目的 探討新一代抗芳香化酶藥物依西美坦用于乳腺癌臨床治療的研究進展。方法 采用文獻回顧的方法,對目前國內、外有關依西美坦治療乳腺癌的研究進展加以分析與綜述。 結果 依西美坦是口服有效的芳香化酶滅活劑,其耐受性好、安全性高,在乳腺癌的輔助治療、新輔助治療及轉移性乳腺癌的治療中均取得較好療效。結論 依西美坦可能具有深遠的臨床應用潛力,隨著治療實踐的增多,將會進一步確定其在乳腺癌綜合治療中的作用和地位。
引用本文: 趙菲,姜軍. 依西美坦治療乳腺癌的臨床研究進展. 中國普外基礎與臨床雜志, 2006, 13(6): 741-744. doi: 復制
1. | 楊金巧. 乳腺癌的內分泌治療及研究進展 [J]. 中國普外基礎與臨床雜志, 2004; 11(1)∶12. |
2. | Jensen EV, Desombre ER, Hurst DJ, et al. Estrogen-receptor interactions in target tissues [J].Arch Anat Microsc Morphol Exp, 1967; 56(3)∶547. |
3. | Giudici D, Ornati G, Briatico G, et al. 6-Methylenandrosta-1, 4-diene-3, 17-dione (FCE 24304): a new irreversible aromatase inhibitor [J]. J Steroid Biochem, 1988; 30(1-6)∶391. |
4. | Higa GM. Exemestane: treatment of breast cancer with selective inactivation of aromatase [J].Am J Health Syst Pharm, 2002; 59(22)∶2194. |
5. | Brueggemeier RW. Overview of the pharmacology of the aromatase inactivator exemestane [J].Breast Cancer Res Treat, 2002; 74(2)∶177. |
6. | Buzdar AU, Robertson JF, Eiermann W, et al. An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane [J]. Cancer, 2002; 95(9)∶2006. |
7. | Marchetti P, Di-Rocco CZ, Ricevuto E, et al. Reducing breast cancer incidence in familial breast cancer: overlooking the present panorama [J]. Ann Oncol, 2004; 15(S1)∶127. |
8. | Goss P. Breast cancer prevention——clinical trials strategies involving aromatase inhibitors [J]. J Steroid Biochem Mol Biol, 2003; 86(3-5)∶487. |
9. | Coombes RC, Hall E, Gibson LJ, et al. A randomized trial of exemestane after two to three years of tamoxifen therapy in postmenopausal women with primary breast cancer [J]. N Engl J Med, 2004; 350(11)∶1081. |
10. | Piccart-Gebhart MJ. New stars in the sky of treatment for early breast cancer [J]. N Engl J Med, 2004; 350(11)∶1140. |
11. | Fisher BJ, Perera FE, Cooke AL, et al. Long-term follow-up of axillary node-positive breast cancer patients receiving adjuvant tamoxifen alone: patterns of recurrence [J].Int J Radiat Oncol Biol Phys, 1998; 42(1)∶117. |
12. | Gasparini G, Fanelli M, Boracchi P, et al. Behaviour of metastasis in relation to vascular index in patients with node-positive breast cancer treated with adjuvant tamoxifen [J]. Clin Exp Metastasis, 2000; 18(1)∶15. |
13. | Mamounas EP. Adjuvant exemestane therapy after 5 years of tamoxifen: rationale for the NSABP B-33 trial [J]. Oncology (Williston Park), 2001; 15(5 Suppl 7)∶35. |
14. | Francis P, Fleming G. Phase Ⅲ trial evaluating the role of ovarian function suppression and exemestane as adjuvant therapies for premenopausal women with endocrine-responsive breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶10. |
15. | Pagani O, Walley B. Phase Ⅲ trial evaluating the role of exemestane plus GnRH analogue as adjuvant therapy for premenopausal women with endocrine-responsive breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶11. |
16. | Pollow K. Pilot study of adjuvant exemestane combined with goserelin, with or without tibolone, for the treatment of receptor-positive, node-negtive, primary breast cancer in premenopausal women [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶14. |
17. | Mustacchi G. Study of primary hormonal therapy with exemestane in elderly women with operable or locally advanced breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶16. |
18. | Barnadas A. Neoadjuvant treatment with exemestane in elderly patients >65 years with T>3 cm; multicenter phaseⅡtrial [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶17. |
19. | Tubiana-Hulin M. PhaseⅡstudy evaluating objective response rate, histological response rate, and anti-aromatase activity of exemestane as neoadjuvant treatment for operable breaast cancer patients [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶22. |
20. | Hausmaninger H, Jakesz R. A multicenter pilot trial of exemestane as neoadjuvant therapy in postmenopausal women [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶23. |
21. | Wallwiener D. Study to evaluate safety and efficacy of exemestane administered as preoperative treatment for patients with primary breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶18. |
22. | Blohmer J. PhaseⅠ/Ⅱstudy to evaluate safefy and efficacy of exemestane administered concomitantly with weekly docetaxel as preoperative treatment for patients with primary breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶19. |
23. | Eirmann W. PhaseⅠ/Ⅱstudy to evaluate safefy and efficacy of exemestane administered concomitantly with weekly epirubicin as preoperaive treatment for patients with primary breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶20. |
24. | Ortmann O. PhaseⅠ/Ⅱstudy to evaluate safefy and efficacy of exemestane administered concomitantly with weekly pacilitaxel as preoperative treatment for patients with primary breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶21. |
25. | Cameron D, Miller W. A crossover study looking at exemestane and a nonsteroidal third-generation aromatase inhibitor [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶25. |
26. | Paridaens R, Dirix L, Lohrisch C, et al. Mature results of a randomized phase Ⅱ multicenter study of exemestane versus tamoxifen as first-line hormone therapy for postmenopausal women with metastatic breast cancer [J]. Ann Oncol, 2003; 14(9)∶1391. |
27. | Bertelli G, Garrone O, Merlano M, et al. Sequential treatment with exemestane and non-steroidal aromatase inhibitors in advanced breast cancer [J]. Oncology, 2005; 69(6)∶471. |
28. | Llombart A. Pilot, randomized, open, crossover, multicenter trial of sequential use of first-line exemestane followed by anastozole at progression compared with the opposite sequence in postmenopausal patients with hormone receptor-positive advanced breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶30. |
29. | Cameron D, Winer E. A pilot phase Ⅱ, open label, randomized, comparative study of exemestane vs anastrozole in postmenopausal breast cancer patients with visceral disease [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶31. |
30. | 樊青霞, 許 莉, 吳欣愛, 等. 依西美坦片治療絕經后晚期乳腺癌Ⅱ期臨床觀察 [J]. 河南腫瘤學雜志, 2002; 15(6)∶434. |
31. | 鄭弘宇, 黃 萍, 張其忠, 等. 依西美坦片治療絕經后晚期乳腺癌Ⅱ期臨床研究 [J]. 實用醫學雜志, 2002; 18(10)∶1108. |
32. | 黎治平, 鐘 睿, 馬行天, 等. 依西美坦治療絕經后婦女晚期乳腺癌的臨床療效觀察 [J]. 實用癌癥雜志, 2002; 17(5)∶542. |
33. | Fisher B, Redmond C, Brown A, et al. Adjuvant chemotherapy with and without tamoxifen in the treatment of primary breast cancer: Five-year results from the NSABP trial [J]. J Clin Oncol, 1986; 4(4)∶459. |
34. | Fisher B, Wickerham DL, Redmond C, et al. Increased benefit from addition of adriamycin to adjuvant therapy for stage Ⅱ breast cancer: Results from NSABP protocols B-11 and B-12 [J]. Pro Am So Clin Oncol, 1987; 6(1)∶62. |
35. | Fisher B, Redmond C, Legault-Poisson S, et al. Postoperative chemotherapy and tamoxifen compared with tamoxifen alone in the treatment of positive-node breast cancer patients aged 50 years and older with tumor responsive to tamoxifen: Results from NSABP B-16 [J]. J Clin Oncol, 1990; 8(6)∶1005. |
36. | Elling D. Randomized phase Ⅱ/Ⅲ study of exemestane (Aromasin) vs.docetaxel (Taxotere) vs.Aromasin/Taxotere for the treatment of low-risk advanced breast cancer (ATax) [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶32. |
37. | Kohler U, Hilfrich J. Exemestane in combination with fractionated weekly epirubicin or paclitaxel for the treatment of advanced breast cancer (ACEPT-1) [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶33. |
38. | Bernado G. Treatment of elderly patients with metastatic breast cancer with chemohormonal therapy with oral idarubicin and exemestane [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶36. |
39. | Alba E. Multicenter, pilot, phase Ⅱ trail of hormonochemotherapy of advanced breast cancer with fluorouracil, epirubicin, and cyclophosphamide (FEC) and exemestane administered simultaneously as first-line therapy [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶41. |
- 1. 楊金巧. 乳腺癌的內分泌治療及研究進展 [J]. 中國普外基礎與臨床雜志, 2004; 11(1)∶12.
- 2. Jensen EV, Desombre ER, Hurst DJ, et al. Estrogen-receptor interactions in target tissues [J].Arch Anat Microsc Morphol Exp, 1967; 56(3)∶547.
- 3. Giudici D, Ornati G, Briatico G, et al. 6-Methylenandrosta-1, 4-diene-3, 17-dione (FCE 24304): a new irreversible aromatase inhibitor [J]. J Steroid Biochem, 1988; 30(1-6)∶391.
- 4. Higa GM. Exemestane: treatment of breast cancer with selective inactivation of aromatase [J].Am J Health Syst Pharm, 2002; 59(22)∶2194.
- 5. Brueggemeier RW. Overview of the pharmacology of the aromatase inactivator exemestane [J].Breast Cancer Res Treat, 2002; 74(2)∶177.
- 6. Buzdar AU, Robertson JF, Eiermann W, et al. An overview of the pharmacology and pharmacokinetics of the newer generation aromatase inhibitors anastrozole, letrozole, and exemestane [J]. Cancer, 2002; 95(9)∶2006.
- 7. Marchetti P, Di-Rocco CZ, Ricevuto E, et al. Reducing breast cancer incidence in familial breast cancer: overlooking the present panorama [J]. Ann Oncol, 2004; 15(S1)∶127.
- 8. Goss P. Breast cancer prevention——clinical trials strategies involving aromatase inhibitors [J]. J Steroid Biochem Mol Biol, 2003; 86(3-5)∶487.
- 9. Coombes RC, Hall E, Gibson LJ, et al. A randomized trial of exemestane after two to three years of tamoxifen therapy in postmenopausal women with primary breast cancer [J]. N Engl J Med, 2004; 350(11)∶1081.
- 10. Piccart-Gebhart MJ. New stars in the sky of treatment for early breast cancer [J]. N Engl J Med, 2004; 350(11)∶1140.
- 11. Fisher BJ, Perera FE, Cooke AL, et al. Long-term follow-up of axillary node-positive breast cancer patients receiving adjuvant tamoxifen alone: patterns of recurrence [J].Int J Radiat Oncol Biol Phys, 1998; 42(1)∶117.
- 12. Gasparini G, Fanelli M, Boracchi P, et al. Behaviour of metastasis in relation to vascular index in patients with node-positive breast cancer treated with adjuvant tamoxifen [J]. Clin Exp Metastasis, 2000; 18(1)∶15.
- 13. Mamounas EP. Adjuvant exemestane therapy after 5 years of tamoxifen: rationale for the NSABP B-33 trial [J]. Oncology (Williston Park), 2001; 15(5 Suppl 7)∶35.
- 14. Francis P, Fleming G. Phase Ⅲ trial evaluating the role of ovarian function suppression and exemestane as adjuvant therapies for premenopausal women with endocrine-responsive breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶10.
- 15. Pagani O, Walley B. Phase Ⅲ trial evaluating the role of exemestane plus GnRH analogue as adjuvant therapy for premenopausal women with endocrine-responsive breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶11.
- 16. Pollow K. Pilot study of adjuvant exemestane combined with goserelin, with or without tibolone, for the treatment of receptor-positive, node-negtive, primary breast cancer in premenopausal women [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶14.
- 17. Mustacchi G. Study of primary hormonal therapy with exemestane in elderly women with operable or locally advanced breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶16.
- 18. Barnadas A. Neoadjuvant treatment with exemestane in elderly patients >65 years with T>3 cm; multicenter phaseⅡtrial [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶17.
- 19. Tubiana-Hulin M. PhaseⅡstudy evaluating objective response rate, histological response rate, and anti-aromatase activity of exemestane as neoadjuvant treatment for operable breaast cancer patients [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶22.
- 20. Hausmaninger H, Jakesz R. A multicenter pilot trial of exemestane as neoadjuvant therapy in postmenopausal women [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶23.
- 21. Wallwiener D. Study to evaluate safety and efficacy of exemestane administered as preoperative treatment for patients with primary breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶18.
- 22. Blohmer J. PhaseⅠ/Ⅱstudy to evaluate safefy and efficacy of exemestane administered concomitantly with weekly docetaxel as preoperative treatment for patients with primary breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶19.
- 23. Eirmann W. PhaseⅠ/Ⅱstudy to evaluate safefy and efficacy of exemestane administered concomitantly with weekly epirubicin as preoperaive treatment for patients with primary breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶20.
- 24. Ortmann O. PhaseⅠ/Ⅱstudy to evaluate safefy and efficacy of exemestane administered concomitantly with weekly pacilitaxel as preoperative treatment for patients with primary breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶21.
- 25. Cameron D, Miller W. A crossover study looking at exemestane and a nonsteroidal third-generation aromatase inhibitor [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶25.
- 26. Paridaens R, Dirix L, Lohrisch C, et al. Mature results of a randomized phase Ⅱ multicenter study of exemestane versus tamoxifen as first-line hormone therapy for postmenopausal women with metastatic breast cancer [J]. Ann Oncol, 2003; 14(9)∶1391.
- 27. Bertelli G, Garrone O, Merlano M, et al. Sequential treatment with exemestane and non-steroidal aromatase inhibitors in advanced breast cancer [J]. Oncology, 2005; 69(6)∶471.
- 28. Llombart A. Pilot, randomized, open, crossover, multicenter trial of sequential use of first-line exemestane followed by anastozole at progression compared with the opposite sequence in postmenopausal patients with hormone receptor-positive advanced breast cancer [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶30.
- 29. Cameron D, Winer E. A pilot phase Ⅱ, open label, randomized, comparative study of exemestane vs anastrozole in postmenopausal breast cancer patients with visceral disease [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶31.
- 30. 樊青霞, 許 莉, 吳欣愛, 等. 依西美坦片治療絕經后晚期乳腺癌Ⅱ期臨床觀察 [J]. 河南腫瘤學雜志, 2002; 15(6)∶434.
- 31. 鄭弘宇, 黃 萍, 張其忠, 等. 依西美坦片治療絕經后晚期乳腺癌Ⅱ期臨床研究 [J]. 實用醫學雜志, 2002; 18(10)∶1108.
- 32. 黎治平, 鐘 睿, 馬行天, 等. 依西美坦治療絕經后婦女晚期乳腺癌的臨床療效觀察 [J]. 實用癌癥雜志, 2002; 17(5)∶542.
- 33. Fisher B, Redmond C, Brown A, et al. Adjuvant chemotherapy with and without tamoxifen in the treatment of primary breast cancer: Five-year results from the NSABP trial [J]. J Clin Oncol, 1986; 4(4)∶459.
- 34. Fisher B, Wickerham DL, Redmond C, et al. Increased benefit from addition of adriamycin to adjuvant therapy for stage Ⅱ breast cancer: Results from NSABP protocols B-11 and B-12 [J]. Pro Am So Clin Oncol, 1987; 6(1)∶62.
- 35. Fisher B, Redmond C, Legault-Poisson S, et al. Postoperative chemotherapy and tamoxifen compared with tamoxifen alone in the treatment of positive-node breast cancer patients aged 50 years and older with tumor responsive to tamoxifen: Results from NSABP B-16 [J]. J Clin Oncol, 1990; 8(6)∶1005.
- 36. Elling D. Randomized phase Ⅱ/Ⅲ study of exemestane (Aromasin) vs.docetaxel (Taxotere) vs.Aromasin/Taxotere for the treatment of low-risk advanced breast cancer (ATax) [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶32.
- 37. Kohler U, Hilfrich J. Exemestane in combination with fractionated weekly epirubicin or paclitaxel for the treatment of advanced breast cancer (ACEPT-1) [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶33.
- 38. Bernado G. Treatment of elderly patients with metastatic breast cancer with chemohormonal therapy with oral idarubicin and exemestane [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶36.
- 39. Alba E. Multicenter, pilot, phase Ⅱ trail of hormonochemotherapy of advanced breast cancer with fluorouracil, epirubicin, and cyclophosphamide (FEC) and exemestane administered simultaneously as first-line therapy [C]. Exemestane: Clinical Trial of Breast Cancer——Compilation of the 8th International St. Gallen Breast Cancer Conference, 2003∶41.