Research ArticleClinical Studies

A Randomized Controlled Non-inferiority Study Comparing the Antiemetic Effect between Intravenous Granisetron and Oral Azasetron Based on Estimated 5-HT3 Receptor Occupancy

JUNKI ENDO, HIROTOSHI IIHARA, MAYA YAMADA, KOUMEI YANASE, FUMIHIKO KAMIYA, FUMITAKA ITO, NORIHIKO FUNAGUCHI, YASUSHI OHNO, SHINYA MINATOGUCHI and YOSHINORI ITOH
Anticancer Research September 2012, 32 (9) 3939-3947;

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Figures

  • Figure 1.
    Figure 1.

    Time course of 5-hydroxytryptamine 3 (5-HT3) receptor occupancy after administration of various injectable (A) and oral (B) 5-HT3 receptor antagonists. 5-HT3 receptor occupancy was calculated as 100×Cplasma-free/(Ki+Cplasma-free), where Ki is the inhibition constant of each antagonist for 5-HT3 receptor binding and Cplasma-free is plasma concentration of unbound 5-HT3 receptor antagonist.

  • Figure 2.
    Figure 2.

    Correlation between 5-hydroxytryptamine 3 (5-HT3) receptor occupancy estimated at 12 h (A) and 24 h (B) after treatment and the control of emesis after treatment with injectable and oral formulations of 5-HT3 antagonists in patients undergoing cisplatin-containing cancer chemotherapy. Pharmacokinetic, physicochemical and clinical data were obtained from the Ethical Drug Package Insert of each 5-HT3 receptor antagonist. The 5-HT3 receptor occupancy was calculated from the Ki (inhibition constant) and plasma concentration of each unbound 5-HT3 antagonist. Control of emesis represents no emesis and no rescue treatment during the first 24 h after chemotherapy. GRN, Granisetron; AZA, azasetron; OND, ondansetrron; RAM, ramosetron; TRP, tropisetron; IND, indisetrron.

  • Figure 3.
    Figure 3.

    Comparison of the time course in the complete protection from nausea (A) and vomiting (B) by oral azasetron and intravenous granisetron in patients with lung cancer undergoing the first course of moderately emetogenic cancer chemotherapy.

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A Randomized Controlled Non-inferiority Study Comparing the Antiemetic Effect between Intravenous Granisetron and Oral Azasetron Based on Estimated 5-HT3 Receptor Occupancy
JUNKI ENDO, HIROTOSHI IIHARA, MAYA YAMADA, KOUMEI YANASE, FUMIHIKO KAMIYA, FUMITAKA ITO, NORIHIKO FUNAGUCHI, YASUSHI OHNO, SHINYA MINATOGUCHI, YOSHINORI ITOH
Anticancer Research Sep 2012, 32 (9) 3939-3947;
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