The pharmacokinetics and safety of darapladib in subjects with severe renal impairment.

ABSTRACT:

Aim

Darapladib is a potent and reversible orally active inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2 ). The aim of the study was to assess the effects of severe renal impairment on the pharmacokinetics and safety/tolerability of darapladib compared with normal renal function.

Methods

This was an open label, parallel group study of darapladib following 10 day once daily 160 mg oral dosing in subjects with normal (n = 8) and severe renal impairment (estimated glomerular filtration rate <30 ml min(-1) 1.73 m(-2) , n = 8). Plasma concentrations of total and unbound darapladib as well as total darapladib metabolites were determined in samples obtained over 24 h on day 10.

Results

Plasma concentrations of total and unbound darapladib as well as all three me

SUBMITTER: Magee MH 

PROVIDER: S-EPMC4594701 | biostudies-literature | 2015 Oct

REPOSITORIES: biostudies-literature