OBJECTIVE: To investigate the influence of @entity955 ( @entity955 ) on the pharmacokinetic (PK) properties of the oral direct @entity556 inhibitor @entity24772 and its active form, @entity18422 . METHODS: In an open study, 12 @entity1 with persistent @entity955 and 12 age- and gender-matched, healthy control subjects received a 10-min intravenous (i.v.) infusion of 2.66 mg @entity18422 followed by oral @entity24772 , 36 mg twice daily, for the subsequent five study days. Plasma and urine samples for PK analyses were collected after i.v. and single and repeated oral dosing. RESULTS: The oral absorption of @entity24772 was rapid, and maximum plasma concentrations of @entity24772 (Cmax) were achieved at about 1 h post-dosing. There were no differences between @entity955 @entity1 and controls for the area under the plasma concentration versus time curve, Cmax, half-life (t1/2), or bioavailability (F) of @entity18422 after oral dosing with @entity24772 . The Cmax of @entity18422 , formed by the rapid bioconversion of @entity24772 , occurred approximately 3 h post-dosing. The geometric means of the t1/2 for @entity18422 were 4.0 h and 4.2 h for the first and last doses, respectively, in @entity1 , and 3.5 h and 3.7 h, respectively, in controls. Geometric means of F of @entity18422 following oral administration of @entity24772 were 22% and 24% for the first and last doses, respectively, in @entity1 and 21% and 23%, respectively, in controls. Approximately 80% of the i.v. dose of @entity18422 was excreted in urine in @entity1 and in controls. CONCLUSION: The PK properties of oral @entity24772 and i.v. @entity18422 in elderly @entity1 with @entity955 are consistent with those in matched, healthy controls.

Consistent pharmacokinetics of the oral direct @entity556 inhibitor @entity24772 in @entity1 with XXXX and in healthy subjects.

@entity1 :: ('9606', 'Species') :: ['patients'] @entity556 :: ('2147', 'Gene') :: ['thrombin'] @entity955 :: ('MESH:D001281', 'Disease') :: ['nonvalvular atrial fibrillation', 'NVAF'] @entity18422 :: ('MESH:C109573', 'Chemical') :: ['melagatran'] @entity24772 :: ('MESH:C426686', 'Chemical') :: ['ximelagatran']
@entity955 :: (MESH:D001281,Disease) :: ['nonvalvular atrial fibrillation']
