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.

PATIENTS AND 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%).

CONCLUSION:

Oral azasetron was found to be non-inferior to intravenous granisetron in the acute antiemetic effect against moderately emetogenic chemotherapy.

• Authors: Junki Endo, Hirotoshi Iihara, Maya Yamada, Koumei Yanase, Fumihiko Kamiya, Fumitaka Ito, Norihiko Funaguchi, Yasushi Ohno, Shinya Minatoguchi, Yoshinori Itoh
• Journal: Anticancer research (Anticancer Res) Vol. 32 Issue 9 Pg. 3939-47 (Sep 2012) ISSN: 1791-7530 [Electronic] Greece
• PMID: 22993341 (Publication Type: Journal Article, Randomized Controlled Trial)

Chemical References

• Antiemetics
• Bridged Bicyclo Compounds, Heterocyclic
• Oxazines
• Receptors, Serotonin, 5-HT3
• Serotonin Antagonists
• azasetron
• Carboplatin
• Granisetron

Topics

• Administration, Oral
• Adult
• Aged
• Aged, 80 and over
• Antiemetics (administration & dosage, pharmacokinetics)
• Antineoplastic Combined Chemotherapy Protocols (adverse effects, therapeutic use)
• Bridged Bicyclo Compounds, Heterocyclic (administration & dosage, pharmacokinetics)
• Carboplatin (administration & dosage, adverse effects)
• Female
• Granisetron (administration & dosage, pharmacokinetics)
• Humans
• Injections, Intravenous
• Lung Neoplasms (blood, drug therapy, metabolism)
• Male
• Middle Aged
• Oxazines (administration & dosage, pharmacokinetics)
• Receptors, Serotonin, 5-HT3 (blood, metabolism)
• Serotonin Antagonists (administration & dosage)