Background: Tegaserod (HTF 919) is a selective 5-HT4 receptor partial agoni
st in development for the treatment of irritable bowel syndrome.
Aim: This study aimed to assess the effect of age and gender on the single-
dose pharmacokinetics of tegaserod.
Methods: In a parallel-group, open-label study, a single dose of tegaserod
(12 mg) was administered to four groups of healthy young male, young female
, elderly male and elderly female subjects (n = 10 per group). Blood sample
s were collected from 0 to 24 h postdose. Non-compartmental pharmacokinetic
s evaluation and statistical analysis (ANOVA and Wilcoxon signed ranks test
for t(max)) were performed.
Results: Tegaserod was well tolerated in all groups. There was no effect of
age or gender on t(max) and C-max. Gender did not affect AUC(0-infinity) a
nd AUC(0-tz); there was a statistically significant effect of age on these
parameters. AUC(0-infinity) and AUC(0-tz) in the elderly were greater than
in the young (AUC(0-infinity) ratio 1.37, P < 0.001; AUC(0-tz) ratio 1.23,
P = 0.029). This increase in exposure is judged not to be clinically releva
nt because it is within the variability in the pharmacokinetics parameters
of tegaserod and because the dose-response relationship of tegaserod is rel
Conclusions: No dose adjustment for age or gender is recommended in tegaser