AIM/METHODS:

Darapladib is a potent and reversible orally active inhibitor of lipoprotein-associated phospholipase A2 (Lp-PLA2 ). This open-label, parallel-group study was conducted to assess the effects of renal impairment on the pharmacokinetics and safety/tolerability 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/1.73 m2 , n = 8). Plasma concentrations of total and unbound darapladib as well as total darapladib metabolites were determined in samples obtained over 24-hour on day 10.

 

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