Dowsett M
Royal Marsden Hospital, London, UK.
Breast Cancer Res Treat. 1998;49 Suppl 1:S39-44; discussion S73-7. doi: 10.1023/a:1006088405721.
A definition of the theoretical components of an ideal aromatase inhibitor is developed, one aspect of which is completeness of enzyme inhibition. The three triazole inhibitors, letrozole, vorozole and anastrozole all inhibit whole body aromatisation by > 96% at their clinically used doses and vorozole and letrozole were more effective in Phase III clinical trials than aminoglutethimide (250 mg bd) which achieves < 90% inhibition. The possibility is considered that the apparent small differences between the triazoles may be associated with differences in clinical effectiveness. These new compounds merit consideration for studies of breast cancer prevention.
对理想芳香化酶抑制剂的理论组成部分进行了定义，其中一个方面是酶抑制的完整性。三种三唑类抑制剂，来曲唑、伏罗唑和阿那曲唑，在临床使用剂量下均能使全身芳香化作用抑制率超过96%，并且在III期临床试验中，伏罗唑和来曲唑比氨鲁米特（每日两次，每次250mg）更有效，后者的抑制率小于90%。人们认为三唑类药物之间明显的微小差异可能与临床疗效差异有关。这些新化合物值得考虑用于乳腺癌预防研究。
