REVIEW ARTICLE Tranexamic Acid in the Treatment of Melasma: A Review of the Literature Marina Perper 1 • Ariel Eva Eber 1 • Rachel Fayne 1 • Sebastian Hugo Verne 1 • Robert James Magno 1 • Jessica Cervantes 1 • Mana ALharbi 2 • Ibrahim ALOmair 2 • Abdulkarem Alfuraih 2 • Keyvan Nouri 1 Ó Springer International Publishing Switzerland 2017 Abstract Melasma is a common acquired pigmentary disorder marked by irregular hyperpigmented macules or patches and most commonly occurs in women of darker skin color. It is a chronic often-relapsing condition that causes negative psychosocial effects in those affected. Current treatments such as hydroquinone, kojic acid, and retinoids, among others, demonstrate variable efficacy and side-effect profiles. We conducted a comprehensive liter- ature review examining the use of tranexamic acid (TA), a well-known anti-fibrinolytic agent, in the treatment of melasma. TA delivered orally, topically, and through physical methods works via the inhibition of ultraviolet (UV)-induced plasmin activity in keratinocytes. Predefined search terms were entered into PubMed. Articles were then independently screened by two authors to include only those written in the English language and relating to human subjects with at least mild melasma. The search identified 28 articles, 15 of which met the criteria for full review. The review revealed that TA treatment for melasma is equally effective or more effective than other standard therapies and may induce fewer side effects. Our comprehensive review suggests that TA may be a promising treatment option for melasma because of its demonstrated effective- ness alone and in combination with other modalities as well as its limited side-effect profile. Key Points Tranexamic acid (TA) may be a promising treatment for melasma, a highly prevalent pigmentary disorder with a propensity for recurrence. The treatment’s main mechanism of action involves inhibiting the conversion of plasminogen to plasmin, which is a known melanogenic factor. Three different methods of TA delivery—oral, topical, and physical (injection and micro- needling)—have been implicated for the treatment of melasma and are evaluated for efficacy and safety in this review. 1 Introduction Melasma, also occasionally referred to as chloasma, is a common acquired benign condition characterized by sym- metric hyperpigmented macules or patches with irregular borders, most often distributed on the face [1]. Areas of hyperpigmentation can be further categorized by the area of distribution: centrofacial (involving the forehead, cheeks, nose, upper lip, and chin), malar (affecting the cheeks and nose), or mandibular (along the jawline). It is most prevalent among young to middle-aged female patients of African, Asian, or Hispanic descent [2]. The exact pathogenesis for melasma has not been elucidated, but several theories exist. Triggering factors have been clearly identified; those most frequently cited include pregnancy, the use of hormonal & Marina Perper m.perper@umiami.edu 1 Department of Dermatology and Cutaneous Surgery, University of Miami Hospital, 1475 NW 12th Ave. Suite 2175, Miami, FL 33136, USA 2 Imam Muhammad Ibn Saud Islamic University (IMSIU), Riyadh, Saudi Arabia Am J Clin Dermatol DOI 10.1007/s40257-017-0263-3