A et al. Multicenter, Phase II trial of exemestane as third-line hormonal therapy of postmenopausal women with metastatic breast cancer. Aromasin Study Group. J Clin Oncol. 1999; 17:3418-25.
40. Lonning PE, Bajetta E, Murray R et al. Activity of exemestane in metastatic breast cancer after failure of nonsteroidal aromatase inhibitors: A Phase II trial. J Clin Oncol. 2000; 18:2234-44.
41. Buzdar A, Jonat W, Howell A et al. Anastrozole, a potent and selective aromatase inhibitor, versus megestrol acetate in postmenopausal women with advanced breast cancer: Results of overview analysis of two Phase III trials. Arimidex Study Group. J Clin Oncol. 1996; 14:2000-11.
42. 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.
43. Dirix L, 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 on Cancer (EORTC Breast Group) Phase II trial with Pharmacia and Upjohn. Proc Am Soc Clin Oncol. 2001; 20:29a. Abstract.
44. Early Breast Cancer Trialists' Collaborative Group. Systemic treatment of early breast cancer by hormonal, cytotoxic, or immune therapy. 133 Randomized trials involving 31,000 recurrences and 24,000 deaths among 75,000 women. Lancet. 1992; 339:71-85.
45. Early Breast Cancer Trialists' Collaborative Group. Tamoxifen for early breast cancer: An overview of the randomised trials. Lancet. 1998; 351:1451-67.
46. Lonning PE. The role of aromatase inactivators in the treatment of breast cancer. Int J Clin Oncol. 2002; 7:265-70.
47. Simpson ER, Mehendroo MS, Means GD. Tissue-specific promoters regulate cytochrome P-450 expression. J Steroid Biochem Mol Biol. 1993; 44:321-30.
48. Lien EA, Anker G, Lonning PE et al. Decreased serum concentrations of tamoxifen and its metabolites induced by aminoglutethimide. Cancer Res. 1990; 50:5851-7.
49. Ingle JN, Suman VJ, Johnson PA et al. Evaluation of tamoxifen plus letrozole with assessment of pharmacokinetic interaction in postmenopausal women with metastatic breast cancer. Clin Cancer Res. 1999; 5:1642-9.
50. Lindgren P, Jonsson B, Redaelli A, Radice D. Cost-effectiveness analysis of exemestane compared to megestrol in advanced breast cancer: A model for Europe and Australia. Pharmacoeconomics. 2002; 20:101-8.
51. Hillner BE, Radice D. Cost-effectiveness analysis of exemestane compared with megestrol in patients with advanced breast carcinoma. Cancer. 2001; 91:484-9.
52. Drug Topics Red Book. Montvale, NJ: Medical Economics; 2002:214.
53. 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. J Clin Oncol. 2000; 18:3758-67.
54. 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; 18:3748-57.
55. 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.
56. Thompson TA, Vermeulen JD, Wagner WE et al. Aminoglutethimide bioavailability, pharmacokinetics, and binding to blood constituents. J Pharm Sci. 1981; 70:1040-3.
57. 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.
58. Smith IE, Norton A. Fadrozole and letrozole in advanced breast cancer: Clinical and biochemical effects. Breast Cancer Res Treat. 1998; 49:S67-71,S73-7.
59. Kochak GM, Mangat S, Mulagha MT et al. The pharmacodynamic inhibition of estrogen synthesis by fadrozole, an aromatase inhibitor, and its pharmacokinetic disposition. J Clin Endocrinol Metab. 1990; 71:1349-55.
60. Lamb HM, Adkins JC. Letrozole. A review of its use in postmenopausal women with advanced breast cancer. Drugs. 1998; 56:1125-40.
61. Demers LM. Effects of fadrozole (CGS 16949A) and letrozole (CGS 20267) on the inhibition of aromatase activity in breast cancer patients. Breast Cancer Res Treat. 1994; 30:95-102.
62. Dowsett M, Cunningham DC, Stein RC et al. Dose-related endocrine effects and pharmacokinetics of oral and intramuscular 4-hydroxyandrostenedione in postmenopausal breast cancer patients. Cancer Res. 1989; 49:1306-12.
63. Carrion RC, Candel V, Calabresi F et al. Comparison of the selective aromatase inhibitor formestane with tamoxifen as first-line hormonal therapy in postmenopausal women with advanced breast cancer. Ann Oncol. 1994; 5:S19-24.
64. Thurlimann B, Castiglione M, Hsu-Schmitz SF et al. Formestane versus megestrol acetate in postmenopausal breast cancer patients after failure of tamoxifen: A Phase III prospective randomised cross over trial of second-line hormonal treatment (SAKK 20/90). Swiss Group for Clinical Cancer Research (SAKK). Eur J Cancer. 1997; 33:1017-24.