Mechanism of Action of Topical Tranexamic Acid in the Treatment of Melasma and Sun-Induced Skin Hyperpigmentation

Tranexamic acid (TXA) has anti-plasmin activity and has been shown when administered orally to be effective against melasma, for which it is considered first-line pharmacotherapy. Several studies have shown that topically applied TXA is also effective against melasma and skin hyperpigmentation caused by sunburn and inflammation. The TXA concentration in the epidermis and dermis/vasculature has been estimated from its distribution in the skin after closed application, and topically applied TXA has thus been shown to act on neutrophils and mast cells in the dermis and on the vascular system. It is unlikely that topically applied TXA acts on dermal neutrophils or mast cells or on the vascular system to form thrombi. As discussed in the present review, studies on the effects of topical TXA on the hyperpigmentation process indicate that the resulting skin-lightening mechanism involves the suppression of cytokine/chemical mediator production, which stimulates melanin production via the keratinocyte-derived urokinase-type plasminogen activator and plasminogen derived from dermal vascular in the basal layer of the epidermis, thereby suppressing the production of excessive melanin to prevent hyperpigmentation.