Santner S J, Rosen H, Osawa Y, Santen R J
J Steroid Biochem. 1984 Jun;20(6A):1239-42. doi: 10.1016/0022-4731(84)90151-1.
In vitro p450 spectral data suggested that combinations of aromatase inhibitors might produce enhanced biologic effects. If correct, two clinically available aromatase inhibitors, aminoglutethimide (AG) and testololactone (TL) could potentially be given together at lower than usual dosage with reduction of patient side effects and preservation of aromatase inhibition. Using a [3H]water aromatase assay and a placental microsomal system, AG and TL were tested individually and in combination over their respective dose response ranges. Additive effects of these two compounds were observed. Another inhibitor, 4-hydroxyandrostenedione, given with AG produced similar additive inhibition. These data provide a basis for a future trial of AG and TL in combination in patients with breast carcinoma.
体外细胞色素P450光谱数据表明，芳香化酶抑制剂的联合使用可能会产生增强的生物学效应。如果这一结论正确，那么两种临床可用的芳香化酶抑制剂，氨鲁米特（AG）和睾内酯（TL），有可能以低于常规剂量联合使用，从而减少患者的副作用并维持对芳香化酶的抑制作用。采用[3H]水芳香化酶检测法和胎盘微粒体系统，分别对AG和TL在各自剂量反应范围内进行了单独及联合测试。观察到这两种化合物具有相加作用。另一种抑制剂4-羟基雄烯二酮与AG联合使用时也产生了类似的相加抑制作用。这些数据为未来在乳腺癌患者中联合使用AG和TL进行试验提供了依据。
