Kerbrat P, Lefeuvre C
Département d'oncologie médicale, Centre Eugène-Marquis, rue de la Bataille-Flandres-Dunkerque, CS 44229, 35042 Rennes Cedex, France.
Bull Cancer. 2000 Dec;87 Spec No:31-39.
To increase the therapeutic index of second line hormonal treatment of breast cancer, new aromatase inhibitors have been synthetized; they belong to two groups: type I (formestane and exemestane) are steroidal irreversible and specific inhibitors, type II (anastrozole, letrozole and vorozole) are non steroidal reversible inhibitors, interfering with the aromatase heme. Several phase II and III trials demonstrated that these drugs are, at least, as active as aminoglutethimid or progestins in second line treatment, and are less toxic. Recently, an identical activity have been observed for anastrozole and tamoxifen in first line. In metastatic and adjuvant settings, large trials are ongoing to clarify the exact value of these drugs.
为提高乳腺癌二线激素治疗的治疗指数,已合成了新型芳香化酶抑制剂;它们分为两类:I型(福美司坦和依西美坦)是甾体类不可逆特异性抑制剂,II型(阿那曲唑、来曲唑和伏氯唑)是非甾体类可逆抑制剂,可干扰芳香化酶血红素。多项II期和III期试验表明,这些药物在二线治疗中至少与氨鲁米特或孕激素活性相当,且毒性较小。最近,在一线治疗中观察到阿那曲唑和他莫昔芬具有相同的活性。在转移性和辅助治疗环境中,正在进行大型试验以阐明这些药物的确切价值。