• Keith A Moore, Timothy S Callahan, Pierre Maison-Blanche, Isabelle Morin, Ted Marenco, Dennis Swearingen, and Joy Olbertz.
• Xanodyne Pharmaceuticals, Inc., Clinical Research & Product Development, One Riverfront Place, Newport, KY 41071-4563, USA. kmoore@xanodyne.com
• Expert Opin Pharmacother. 2010 Oct 1; 11 (14): 2281-90.

ObjectiveTo assess the effect of a novel oral tranexamic acid treatment on cardiac repolarization in a randomized, double-blind, positive- and placebo-controlled, four-treatment single-dose cross-over inpatient study.MethodsQTc interval and drug exposure relationship analyses were performed using triplicate digital electrocardiographs (ECGs) collected from 12-lead Holter monitors from healthy females (n = 48) with plasma drug concentrations and pharmacokinetics simultaneously evaluated over 24 h post-dose. Therapeutic (1.3 g) and supratherapeutic (3.9 g) tranexamic acid modified immediate-release doses, a positive-control 0.4 g moxifloxacin dose, and a placebo-control were administered at each period.ResultsAll post-dose, time-matched, baseline-adjusted, mean QTcF (Fridericia's heart rate correction, QT/RR(1/3)) treatment-placebo differences (DeltaDeltaQTcF), were less than 5 milliseconds (ms) for the 1.3 g and 3.9 g tranexamic acid doses. Upper limits of the 95% confidence interval (CI) for all tranexamic acid-placebo DeltaDeltaQTcF doses were < 10 ms for all time points. Lower limits of the 95% CI for the positive-control (moxifloxacin-placebo) DeltaDeltaQTcF were > 5 ms at multiple time points demonstrating assay sensitivity. No correlation between tranexamic acid plasma concentrations and adjusted QTc intervals was observed. A positive linear relationship was observed for moxifloxacin (p < 0.01).ConclusionCardiac repolarization is not influenced by tranexamic acid at the doses studied.

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