In patients with uncontrolled, extracranial bleeding, the median time to hemostasis was 2.5 hours after idarucizumab administration. Reversal was rapid and occurred independently of baseline dabigatran concentration. Among patients receiving dabigatran and treated with idarucizumab for uncontrolled bleeding or undergoing an urgent procedure (total n = 503), the median maximum percentage reversal within 4 hours of idarucizumab administration was 100%, as assessed by either diluted thrombin time or the ecarin clotting time. The reduction in dabigatran plasma concentration was seen over the entire observation period of at least 24 hours. The diluted thrombin time, ecarin clotting time, activated partial thromboplastin time, thrombin time, and activated clotting time returned to baseline. In healthy subjects aged 45 to 64 years, the plasma concentrations of unbound dabigatran were decreased to the lower limit of quantification immediately after administration of idarucizumab 5 g. The remaining part of the dose is assumed to be eliminated via protein catabolism, mainly in the kidney.

Approximately 32% of the dose is recovered in the urine within a collection period of 6 hours and less than 1% in the following 18 hours. Idarucizumab is rapidly eliminated with an initial half-life of 47 minutes and a terminal half-life of 10.3 hours. Idarucizumab undergoes biodegradation of the antibody to smaller peptides or amino acids which are then reabsorbed and incorporated in the general protein synthesis. It exhibits limited extravascular distribution and follows multiphasic disposition kinetics. Idarucizumab is administered intravenously.

Idarucizumab dose