The effects of tranexamic acid (TXA), an effective ingredient against melasma and hyperpigmentation due to sunburn, were studied extensively in this article. It indicate that the resulting skin-lightening mechanism after application of TXA on skin 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.