Pharmacokinetics of third-generation aromatase inhibitors

Seminars in Oncology

Volumn 30, Issue 4 SUPPL. 14, 2003, Pages 23-32

  Lønning, Per ^a   Pfister, Christian ^b   Martoni, Andrea ^b   Zamagni, Claudio ^b  

^a UNIVERSITY OF BERGEN   (Norway)

^b NONE

Author keywords

[No Author keywords available]

Indexed keywords

AMINOGLUTETHIMIDE; ANALGESIC AGENT; ANASTROZOLE; ANTICOAGULANT AGENT; ANTIHYPERTENSIVE AGENT; AROMATASE; AROMATASE INHIBITOR; BENZODIAZEPINE DERIVATIVE; CIMETIDINE; EXEMESTANE; FADROZOLE; FORMESTANE; KETOCONAZOLE; LETROZOLE; NONSTEROID ANTIINFLAMMATORY AGENT; NORTAMOXIFEN; PHENOBARBITAL; PYRIDOGLUTETHIMIDE; TAMOXIFEN; TESTOLACTONE; TRIAZOLE DERIVATIVE; VOROZOLE; WARFARIN;

BONE MARROW SUPPRESSION; BREAST CANCER; CANCER CHEMOTHERAPY; CLINICAL TRIAL; DROWSINESS; DRUG CLEARANCE; DRUG EFFECT; DRUG EFFICACY; DRUG ERUPTION; DRUG HALF LIFE; DRUG MECHANISM; DRUG METABOLISM; FOOD AND DRUG ADMINISTRATION; HUMAN; LETHARGY; LONG TERM CARE; NONHUMAN; POSTMENOPAUSE; PRIORITY JOURNAL; REVIEW; TREATMENT OUTCOME;

EID: 0141428055     PISSN: 00937754     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0093-7754(03)00305-1     Document Type: Article

References (75)

1. 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 38:476-479, 1974
2. Thorsen T, Tangen M, Stoa K: Concentrations of endogenous estradiol as related to estradiol receptor sites in breast tumor cytosol. Eur J Cancer Clin Oncol 18:333-337, 1982
3. van Landeghem AA, Poortman J, Nabuurs M, et al: Endogenous concentration and subcellular distribution of estrogens in normal and malignant human breast tissue. Cancer Res 45:2900-2906, 1985
4. Blankenstein MA, Szymczak J, Daroszewski J, et al: Estrogens in plasma and fatty tissue from breast cancer patients and women undergoing surgery for non-oncological reasons. Gynecol Endocrinol 6:13-17, 1992
5. Thijssen JH, Blankenstein MA, Miller WR, et al: Estrogens in tissues: Uptake from the peripheral circulation or local production. Steroids 50:297-306, 1987
6. Szymczak J, Milewicz A, Thijssen JH, et al: Concentration of sex steroids in adipose tissue after menopause. Steroids 63:319-321, 1998
7. Geisler J, Berntsen H, Lønning PE: A novel HPLC-RIA method for the simultaneous detection of estrone, estradiol and estrone sulphate levels in breast cancer tissue. J Steroid Biochem Mol Biol 72:259-264, 2000
8. Miller WR: Aromatase activity in breast tissue. J Steroid Biochem Mol Biol 39:783-790, 1991
9. Sasano H, Nagura H, Harada N, et al: Immunolocalization of aromatase and other steroidogenic enzymes in human breast disorders. Hum Pathol 25:530-535, 1994
10. Bulun SE, Price TM, Aitken J, et al: A link between breast cancer and local estrogen biosynthesis suggested by quantification of breast adipose tissue aromatase cytochrome P450 transcripts using competitive polymerase chain reaction after reverse transcription. J Clin Endocrinol Metab 77:1622-1628, 1993
11. Lønning PE, Kvinnsland S: Mechanisms of action of aminoglutethimide as endocrine therapy of breast cancer. Drugs 35:685-710, 1988
12. Buzdar AU, Smith R, Vogel C, et al: Fadrozole HCL (CGS-16949A) versus megestrol acetate treatment of postmenopausal patients with metastatic breast carcinoma: Results of two randomized double blind controlled multiinstitutional trials. Cancer 77:2503-2513, 1996
13. 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 33:1017-1024, 1997
14. Thurlimann B, Beretta K, Bacchi M, et al: First-line fadrozole HCI (CGS 16949A) versus tamoxifen in postmenopausal women with advanced breast cancer. Prospective randomised trial of the Swiss Group for Clinical Cancer Research SAKK 20/88. Ann Oncol 7:471-479, 1996
15. Falkson CI, Falkson HC: A randomised study of CGS 16949A (fadrozole) versus tamoxifen in previously untreated postmenopausal patients with metastatic breast cancer. Ann Oncol 7:465-469, 1996
16. Perez Carrion R, Alberola 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 5:S19-S24, 1994 (suppl 7)
17. MacNeill F, Jones A, Jacobs S, et al: The influence of aminoglutethimide and its analogue rogletimide on peripheral aromatization in breast cancer. Br J Cancer 66:692-697, 1992
18. Jones AL, MacNeill F, Jacobs S, et al: The influence of intramuscular 4-hydroxyandrostenedione on peripheral aromatisation in breast cancer patients. Eur J Cancer 28A:1712-1716, 1992
19. MacNeill F, Jacobs S, Dowsett M, et al: The effects of oral 4-hydroxyandrostenedione on peripheral aromatisation in post-menopausal breast cancer patients. Cancer Chemother Pharmacol 36:249-254, 1995
20. Dowsett M, Lloyd P: Comparison of the pharmacokinetics and pharmacodynamics of unformulated and formulated 4-hydroxyandrostenedione taken orally by healthy men. Cancer Chemother Pharmacol 27:67-71, 1990
21. 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 3:1101-1108, 1997
22. 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 74:1286-1291, 1996
23. 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 1:1511-1515, 1995
24. Yates RA, Dowsett M, Fisher GV, et al: Arimidex (ZD1033): A selective, potent inhibitor of aromatase in postmenopausal female volunteers. Br J Cancer 73:543-548, 1996
25. 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 20:751-757, 2002
26. Lønning PE: Stepwise estrogen suppression manipulating the estrostat. J Steroid Biochem Mol Biol 79:127-132, 2001
27. 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 4:2089-2093, 1998
28. Lønning PE: Cross-resistance to different aromatase inhibitors in breast cancer treatment. Endocr Relat Cancer 6:251-257, 1999
29. 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 37:1021-1027, 1990
30. Bhatnagar AS, Batzl C, Hausler A, et al: Pharmacology of nonsteroidal aromatase inhibitors, in Katzenellenbogen BS (ed): Hormone Dependent Cancer. New York, NY, Marcel Dekker, 1996, pp 155-168
31. 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 52:5933-5939, 1992
32. Bajetta E, Zilembo N, Dowsett M, et al: Double-blind, randomised, multicentre endocrine trial comparing two letrozole doses, in postmenopausal breast cancer patients. Eur J Cancer 35:208-213, 1999
33. Bisagni G, Cocconi G, Scaglione F, et al: Letrozole, a new oral non-steroidal aromastase inhibitor in treating postmenopausal patients with advanced breast cancer. A pilot study. Ann Oncol 7:99-102, 1996
34. Baldinger SL, De Fusco P: Focus on anastrozole: an aromatase inhibitor for the treatment of hormonally dependent advanced breast cancer. Formulary 31:363-364, 1996
35. Buzdar A, Esparza-Guerra L: Anastrozole 'Arimidex' does not impair adrenal cortisol or aldosterone synthesis in postmenopausal women with advanced breast cancer. Proc Am Soc Clin Oncol 20:52b(abstr 1954), 2001
36. Lønning PE: Aminoglurethimide enzyme induction: pharmacological and endocrinological implications. Cancer Chemother Pharmacol 26:241-244, 1990
37. Lien EA, Anker G, Lønning PE, et al: Decreased serum concentrations of tamoxifen and its metabolites induced by aminoglutethimide. Cancer Res 50:5851-5857, 1990
38. Dehal SS, Brodie AM, Kupfer D: The aromatase inactivator 4-hydroxyandrostenedione (4-OH-A) inhibits tamoxifen metabolism by rat hepatic cytochrome P-450 3A: Potential for drug-drug interaction of tamoxifen and 4-OH-A in combined antibreast cancer therapy. Drug Metab Dispos 27:389-394, 1999
39. Tominaga T, Kimura M, Toge T, et al: A combined effect of fadrozole and tamoxifen in postmenopausal patients with recurrent breast cancer: A preliminary report. Japanese Cooperative Study Group of Fadrozole and Tamoxifen. Gan To Kagaku Ryoho 27:1709-1718, 2000
40. Brodie AM, Schwarzel WC, Shaikh AA, et al: The effect of an aromatase inhibitor, 4-hydroxy-4-androstene-3,17-dione, on estrogen-dependent processes in reproduction and breast cancer. Endocrinology 100:1684-1695, 1977
41. Wiseman LR, McTavish D: Formestane. A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential in the management of breast cancer and prostatic cancer. Drugs 45:66-84, 1993
42. Dowsett M, Mehta A, King N, et al: An endocrine and pharmacokinetic study of four oral doses of formestane in postmenopausal breast cancer patients. Eur J Cancer 28:415-420, 1992
43. Lønning PE, Geisler J, Johannessen DC, et al: Pharmacokinetics and metabolism of formestane in breast cancer patients. J Steroid Biochem Mol Biol 77:39-47, 2001
44. Choi RL, Sun JX, Kochak GM: The effect of food on the relative bioavailability of fadrozole hydrochloride. Biopharm Drug Dispos 14:779-784, 1993
45. Kochak GM, Choi RL, Entwistle EA: Dose proportionality and population characteristics of oral fadrozole hydrochloride, an aromatase inhibitor, in postmenopausal women. Pharm Res 10:1760-1764, 1993
46. Goss PE, Winer EP, Tannock IF, et al: Randomized phase III trial comparing the new potent and selective third-generation aromatase inhibitor vorozole with megestrol acetate in postmenopausal advanced breast cancer patients. North American Vorozole Study Group. J Clin Oncol 17:52-63, 1999
47. Johnson PE, Buzdar A: Are differences in the available aromatase inhibitors and inactivators significant? Clin Cancer Res 7:4360s-4368s; discussion 4411s-4412s, 2001
48. 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 14:2000-2011, 1996
49. Buzdar A, Douma J, Davidson N, et al: Phase III, multicenter, double-blind, randomized study of letrozole, an aromatase inhibitor, for advanced breast cancer versus megestrol acetate. J Clin Oncol 19:3357-3366, 2001
50. 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 16:453-461, 1998
51. 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 9:639-645, 1998
52. 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 18:1399-1411, 2000
53. 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 92:2247-2258, 2001
54. 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 Letrozle Breast Cancer Group. J Clin Oncol 19:2596-2606, 2001
55. 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. Proc Am Soc Clin Oncol 20:29a, 2001 (abstr 114a)
56. Lønning 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 18:2234-2244, 2000
57. Zilembo N, Noberasco C, Bajetta E, et al: Endocrinological and clinical evaluation of exemestane, a new steroidal aromatase inhibitor. Br J Cancer 72:1007-1012, 1995
58. Spinelli R, Jannuzzo MG, Poggesi I, et al: Pharmocokinetics (PK) of Aromasin (exemestane, EXE) after single and repeated doses in healthy postmenopausal volunteers (HPV). Eur J Cancer 35:S295, 1999 (abstr 1185)
59. Jannuzzo M, Spinelli R, Poggesi I, et al: Inhibition of CYP3A4 does not influence Aromasin (R) (Exemestane, EXE) pharmacokinetics (PK) in healthy postmenopausal volunteers (HPV). Eur J Cancer 35:S294(abstr 1184), 1999 (suppl 4)
60. Camp-Sorrell D: Anastrozole. An effective, second-line hormonal treatment for advanced breast cancer. Cancer Pract 5:391-393, 1997
61. Grimm S, Dyroff M: Inhibition of human drug metabolizing cytochromes P450 by anastrozole, a potent and selective inhibitor of aromatase. Drug Metab Dispos 25:598-602, 1997
62. Sioufi A, Gauducheau N, Pineau V, et al: Absolute bioavailability of letrozole in healthy postmenopausal women. Biopharm Drug Dispos 18:779-789, 1997
63. Sioufi A, Sandrenan N, Godbillon J, et al: Comparative bioavailability of letrozole under fed and fasting conditions in 12 healthy subjects after a 2. 5 mg single oral administration. Biopharm Drug Dispos 18:489-497, 1997
64. 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 22:191-197, 2001
65. Colussi DM, Parisot CY, Lefevre GY: Plasma protein binding of letrozole, a new nonsteroidal aromatase enzyme inhibitor. J Clin Pharmacol 38:727-735, 1998
66. Wirz B, Valles B, Parkinson A: CYP3A4 and CYP2A6 are involved in the biotransformation of letrozole. 7th North American ISSX Meeting. San Diego, CA, 1996, vol 10, S359 (abstr)
67. Damanhouri Z, Herbert S, Nicholls P: Aminoglutethimide as an inducer of oxidative drug metabolism in the rat. Pharmacol Ther 33:145-152, 1987
68. Murray M, Cantrill E, Farrell G: Induction of cytochrome P450 2B1 in rat liver by the aromatase inhibitor aminoglutethimide. J Pharmacol Exp Ther 265:477-481, 1993
69. Kao Y, Okubo T, Sun X, et al: Induction of aromatase expression by aminoglutethimide, an aromatase inhibitor that is used to treat breast cancer in postmenopausal women. Anticancer Res 19:2049-2056, 1999
70. 14C-aminoglutethimide in several animal species and man. Xenobiotica 18:75-81, 1988
71. Baum M, Dowsett M, Coibion M, et al: Pharmacokinetics of anastrozole and tamoxifen alone, and in combination, during adjuvant endocrine therapy for early breast cancer in postmenopausal women: A sub-protocol of the 'Arimidex and Tamoxifen Alone or in Combination' (ATAC) trial. Br J Cancer 85:317-324, 2001
72. 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 5:1642-1649, 1999
73. Dowsett M, Pfister C, Johnston SR, et al: Impact of tamoxifen on the pharmacokinetics and endocrine effects of the aromatase inhibitor letrozole in postmenopausal women with breast cancer. Clin Cancer Res 5:2338-2343, 1999
74. Yates RA, Wong J, Seiberling M, et al: The effect of anastrozole on the single pharmacokinetics and anticoagulant activity of warfarin in healthy volunteers. Br J Clin Pharmacol 51:429-435, 2001
75. Dowsett M: Drug and hormone interactions of aromatase inhibitors. Endocr Relat Cancer 6:181-185, 1999