Tranexamic acid is a synthetic derivative of the amino acid lysine and is classified pharmacologically as an antifibrinolytic agent. It is a white crystalline compound that is readily soluble in water. Its primary pharmaceutical function is to inhibit fibrinolysis, but research has also identified mechanisms that make it relevant to dermatological and cosmetic applications, particularly pigmentation disorders.

INCI Name: Tranexamic Acid
CAS Number: 1197-18-8
EC Number: 214-818-2
Molecular Formula: C8H15NO2
Molecular Weight: 157.21 g/mol
Chemical Class: Amino Acid Derivative
Function: Skin Conditioning Agent, Skin Brightening Agent

Cosmetic Applications

Tranexamic acid is increasingly used in skincare formulations designed to improve the appearance of uneven skin tone and hyperpigmentation. It is particularly associated with products targeting melasma and post-inflammatory hyperpigmentation.

It may be incorporated into serums, creams, lotions and other leave-on skincare products. Topical tranexamic acid has been investigated both as a standalone active and in combination with other cosmetic ingredients used for pigmentation concerns.

Clinical research has evaluated topical tranexamic acid in concentrations including 2% and 5%, although the appropriate concentration for a cosmetic formulation depends on the intended product, formulation system, target market and applicable regulatory requirements.

How Tranexamic Acid Works

Tranexamic acid primarily acts by inhibiting the interaction of plasminogen and plasmin with fibrin. This antifibrinolytic activity is well established in its pharmaceutical use.

In skin, the mechanism is more complex. Ultraviolet radiation and inflammatory processes can increase plasmin activity in keratinocytes. Increased plasmin activity may contribute to the release of inflammatory and melanogenic mediators that influence melanocyte activity and melanin production.

By inhibiting plasminogen activation and plasmin-related pathways, tranexamic acid may reduce several processes associated with melanogenesis. Research has also investigated anti-inflammatory and anti-angiogenic effects that may contribute to its activity in melasma and other pigmentation disorders.

The exact mechanism by which topical tranexamic acid improves pigmentation is not completely understood, and several biological pathways are likely involved.

Formulation Considerations

Tranexamic acid is water soluble, which makes it suitable for incorporation into aqueous cosmetic systems such as serums, gels and emulsions.

When developing a formulation containing tranexamic acid, the compatibility of the ingredient with the complete formulation system should be considered. pH, solvent system, preservatives, other active ingredients and packaging can all influence the stability and performance of the finished product.

Because tranexamic acid is often combined with other ingredients targeting uneven pigmentation, the overall formulation should be assessed for compatibility and skin tolerability. Combinations with ingredients such as niacinamide, vitamin C derivatives, azelaic acid and exfoliating acids may require particular attention to formulation pH and irritation potential.

Stability

Tranexamic acid is considered a relatively stable water-soluble ingredient, although the stability of a finished formulation depends on the complete formulation system.

Factors including pH, temperature, concentration, water quality, interactions with other ingredients and packaging should be considered during formulation development.

Finished products should undergo appropriate stability testing to evaluate changes in appearance, color, odor, pH, viscosity, microbial quality and other relevant quality characteristics throughout the intended shelf life.

Skin Compatibility

Topical tranexamic acid has generally demonstrated good tolerability in clinical studies. Compared with some traditional depigmenting ingredients, topical tranexamic acid has been reported to cause relatively few local adverse effects.

However, irritation, dryness, redness, itching or a transient burning or stinging sensation may occur, particularly when tranexamic acid is combined with other active ingredients that can affect skin tolerance.

The tolerability of the finished product depends on the concentration, formulation vehicle, pH, frequency of application and combination with other ingredients.

Safety

The safety profile of topical tranexamic acid differs from that of systemic administration. Oral tranexamic acid is a pharmaceutical medicine with systemic antifibrinolytic effects and requires medical consideration because of its potential effects on blood clotting.

Topical cosmetic use results in a different exposure profile, and clinical studies of topical tranexamic acid have generally reported good local tolerability. Nevertheless, the safety of a finished cosmetic formulation must be assessed based on its actual concentration, exposure, application area, frequency of use and intended consumer population.

Claims or formulations involving systemic treatment should not be extrapolated from cosmetic topical use.

Evidence in Hyperpigmentation

Tranexamic acid has been investigated extensively for melasma and other pigmentation disorders. A 2023 focused review covering 46 studies concluded that oral, topical and intralesional tranexamic acid had demonstrated improvements in melasma outcomes, while also noting that topical administration was generally better tolerated than systemic administration.

A randomized controlled study investigating topical 5% tranexamic acid in women with melasma reported improvement over a 12-week treatment period.

More recent literature has continued to investigate topical tranexamic acid for melasma and post-inflammatory hyperpigmentation. A 2026 review concluded that topical and intradermal tranexamic acid show promising results for hyperpigmentation disorders, while emphasizing that evidence and regulatory status vary depending on the condition and route of administration.

Regulatory Considerations

Tranexamic acid is primarily recognized as a pharmaceutical active ingredient rather than a conventional cosmetic ingredient. Its regulatory status and permitted use in cosmetic products therefore need to be assessed carefully in the target market.

In particular, the distinction between a cosmetic product and a medicinal product is important when determining product claims. Claims that a product treats, prevents or cures a medical condition may cause the product to fall under medicinal product regulations rather than cosmetic regulations.

The applicable regulatory framework, ingredient status, concentration and intended claims should therefore be evaluated before commercializing a product containing tranexamic acid.

References

AlJabr, A., AlAnazi, A. M. I., and AlEtebi, R. A. A. “Tranexamic Acid for Hyperpigmentation Disorders: A Literature Review on Efficacy and Safety in Melasma and PIH.” Journal of Cosmetic Dermatology, 2026, 25(2), e70692. DOI: 10.1111/jocd.70692.

Maeda, K. “Mechanism of Action of Topical Tranexamic Acid in the Treatment of Melasma and Sun-Induced Skin Hyperpigmentation.” Cosmetics, 2022, 9(5), 108. DOI: 10.3390/cosmetics9050108.

Konisky, H., Balazic, E., Jaller, J. A., Khanna, U., and Kobets, K. “Tranexamic acid in melasma: A focused review on drug administration routes.” Journal of Cosmetic Dermatology, 2023, 22(4), 1197–1206. DOI: 10.1111/jocd.15589.

Na Ayuthaya, K. P., Niumphradit, N., Manosroi, A., and Nakakes, A. “Topical 5% tranexamic acid for the treatment of melasma in Asians: a double-blind randomized controlled clinical trial.” Journal of Cosmetic and Laser Therapy, 2012, 14(3), 150–154. DOI: 10.3109/14764172.2012.685478.

Kim, K. M. and Lim, H. W. “The uses of tranexamic acid in dermatology: a review.” International Journal of Dermatology, 2023, 62(5), 589–598. DOI: 10.1111/ijd.16160.

National Center for Biotechnology Information. PubChem – Tranexamic Acid.

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