What is the mechanism of action of tranexamic acid (TXA) in improving skin?

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Last updated: April 11, 2025 • View editorial policy

From the Guidelines

Tranexamic acid is a medication that improves skin by reducing hyperpigmentation and inflammation, and its topical application is generally well-tolerated and effective in concentrations of 2-5%. It works by inhibiting the enzyme plasmin, which plays a role in melanin production and inflammation in the skin 1. By blocking this pathway, tranexamic acid helps prevent the formation of dark spots and melasma, particularly those caused by sun exposure or hormonal changes.

Key Points to Consider

  • In skincare products, tranexamic acid is typically found in concentrations of 2-5% in serums, creams, or toners.
  • For optimal results, apply tranexamic acid products once or twice daily to clean skin, followed by moisturizer and sunscreen during daytime use.
  • Most people begin seeing improvements after 8-12 weeks of consistent use.
  • Tranexamic acid can be combined with other brightening ingredients like vitamin C or niacinamide for enhanced effects. However, it's essential to note that the oral form of this medication affects blood clotting, and its use in certain medical conditions, such as cirrhosis, is not recommended due to the risk of thrombotic events 2. If you have a history of blood clots or are pregnant, consult a dermatologist before using tranexamic acid products.

From the FDA Drug Label

Tranexamic acid is a synthetic lysine amino acid derivative, which diminishes the dissolution of hemostatic fibrin by plasmin. In the presence of tranexamic acid, the lysine receptor binding sites of plasmin for fibrin are occupied, preventing binding to fibrin monomers, thus preserving and stabilizing fibrin’s matrix structure

The FDA drug label does not answer the question of how tranexamic acid improves skin. The provided text only explains the mechanism of action of tranexamic acid as an antifibrinolytic agent, which is related to its effects on blood clotting and fibrinolysis, but does not mention its effects on skin.

From the Research

What is Tranexamic Acid

  • Tranexamic acid (TXA) is a novel treatment for melasma, a common acquired disorder of hyperpigmentation that commonly affects those with skin of color 3.
  • It is a plasmin inhibitor that works via the inhibition of ultraviolet (UV)-induced plasmin activity in keratinocytes 4.

Mechanism of Action

  • TXA has a multimodal mechanism of action, making it an effective treatment for melasma 3.
  • It inhibits the activity of plasmin, an enzyme that breaks down blood clots, which can contribute to the development of melasma 4.

Forms of Administration

  • TXA can be administered orally, topically, or intralesionally, and each method has been shown to be safe and effective for the treatment of melasma 5.
  • Oral TXA has been found to be the most effective form of treatment, especially in cases of refractory melasma 5.
  • Topical TXA can be used alone or in combination with other cosmeceuticals to improve outcomes, and is better tolerated than hydroquinone, a traditional topical melasma treatment 5.

Efficacy and Safety

  • Studies have shown that TXA is a safe and efficacious treatment for melasma, with few and mild side effects 3, 6, 4.
  • Oral TXA has been found to be effective in reducing the severity of melasma, even in low doses and over short periods of time 3.
  • Topical liposomal TXA has been shown to be a new, effective, safe, and promising therapeutic agent in the treatment of melasma 6.
  • TXA may be a promising treatment option for melasma due to its demonstrated effectiveness and limited side-effect profile 4, 7.

Professional Medical Disclaimer

This information is intended for healthcare professionals. Any medical decision-making should rely on clinical judgment and independently verified information. The content provided herein does not replace professional discretion and should be considered supplementary to established clinical guidelines. Healthcare providers should verify all information against primary literature and current practice standards before application in patient care. Dr.Oracle assumes no liability for clinical decisions based on this content.