Table 1.

Experimental data sets of phase I studies assessing the pharmacokinetics of rivaroxaban in healthy male adult subjects

Study	Topic	Main outcome
Study A	Mass balance and safety [37]	Rivaroxaban and its metabolites were eliminated via renal (66 %) and biliary/faecal routes (28 %)
Study B	Absolute bioavailability [32]	Compared with a 1 mg IV dose, under fasted conditions the bioavailability of rivaroxaban 5 mg was complete and was 66 % for rivaroxaban 20 mg. Bioavailability of rivaroxaban 20 mg was 59 % relative to the 5 mg dose
Study C	Pharmacokinetics across a wide dose range [16]	Rivaroxaban had well-defined pharmacokinetic characteristics across doses of 1.25–80 mg administered as oral solution or tablet
Study D	Absorption from proximal and distal small bowel and ascending colon	The relative bioavailability of rivaroxaban depends on the site of absorption along the gastrointestinal tract and is poorest in the ascending colon
Study E	Food effect on pharmacokinetics of two 5 mg tablets	Compared with fasted conditions, mean t max, mean AUC and mean C max of rivaroxaban 10 mg were increased when taken with food
Study F	Food effect on pharmacokinetics of four 5 mg tablets or one 20 mg tablet	There were no pharmacokinetic differences between the two dosing regimens or between two types of meals. Mean t max, mean AUC and mean C max were significantly higher after food
Study G	Food effect on pharmacokinetics of one 10 mg tablet or one 20 mg tablet	Bioavailability of rivaroxaban 10 mg was independent of food Bioavailability of rivaroxaban 20 mg was similar when taken with food and lower when taken without food
Study H	Food effect on pharmacokinetics of 10 mg and 20 mg oral solution	Bioavailability of rivaroxaban 10 mg was independent of food Bioavailability of rivaroxaban 20 mg was similar when taken with food and lower when taken without food

AUC area under the plasma concentration–time curve, C _max maximum (peak) plasma drug concentration, IV intravenous, t _max time to C _max