Letrozole for the management of breast cancer

References

• Greenlee RT, Hill-Harmon MB, Murray T, Thun M. Cancer statistics, 2001. CA Cancer J. Chn. 51,15-36 (2001).
   Google Scholar
• Sant M, Capocaccia R, Coleman MP et al Cancer survival increases in Europe but international differences remain wide. Eur. J. Cancer 37,1659–1667 (2001).
   PubMed Web of Science ®Google Scholar
• Szymczak J, Milewicz A, Thijssen JH, Blankenstein MA, Daroszewski J. Concentration of sex steroids in adipose tissue after menopause. Steroids 63,319–321 (1998).
   Google Scholar
• Miller WR, Mullen P, Sourdaine P et al. Regulation of aromatase activity within the breast.' Steroid Biochem. Mot Biol. 61, 193–202 (1997).
   PubMed Web of Science ®Google Scholar
• Santen RJ, Harvey HA. Use of aromatase inhibitors in breast carcinoma. Endocr. Relat. Cancer 6,75–92 (1999).
   PubMed Web of Science ®Google Scholar
• Dowsett M, Lee K, Macaulay VM et al. The control and biological importance of intratumoural aromatase in breast cancer.' Steroid Biochem. MoZ Biol. 56,145–150 (1996).
   PubMedGoogle Scholar
• Santen RJ, Martel J, Hoagland M et al. Demonstration of aromatase activity and its regulation in breast tumor and benign breast fibroblasts. Breast Cancer Res. Treat. 49, S93-99; discussion S109-119 (1998).
   Google Scholar
• Dickson RB, Lippman ME. Molecular basis of breast cancer. In: The Molecular Basis of Cancer. Mendelsohn J (Ed.), WB Saunders, Philadelphia, PA, USA, 358–384 (1995)•
   Google Scholar
• Dowsett M, Detre S, Rowlands M, Grimshaw R Oestrogen formation in breast: clinical and biological importance.' Endocrinol. 150(Suppl.), S59-63 (1996).
   Google Scholar
• Cheung KL, Howell A, Robertson JF. Preoperative endocrine therapy for breast cancer. Endocr. Relat. Cancer7, 131–141 (2000).
   PubMedGoogle Scholar
• Hemsell DL, Grodin JM, Brenner PF, Siiteri PK, MacDonald PC. Plasma precursors of estrogen II. Correlation of the extent of conversion of plasma androstenedione to estrone with age. J. Clin. Endocrinot Meth. 38,476–479 (1974).
   Google Scholar
• Dowsett M. Rationale for the endocrine treatment of breast cancer. In: Endocrine Aspects of Breast Cancer. Dowsett M (Ed.), CRC Press, Camforth, UK, 11–24 (1992).
   Google Scholar
• Santen RJ. Long-term tamoxifen therapy: can an antagonist become an agonist?" Clin.Endocrind Meth. 81,2027-2029 (1996).
   Google Scholar
• •Highlights the importance of endocrine therapy in breast cancer treatment.
   Google Scholar
• Lee H, Jiang F, Wang Q et al. MEKK1 activation of human estrogen receptor alpha and stimulation of the agonistic activity of 4-hydroxytamoxifen in endometrial and ovarian cancer cells. Mot Endocrind 14, 1882–1896 (2000).
   PubMed Web of Science ®Google Scholar
• •Important study that shows the agonist activity of tamoxifen in other ER-driven cancers.
   Google Scholar
• Jones AL, Powles TJ, Treleaven JG et al. Haemostatic changes and thromboembolic risk during tamoxifen therapy in normal women. Br. J. Cancer 66,711 747 (1992).
   Google Scholar
• Bergman L, Beelen ML, Gallee MP et al. Risk and prognosis of endometrial cancer after tamoxifen for breast cancer. Comprehensive Cancer Centres' ALERT (Assessment of Liver and Endometrial Cancer Risk following Tamoxifen) Group. Lancet 356,881–887(2000).
   Google Scholar
• Ingle JN, Ahmann DL, Green SJ et id Randomized clinical trial of megestrol acetate versus tamoxifen in paramenopausal or castrated women with advanced breast cancer. Am." Clin. Oncol. 5, 155–160 (1982).
   Google Scholar
• MUSS HB, Wells HB, Paschold EH et al. Megestrol acetate versus tamoxifen in advanced breast cancer: 5-year analysis-a Phase III trial of the Piedmont Oncology Association.' Clin. Oncol. 6,1098-1106 (1988).
   Google Scholar
• Stuart NS, Warwick J, Blackledge GR et al. A randomised Phase III cross-over study of tamoxifen versus megestrol acetate in advanced and recurrent breast cancer. Eur. f Cancer 32A, 1888–1892 (1996).
   PubMed Web of Science ®Google Scholar
• Mouridsen H, Gershanovich M, Sun Y et aZ 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." Clin. Oncol. 19,2596-2606 (2001).
   Google Scholar
• ••A critical study that demonstrates thesuperiority of letrozole over the gold standard, tamoxifen, in the treatment of breast cancer in postmenopausal women.
   Google Scholar
• Lang M, Batzl C, Furet P et al. Structure- activity relationships and binding model of novel aromatase inhibitors. J. Steroid Biochem. Mot Biol. 44,421–428 (1993).
   PubMed Web of Science ®Google Scholar
• •Examines the structure activity relationships of the newer aromatase inhibitors.
   Google Scholar
• Murphy MJ, Jr. Molecular action and clinical relevance of aromatase inhibitors. Onco/ogist 3,129–130 (1998).
   PubMedGoogle Scholar
• Hausler A, Monnet G, Borer C, Bhatnagar AS. Evidence that corticosterone is not an obligatory intermediate in aldosterone biosynthesis in the rat adrenal." Steroid Biochem. 34,567-570 (1989)•
   Google Scholar
• Hausler A, Schenkel L, Krahenbuhl C, Monnet G, Bhatnagar AS. An in vitro method to determine the selective inhibition of estrogen biosynthesis by aromatase inhibitors.' Steroid Biochem. 33, 125–131 (1989).
   Google Scholar
• Thompson EA Jr, Siiteri PK. The involvement of human placental microsomal cytochrome P450 in aromatization. I Biol. Chem. 249,5373-5378 (1974).
   Google Scholar
• Miller WR, Dixon JM. Anti-aromatase agents: preclinical data and neoadjuvant therapy. (lin. Breast Cancer Suppl. 1\(Supp1.1), S9—S14 (2000).
   Google Scholar
• Bhatnagar AS, Brodie AM, Long BJ, Evans DB, Miller WR. Intracellular aromatase and its relevance to the pharmacological efficacy of aromatase inhibitors.' Steroid Biochem. Mot Biol. 76,199–202 (2001).
   Google Scholar
• ••Shows the superior in vitro potency ofletrozole compared with other aromatase inhibitors.
   Google Scholar
• Schieweck K, Bhatnagar AS, Batzl C, Lang M. Antitumor and endocrine effects of non-steroidal aromatase inhibitors on estrogen-dependent it mammary tumors.' Steroid Biochem. Mot Biol. 44,633–636 (1993).
   PubMed Web of Science ®Google Scholar
• Bhatnagar A, Häusler A, Schieweck K, Lang M, Bowman R Highly selective inhibition of estrogen biosynthesis by CGS 20267, a new non-steroidal aromatase inhibitor." Steroid Biochem. Malec. Biol. 37,1021-1027 (1990).
   Google Scholar
• Lu Q, Yue W, Wang J et at The effects of aromatase inhibitors and anti-estrogens in the nude mouse model. Breast Cancer Res. Treat. 50,63–71 (1998).
   PubMed Web of Science ®Google Scholar
• Lu Q Liu Y, Long BJ et at The effect of combining aromatase inhibitors with anti-estrogens on tumor growth in a nude mouse model for breast cancer. Breast Cancer Res. Treat. 57,183–192 (1999).
   Google Scholar
• Brodie A, Lu Q, Liu Yet al. Predinical studies using the intratumoral aromatase model for postmenopausal breast cancer. Onco/ogy 12,36–40 (1998).
   Google Scholar
• ••Examines the efficacy of letrozole versustamoxifen and a combination of both treatments on tumor regression using the intraturnoral aromatase model.
   Google Scholar
• Brodie A, Lu Q Yue W, Wang J, Liu Y. Intratumoral aromatase model: the effects of letrozole (CGS 20267). Breast Cancer Res. Treat. 49, S23-26 discussion S33-27 (1998).
   Google Scholar
• Yue W, Wang J, Savinov A, Brodie A. Effect of aromatase inhibitors on growth of mammary tumors in a nude mouse model. Cancer Res. 55,3073–3077 (1995).
   PubMed Web of Science ®Google Scholar
• Brodie A, Lu Q, Liu Y, Long B. Aromatase inhibitors and their antitumor effects in model systems. Endocr. Relat. Cancer 6, 205–210 (1999).
   PubMed Web of Science ®Google Scholar
• Lipton A, Bemers L, Harvey H et at Letrozole (CGS 20267): a Phase I study of a new potent oral aromatase inhibitor of breast cancer. Cancer 75,2132–2138 (1995)•
   Google Scholar
• •One of the first studies to examine the pharmacokinetics of letrozole.
   Google Scholar
• Sioufi A, Sandrenan N, Godbillon J et at 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).
   Google Scholar
• •Examines the pharmacokinetics of letrozole under different conditions.
   Google Scholar
• Colussi DM, Parisot CY, Lefevre GY. Plasma protein binding of letrozole, a new nonsteroidal aromatase enzyme inhibitor.' Clin. Pharmacol. 38,727–735 (1998).
   Google Scholar
• Trunet P, Mueller P, Bhatnagar A et al. Open dose-finding study of a new potent and selective non-steroidal aromatase inhibitor, CGS 20 267, in healthy male subjects.' Clin. Endo. Meth. 77, 319–323 (1993).
   Google Scholar
• Sioufi A, Gauducheau N, Pineau V et at Absolute bioavailability of letrozole in healthy postmenopausal women. Biop harm. Drug Divs. 18,779–789 (1997).
   PubMed Web of Science ®Google Scholar
• Bajetta E, Zilembo N, Dowsett M et al. Double-blind, randomised, rnulticentre endocrine trial comparing two letrozole doses, in postmenopausal breast cancer patients. Eur. j Cancer 35,208–213 (1999).
   PubMed Web of Science ®Google Scholar
• 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).
   PubMed Web of Science ®Google Scholar
• ••Examines the pharmacokinetic interactionbetween the coadministration of letrozole and tamoxifen.
   Google Scholar
• 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. Cancer 85,317–324 (2001).
   Google Scholar
• •Examines the pharmacokinetic interaction between another aromatase inhibitor, anastrozole, and tamoxifen.
   Google Scholar
• Ingle JN, Suman VJ, Johnson PA et at Evaluation of tamoxifen plus letrozole with assessment of pharmacokinetic interaction in postmenopausal women with metastatic breast cancer. Clin. Cancer Res. 5,1642–1649 (1999).
   PubMed Web of Science ®Google Scholar
• ••Examines the pharmacokinetic interactionbetween coadministered letrozole and tamoxifen.
   Google Scholar
• Iveson T, Smith I, Ahern J et al. Phase I study of the oral non-steroidal aromatase inhibitor CGS 20267 in healthy postmenopausal women. J. Clin. Endocrinot Meth. 77,324-331 (1993).
   Google Scholar
• •Examines the dose-response effect of letrozole on serum estrone and estradiol inhibition in postmenopausal women.
   Google Scholar
• Iveson TJ, Smith IE, Ahern J et al. Phase I study of the oral nonsteroidal aromatase inhibitor CGS 20267 in postmenopausal patients with advanced breast cancer. Cancer Res. 53,266–270 (1993).
   PubMed Web of Science ®Google Scholar
• Demers LM, Lipton A, Harvey HA et al. The efficacy of CGS 20267 in suppressing estrogen biosynthesis in patients with advanced stage breast cancer. J. Steroid Biochem. Mot Biol. 44,687-691 (1993).
   Google Scholar
• 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. 30,95-102 (1994).
   Google Scholar
• 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).
   Google Scholar
• Bisagni G, Cocconi G, Scaglione F et at Letrozole, a new oral non-steroidal aromatase inhibitor in treating postmenopausal patients with advanced breast cancer. A pilot study. Ann. Oncol. 7, 99–102 (1996).
   PubMed Web of Science ®Google Scholar
• Geisler J, Haynes B, Anker G, Dowsett M, Lonning PE. 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. Clin. Oncol 20, 751–757 (2002).
   Google Scholar
• •Crossover study that examines the effect of crossover from anastrozole to letrozole and vice versa on estrogen levels in postmenopausal women with breast cancer.
   Google Scholar
• Ingle JN, Johnson PA, Suman VJ et al. A randomized Phase II trial of two dosage levels of letrozole as third-line hormonal therapy for women with metastatic breast carcinoma. Cancer 80, 218–224 (1997).
   PubMed Web of Science ®Google Scholar
• 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 aminoglutethirnide in postmenopausal women with advanced breast cancer. Letrozole International Trial Group (AR/ BC3). Ann. Oncol 9, 639–645 (1998).
   Google Scholar
• ••One of the first studies to compareletrozole with standard second-line therapy for the treatment of breast cancer in postmenopausal women.
   Google Scholar
• Dombemowsky P, Smith I, Falkson Get 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.' Clin. Oncol 16, 453–461 (1998).
   Google Scholar
• ••One of the first studies to compareletrozole with standard second-line therapy for the treatment of breast cancer in postmenopausal women.
   Google Scholar
• 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).
   PubMed Web of Science ®Google Scholar
• ••Another study comparing the efficacy ofletrozole and megestrol acetate in the treatment of breast cancer in postmenopausal women. The dosing regimen for meg-astrol acetate has been altered from the trial by Dombernowsky.
   Google Scholar
• Mundy GR, Guise TA, Yoneda T. Biology of bone metastases. In: Diseases of the Breast. Harris JR (Ed.), Lippincott Williams & Wilkins, Philadelphia, 911–929 (2000).
   Google Scholar
• Mouridsen H, Sun Y, Gershanovich M et al. First-line therapy with letrozole (Femara°) for advanced breast cancer prolongs time to worsening of Karnofsky Performance status compared with tamoxifen. Breast Cancer Res. Treat. 69, 291. Abstract 458 (2001).
   Google Scholar
• •Compares the effect of letrozole on Karnofsky Performance status with that of tamoxifen.
   Google Scholar
• Finkelstein JB. FDA panel recommends two new cancer drugs for approval. J. Natl Cancer Inst. 93, 175–176 (2001).
   PubMed Web of Science ®Google Scholar
• Schwetz BA. Proposal for public disclosure about clinical trails. From the Food and Drug Administration. JAMA 285, 1146 (2001).
   Google Scholar
• Dixon JM, Love CD, Bellamy CO et al Letrozole as primary medical therapy for locally advanced and large operable breast cancer. Breast Cancer Res. Treat. 66, 191–199 (2001).
   PubMed Web of Science ®Google Scholar
• ••The first neoadjuvant study using letrozole2.5 or 10 mg.
   Google Scholar
• Eiermann W Paepke S, Appfelstaedt J et al. Preoperative treatment of postmenopausal breast cancer patients with letrozole: a randomized double-blind multicenter study. Ann. Oncol 12, 1527–1532 (2001).
   PubMedGoogle Scholar
• ••The first neoadjuvant study to comparethe efficacy of letrozole with tamoxifen.
   Google Scholar
• Berry DA, Muss HB, Thor AD et al HER-2/neu and p53 expression versus tamoxifen resistance in estrogen receptor-positive, node-positive breast cancer. J. Clin. Oncol 18, 3471–3479 (2000).
   Google Scholar
• Newby JC, Johnston SR, Smith IE, Dowsett M. Expression of epidermal growth factor receptor and c-erbB2 during the development of tamoxifen resistance in human breast cancer. Clin. Cancer Res. 3, 1643-1651(1997).
   Google Scholar
• Ellis MJ, Coop A, Singh B et al Letrozole is more effective neoadjuvant endocrine therapy than tamoxifen for ErbB-1- and/or ErbB-2-positive, estrogen receptor- positive primary breast cancer: evidence from a Phase III randomized trial." Clin. Oncol 19, 3808–3816 (2001).
   Google Scholar
• ••Compares the efficacy of letrozole andtamoxifen in the neoadjuvant setting in patients with varying ER and HER-2 status.
   Google Scholar
• Benz CC, Scott GK, Sarup JC et al. Estrogen-dependent, tamoxifen-resistant tumorigenic growth of MCF-7 cells transfected with HER2/neu. Breast Cancer Res. Treat. 24, 85–95 (1993).
   Google Scholar
• Nabholtz JM, Bun-Int 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. Arimidex Study Group. J. Clin. Oncol 18, 3758–3767 (2000).
   PubMed Web of Science ®Google Scholar
• 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." Clin. Oncol 18, 3748–3757 (2000).
   Google Scholar
• Kaufmann M, Bajetta E, Dirix LY et al Exemestane improves survival compared with megestrol acetate in postmenopausal patients with advanced breast cancer who have failed on tamoxifen. Results of a double-blind randomised Phase III trial. Eur. J. Cancer 36 (Suppl. 4), S86-87 (2000).
   Google Scholar
• Milla-Santos A, Milla L, Rallo L Phase III trial of anastrozole (AN) vs. tamoxifen (TAM) in postmenopausal (PM) patients (PTS) with hormone-dependent advanced breast cancer (ABC). Eur. J. Cancer 37\(Suppl. 5), 4. Abstract 0–11 (2001).
   Google Scholar
• Sidhu K, Fyles A, Eisenhauer E et al Phase II study of the aromatase inhibitor letrozole in endometrial carcinoma — NCIC CTG IND 126. Proc. Am. Soc. Clin. Oncol 20, Abstract 2520 (2001).
   Google Scholar
• •Examines the use of letrozole in the treatment of endometrial carcinoma.
   Google Scholar
• Maluf FC, Sabbatini P, Schwartz L, Xia J, Aghajanian C. Endometrial stromal sarcoma: objective response to letrozole. Gynecol Oncol 82, 384–388 (2001).
   PubMed Web of Science ®Google Scholar
• Smyth JF, Bowman A, Gabra H et al. CA 125 response and disease stabilization are associated with estrogen receptor expression in a Phase II trial of letrozole in ovarian cancer. Eur. J. Cancer 37\(Supp1.6), S276—S277 Abstract 1020 (2001).
   Google Scholar
• •Examines the use of letrozole in the treatment of ovarian cancer.
   Google Scholar
• Mitwally MF, Casper RE Use of an aromatase inhibitor for induction of ovulation in patients with an inadequate response to clomiphene citrate. Fertil Steril. 75, 305–309 (2001).
   PubMed Web of Science ®Google Scholar
• Elisaf MS, Bairaktari ET, Nicolaides C et al. Effect of letrozole on the lipid profile in postmenopausal women with breast cancer. Eur. Cancer 37, 1510–1513 (2001).
   PubMed Web of Science ®Google Scholar
• Dranitsaris G, Leung P, Mather J, Oza A. Cost-utility analysis of second-line hormonal therapy in advanced breast cancer: a comparison of two aromatase inhibitors to megestrol acetate. Anticancer Drugs 11, 591–601 (2000).
   PubMed Web of Science ®Google Scholar
• Nuijten M, Meester L, Waibel F, Wait S. Cost effectiveness of letrozole in the treatment of advanced breast cancer in postmenopausal women in the UK. Pharmacoeconomics 16, 379–397 (1999).
   PubMed Web of Science ®Google Scholar
• Dirix L, Piccart MJ, Lohrisch Get al. Efficacy of and tolerance to exemestane (E) versus tammdfen M in 1st line hormone therapy (HT) of postmenopausal metastatic breast cancer (MBC) patients (pts): a European Organization for the Research and Treatment of Cancer (EORTC Breast Group) Phase II trial with Pharmacia 8c Upjohn. Proc. Am. Soc. Clin. Oncol. 20, 29a. Abstract 114 (2001).
   Google Scholar
• Goss P, Grynpas M, Qi S, Hu H. The effects of exemestane on bone and lipids in the ovariectoinized rat. Breast Cancer Res. Treat. 69, 224. Abstract 132 (2001).
   Google Scholar
• 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 rnulticentre multinational study. Exemestane Study Group. Eur. I Cancer 33, 1767–1773 (1997).
   PubMed Web of Science ®Google Scholar