Background: Melasma causes considerable cosmetic disfigurement and none of the existing treatment modalities are satisfactory. Recently tranexamic acid has been reported to reduce hyperpigmentation in patients with melasma. Objective: The purpose of the study was to evaluate the efficacy and safety of tranexamic acid containing oral medication for the treatment of melasma. Methods: Forty-five female volunteers who had been diagnosed with melasma were enrolled in the present study. Patients were instructed to take medication for 8 weeks. The melanin index (MI) and erythema index (EI) were measured at baseline, and at 4 and 8 weeks. The melasma area and severity index (MASI) was scored at 0, 4, and 8 weeks. Self-satisfaction and safety evaluations were also performed at each visit. Results: The mean MI measured on the lesional skin was decreased at 4 and 8 weeks compared with baseline (p＜0.01 for both). The mean EI measured on the lesional skin and the MASI also showed a significant decrease from baseline to 8 weeks (p＜0.001 for EI and p=0.020 for MASI). Based on self-assessment, 39.5% of the patients were very satisfied, 44.2% were satisfied, and 11.6% felt moderate improvement after 8 weeks of medication; only 2 patients (4.7%) were dissatisfied. Thus, ＞80% of patients were satisfied with the medication. Adverse effects were minimal and two patients dropped out of the study due to drug-related urticaria and unexpected pregnancy. Conclusion: Tranexamic acid-containing oral medication is an effective and safe therapeutic modality for the treatment of melasma.