Wiseman L R, Spencer C M
Adis International Limited, Auckland, New Zealand.
Drugs Aging. 1997 Sep;11(3):245-50; discussion 251-2. doi: 10.2165/00002512-199711030-00007.
Vorozole is a triazole derivative which binds to the cytochrome P450 moiety of aromatase, thus causing reversible inhibition of the enzyme. Plasma estradiol levels are reduced by about 90% in postmenopausal women treated with vorozole. Phase II clinical studies found vorozole to be an effective agent for the treatment of postmenopausal women with advanced breast cancer, achieving objective responses in up to 35% of patients. In 2 large phase III studies, vorozole 2.5 mg/day demonstrated favourable clinical efficacy compared with aminoglutethimide and megestrol. Vorozole improved patients' quality of life to a greater extent than aminoglutethimide. Clinical trials to date indicate that the tolerability of vorozole is better than that of aminoglutethimide. Vorozole also appears to be at least as well tolerated as megestrol (although inappropriate bodyweight gain is more common in megestrol recipients). The most common adverse events with vorozole are hot flushes, and nausea, which are generally mild in severity.
伏罗唑是一种三唑衍生物，它与芳香化酶的细胞色素P450部分结合，从而导致该酶的可逆性抑制。接受伏罗唑治疗的绝经后女性血浆雌二醇水平降低约90%。II期临床研究发现，伏罗唑是治疗绝经后晚期乳腺癌女性的有效药物，高达35%的患者获得客观缓解。在两项大型III期研究中，与氨鲁米特和甲地孕酮相比，伏罗唑2.5毫克/天显示出良好的临床疗效。伏罗唑比氨鲁米特更大程度地改善了患者的生活质量。迄今为止的临床试验表明，伏罗唑的耐受性优于氨鲁米特。伏罗唑的耐受性似乎也至少与甲地孕酮一样好（尽管接受甲地孕酮的患者体重增加不当更为常见）。伏罗唑最常见的不良事件是潮热和恶心，一般严重程度较轻。
