Tranexamic acid in treatment of melasma: A comprehensive review of clinical studies

Dermatol Ther. 2017 May;30(3). doi: 10.1111/dth.12465. Epub 2017 Jan 30.


Melasma is a human melanogenesis dysfunction that results in localized, chronic acquired hyperpigmentation of the skin. It has a significant impact on appearance, causing psychosocial and emotional distress, and reducing the quality of life of the affected patients. Tranexamic acid (TA) is a plasmin inhibitor used to prevent abnormal fibrinolysis to reduce blood loss and exerts its effect by reversibly blocking lysine binding sites on plasminogen molecules, thus inhibiting plasminogen activator (PA) from converting plasminogen to plasmin. As plasminogen also exists in human epidermal basal cells and cultured human keratinocyte are known to produce PA, there is basic rationale that TA will affect keratinocyte function and interaction. A thorough literature review indicates that while TA is used through various route of administration including oral, topical, and intradermal injection and as adjutant therapy with laser to treat melasma, its efficacy is not established adequately. Further studies are needed to clarify the role of TA in treatment of melasma.

Keywords: hyperpigmentation; melasma; tranexamic acid.

Publication types

  • Review

MeSH terms

  • Administration, Cutaneous
  • Administration, Oral
  • Antifibrinolytic Agents / administration & dosage
  • Antifibrinolytic Agents / adverse effects
  • Dermatologic Agents / administration & dosage*
  • Dermatologic Agents / adverse effects
  • Humans
  • Injections, Intradermal
  • Melanosis / drug therapy*
  • Melanosis / pathology
  • Quality of Life
  • Tranexamic Acid / administration & dosage*
  • Tranexamic Acid / adverse effects


  • Antifibrinolytic Agents
  • Dermatologic Agents
  • Tranexamic Acid