RT Journal Article SR Electronic T1 A Randomized Controlled Non-inferiority Study Comparing the Antiemetic Effect between Intravenous Granisetron and Oral Azasetron Based on Estimated 5-HT3 Receptor Occupancy JF Anticancer Research JO Anticancer Res FD International Institute of Anticancer Research SP 3939 OP 3947 VO 32 IS 9 A1 ENDO, JUNKI A1 IIHARA, HIROTOSHI A1 YAMADA, MAYA A1 YANASE, KOUMEI A1 KAMIYA, FUMIHIKO A1 ITO, FUMITAKA A1 FUNAGUCHI, NORIHIKO A1 OHNO, YASUSHI A1 MINATOGUCHI, SHINYA A1 ITOH, YOSHINORI YR 2012 UL http://ar.iiarjournals.org/content/32/9/3939.abstract AB Background: The acute antiemetic effect was compared between oral azasetron and intravenous granisetron based on the 5-hydroxytryptamine3 (5-HT3) receptor occupancy theory. Patients and Methods: Receptor occupancy was estimated from reported data on plasma concentrations and affinity constants to 5-HT3 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. Results: Azasetron exhibited the highest 5-HT3 receptor occupancy among various first-generation 5-HT3 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%). Conclusion: Oral azasetron was found to be non-inferior to intravenous granisetron in the acute antiemetic effect against moderately emetogenic chemotherapy.