title: A randomized controlled non-inferiority study comparing the antiemetic effect between intravenous granisetron and oral azasetron based on estimated 5-HT3 receptor occupancy.
abstract: BACKGROUND
  The acute antiemetic effect was compared between oral azasetron and intravenous granisetron based on the 5-hydroxytryptamine(3) (5-HT(3)) receptor occupancy theory.
  
  
  METHODS
  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.
  
  
  RESULTS
  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%).
  
  
  CONCLUSIONS
  Oral azasetron was found to be non-inferior to intravenous granisetron in the acute antiemetic effect against moderately emetogenic chemotherapy.
authors.affiliation: Second Department of Internal Medicine, Graduate School of Medicine, Gifu University, Gifu, Japan..
authors.forename: Junki
authors.initials: J
authors.lastname: Endo
authors.forename: Hirotoshi
authors.initials: H
authors.lastname: Iihara
authors.forename: Maya
authors.initials: M
authors.lastname: Yamada
authors.forename: Koumei
authors.initials: K
authors.lastname: Yanase
authors.forename: Fumihiko
authors.initials: F
authors.lastname: Kamiya
authors.forename: Fumitaka
authors.initials: F
authors.lastname: Ito
authors.forename: Norihiko
authors.initials: N
authors.lastname: Funaguchi
authors.forename: Yasushi
authors.initials: Y
authors.lastname: Ohno
authors.forename: Shinya
authors.initials: S
authors.lastname: Minatoguchi
authors.forename: Yoshinori
authors.initials: Y
authors.lastname: Itoh
mesh_terms: D000284:Administration, Oral; D000328:Adult; D000368:Aged; D000369:Aged, 80 and over; D000932:Antiemetics / Q000008:administration & dosage* / Q000493:pharmacokinetics; D000971:Antineoplastic Combined Chemotherapy Protocols / Q000009:adverse effects / Q000627:therapeutic use; D019086:Bridged Bicyclo Compounds, Heterocyclic / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016190:Carboplatin / Q000008:administration & dosage / Q000009:adverse effects; D005260:Female; D017829:Granisetron / Q000008:administration & dosage* / Q000493:pharmacokinetics; D006801:Humans; D007275:Injections, Intravenous; D008175:Lung Neoplasms / Q000097:blood / Q000188:drug therapy* / Q000378:metabolism*; D008297:Male; D008875:Middle Aged; D010078:Oxazines / Q000008:administration & dosage* / Q000493:pharmacokinetics; D044406:Receptors, Serotonin, 5-HT3 / Q000097:blood / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000008:administration & dosage
chemical_list: D000932:Antiemetics; D019086:Bridged Bicyclo Compounds, Heterocyclic; D016190:Carboplatin; D017829:Granisetron; D010078:Oxazines; D044406:Receptors, Serotonin, 5-HT3; D012702:Serotonin Antagonists; C070671:azasetron