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Poster

Effect of Steady-State Esuberaprost (BPS-314d-MR) on the Safety, Pharmacokinetics and Pharmacodynamics of Warfarin in Healthy Adult Subjects

September 25, 2016
ACCP 2016 -- The prostacyclin analogue beraprost (BPS) consists of a mixture of 4 stereoisomers and is available for treatment of PAH in Japan and other Asian countries. Warfarin is administered as a racemic mixture of (R)- and (S)-enantiomers and is completely absorbed after oral administration, with peak concentration generally attained within the first 4 hours. The anticoagulant effect of warfarin generally occurs within 24 hours after drug administration. However, the peak anticoagulant effect may be delayed up to 72 to 96 hours. The duration of action of a single dose of racemic warfarin is 2 to 5 days. Since multiple CYP enzymes are involved in the metabolism of warfarin, and also due to its narrow therpeutic index, other concomitant therapies can cause an increased risk of bleeding or clotting by potentiating the anticoagulation properties of warfarin. Notably, drugs that inhibit platelet activation, such as prostacylins can amplify the bleeding risks associated with warfarin. Therefore, a drug-drug interaction study was conducted to determine the potential effects of BPS-314d-MR tablets on warfarin pharmacokinetics.