BACKGROUND: @entity48152 is a novel angiotensin II receptor blocker. @entity48152 is mainly eliminated via biliary excretion, and its urinary elimination is less than 3%. OBJECTIVE: Based on guidance from the United States Food and Drug Administration, a reduced pharmacokinetic (PK) study was conducted to evaluate the effect of renal function on the PK of @entity48152 in @entity1 with @entity8 and healthy volunteers. METHODS: A single centre, single-dose, open-label, healthy volunteer controlled trial was conducted in @entity1 with @entity8 ( @entity8 ) (estimated glomerular filtration rate lower than 30 mL/ @entity1009 .73 m(2)) and age-, weight- and sex-matched healthy volunteers (estimated glomerular filtration rate higher than 90 mL/ @entity1009 .73 m(2)). All @entity1 received a single oral dose of @entity48152 120 mg, after which serial blood sampling for PK evaluation was conducted. Noncompartmental PK analysis of @entity48152 was performed. A mixed-effects model approach was used to identify significant covariates and PK parameters. RESULTS: Sixteen subjects were enrolled (8 healthy volunteers and 8 @entity8 @entity1 ). The maximum plasma concentrations and areas under the plasma concentration curves of the @entity8 @entity1 were higher than those of the healthy volunteers, with geometric mean ratios of 1.87 and 1.73, respectively. The relative bioavailability of @entity48152 from the population PK analysis was 77% higher in the @entity8 @entity1 than in the healthy volunteers. CONCLUSION: The increased drug exposure of @entity48152 in @entity8 @entity1 was explained by the increased relative bioavailability. This result can be explained from our knowledge concerning alterations in PK related to renal function.

Effect of renal function on the pharmacokinetics of XXXX : a single-dose, open-label, Phase I study.

@entity48152 :: ('MESH:C558933', 'Chemical') :: ['Fimasartan', 'fimasartan'] @entity1 :: ('9606', 'Species') :: ['participants', 'patients'] @entity8 :: ('MESH:D007674', 'Disease') :: ['renal impairment', 'RI'] @entity1009 :: ('966', 'Gene') :: ['min/1']
@entity48152 :: (MESH:C558933,Chemical) :: ['fimasartan']
