Second Department of Internal Medicine, Graduate School of Medicine, Gifu University, Gifu, Japan..
Anticancer Res. 2012 Sep;32(9):3939-47.
The acute antiemetic effect was compared between oral azasetron and intravenous granisetron based on the 5-hydroxytryptamine(3) (5-HT(3)) receptor occupancy theory.
Receptor occupancy was estimated from reported data on plasma concentrations and affinity constants to 5-HT(3) receptor. A randomized non-inferiority study comparing acute antiemetic effects between oral azasetron and intravenous granisetron was performed in 105 patients receiving the first course of carboplatin-based chemotherapy for lung cancer.
Azasetron exhibited the highest 5-HT(3) receptor occupancy among various first-generation 5-HT(3) antagonists. The complete response to oral azasetron was shown to be non-inferior to that of intravenous granisetron, in which the risk difference was 0.0004 (95% confidence interval: -0.0519-0.0527). The lower limit of the confidence intervals did not exceed the negative non-inferiority margin (-0.1). The complete response during the overall period was not different (68% versus 67%).
Oral azasetron was found to be non-inferior to intravenous granisetron in the acute antiemetic effect against moderately emetogenic chemotherapy.
基于 5-羟色胺（3）（5-HT（3））受体占有率理论，比较了口服阿扎司琼和静脉注射格拉司琼的急性止吐作用。
根据 5-HT（3）受体的血浆浓度和亲和力常数的报告数据，估算了受体占有率。对 105 例接受基于卡铂的肺癌首次化疗的患者进行了一项随机非劣效性研究，比较了口服阿扎司琼和静脉注射格拉司琼的急性止吐效果。
阿扎司琼在第一代 5-HT（3）拮抗剂中表现出最高的 5-HT（3）受体占有率。口服阿扎司琼的完全缓解与静脉注射格拉司琼相当，风险差异为 0.0004（95%置信区间：-0.0519-0.0527）。置信区间的下限未超过负非劣效性边界（-0.1）。整个期间的完全缓解率无差异（68%对 67%）。
在中度致吐性化疗的急性止吐作用方面，口服阿扎司琼与静脉注射格拉司琼相当。
