Background: Melasma is an acquired pigmentary disorder classically manifested as hyperpigmented macules and patches distributed symmetrically on the face, neck, and rarely the upper limbs. The exact etio-pathogenesis of melasma is complex and not completely understood. Treatment of melasma includes; topical, oral, procedural or combination treatments. Tranexamic acid is a plasmin inhibitor. Objective: To evaluate the efficacy and safety of oral tranexamic acid for treatment of melasma. Patients and methods: The study involved 40 female patients with oral intake of tranexamic acid 250 mg, twice daily, for three months. All patients were evaluated clinically, dermoscopically and by MASI scoring before and after treatment. Results: Results of the study revealed statistically significant improvement of melasma according to MASI score after 3 months of treatment in all patients, indicating that oral TA may be considered as a very effective treatment for melasma. As regard the response of treatment, 19 (47.5%) patients had excellent response, 12 (30%) patients had very good response, and 9 (22.5%) patients had good response. Dermoscopic features after treatment showed that, there were improvement of pigmentation and elimination of erythema as 27 patients (67.5%) showed fainting of colour and elimination of erythema, and 13 patients (32.5) patients showed light brown pigmentation and elimination of erythema. Conclusion: Oral intake of TA is a safe and effective method for treatment of melasma, with no risk of PIH, thrombotic or bleeding tendency.