: Aleglitazar acts through balanced activation of peroxisome 
proliferator-activated receptors α and γ; warfarin is a commonly prescribed 
anticoagulant. Given the extent of cardiovascular disease in patients with type 
2 diabetes, cotreatment with aleglitazar and warfarin is likely in this 
population. This open-label, randomized, 2-period, crossover study in 12 healthy 
male subjects investigated the potential for drug-drug interactions between 
warfarin and aleglitazar (final data drawn from 11 white subjects). The primary 
objective was to investigate the effect of aleglitazar on the pharmacokinetic 
properties of S-warfarin and on the pharmacodynamics of the racemic mixture; the 
secondary objectives included the effect of aleglitazar on R-warfarin 
pharmacokinetics and of racemic warfarin on aleglitazar pharmacokinetics. 
Subjects were randomized to single-dose warfarin on day 1 or aleglitazar once 
daily (12 days) plus single-dose warfarin on day 6 followed by a 14-day washout 
period, then crossover. Coadministration of aleglitazar reduced S- and 
R-warfarin exposure (AUC0-∞) by 18% and 13%, respectively, but did not change 
its pharmacodynamic effects (prothrombin time and factor VII activity). After 
warfarin dosing, aleglitazar trough concentrations remained within the same 
range. These findings indicate that coadministration of aleglitazar and warfarin 
is unlikely to affect the efficacy or safety of either agent.