Tranexamic acid, a synthetic lysine derivative, is an antifibrinolytic drug that prevents the breakdown of fibrin by competitively blocking binding sites of plasminogen. Tranexamic acid is often considered a first-line treatment for the management of heavy menstrual bleeding (HMB). A new oral formulation of tranexamic acid provides a nonhormonal HMB therapy that is safe, effective and well tolerated; is administered only during menstruation; addresses the excessive fibrinolysis implicated in many cases of HMB; and improves women's health-related quality of life by reducing limitations on physical, social and leisure activities. This article provides a summary of the clinical development, therapeutic efficacy and tolerability profile of this novel formulation of tranexamic acid for the treatment of HMB.