Disease relevance of Dabigatran

• BACKGROUND: Dabigatran etexilate is an oral direct thrombin inhibitor undergoing evaluation for the prevention of venous thromboembolism (VTE) following orthopedic surgery [1].

High impact information on Dabigatran

• Aims To describe the pharmacokinetic-pharmacodynamic (PK-PD) characteristics of the direct thrombin inhibitor dabigatran in hip replacement patients by assessing coagulation parameters activated partial thromboplastin time (aPTT) and ecarin clotting time (ECT), interindividual variability and factors affecting PD responses [2].
• The AUC(0-24) of dabigatran was 88% of the steady-state AUC using a preliminary tablet formulation and 106% of that seen in the healthy volunteer study [3].
• In an open-label, 3-way crossover study, dabigatran etexilate was administered to 18 male volunteers in the fasted state, after administration of food and with coadministration of the proton pump inhibitor, pantoprazole [3].

Gene context of Dabigatran

• When treated with dabigatran (1 microg/ml), scleroderma lung myofibroblasts produced 6-fold less alpha-SMA, 3-fold less CTGF, and 2-fold less type I collagen compared with untreated cells [4].

Analytical, diagnostic and therapeutic context of Dabigatran

• Dabigatran etexilate has recently been evaluated in phase II clinical trials in patients undergoing total hip replacement [5].
• Following oral administration, dabigatran etexilate is rapidly converted to its active form, dabigatran [3].

References