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Apixaban unaffected by gastric acid suppressant

Histamine H2-receptor antagonist famotidine does not affect the pharmacokinetics of apixaban in healthy subjects, suggesting that apixaban can be administered without regard to coadministration of gastric acid modifiers, according to a study1 published recently in Clinical Pharmacology: Advances and Applications.

This two-period, two-treatment crossover study randomised 18 healthy subjects to receive a single oral dose of apixaban 10 mg with and without a single oral dose of famotidine 40 mg administered three hours before dosing with apixaban. Plasma apixaban concentrations were measured up to 60 hours post-dose and pharmacokinetic parameters were calculated.

Famotidine did not affect maximum apixaban plasma concentration (Cmax) or area under the plasma concentration-time curve from zero to infinite time (AUC∞). Point estimates for ratios of geometric means with and without famotidine were close to unity for Cmax (0.978) and AUC∞ (1.007), and 90% confidence intervals were entirely contained within the 80%–125% no-effect interval. Administration of apixaban alone and with famotidine was well tolerated.

These findings are consistent with the physicochemical properties of apixaban (lack of an ionizable group and pH-independent solubility), say the authors. Given that famotidine is also an inhibitor of the human organic cation transporter (hOCT), these results indicate that apixaban pharmacokinetics are not influenced by hOCT uptake transporter inhibitors, they assert.


1. Upreti VV, Song Y, Wang J, et al. Effect of famotidine on the pharmacokinetics of apixaban, an oral direct factor Xa inhibitor. Clin Pharmacol Adv Appl 2013:5;59–66.

Published on: April 26, 2013

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