Originally used in the medical field as an oral fibrinolytic agent to reduce bleeding during surgical procedures, tranexamic acid (TXA) is now gaining increased interest in skincare formulations. This shift began after the accidental observation of its positive effects on skin tone uniformity in certain individuals. However, its skin benefits extend beyond just that. Continue reading to explore its full range of properties.
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Tranexamic Acid: What are the Benefits for the Skin?
Summary
- Benefit No. 1: Tranexamic acid, a promising compound for reducing dark spots
- Benefit No. 2: Tranexamic acid for a stronger skin barrier?
- Benefit No. 3: Reducing redness and inflammation with tranexamic acid?
- Benefit No. 4: Tranexamic acid for inflammatory acne?
- Sources
Published April 26, 2022,
updated on July 11, 2025,
by
Stéphanie, PhD, Doctorate in Life and Health Sciences
—
18 min read
2 to 5%
The optimal concentration of tranexamic acid in skincare products for effectiveness.
8 to 12
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Benefit No. 1: Tranexamic acid, a promising compound for reducing dark spots.
In 1979, a dermatologist accidentally discovered that tranexamic acid could have an unusual effect on the skin. He observed that the complexion of one of his patients treated for chronic hives brightened and evened out. This observation paved the way for the study of this ingredient in skin pigmentation disorders.
While its initial use is medical as an anti-fibrinolytic agent to reduce bleeding, tranexamic acid (TXA) is now attracting increasing interest for its targeted action on pigmentary irregularities, whether caused by sun exposure, hormonal changes, or inflammation, for a more radiant and even complexion.
Several studies have confirmed the effectiveness of tranexamic acid in managing hyperpigmentation, particularly when administered orally, showing more pronounced results. However, its topical application, usually between 2 and 5%, offers a significantly more favorable safety profile, as it eliminates the potential thrombosis risks associated with oral use. Research has shown that at these concentrations, no detectable systemic absorption is observed, thereby limiting concerns related to the pro-coagulant properties of the molecule.
| Sample Size | Type of hyperpigmentation | Protocols | Combined therapy | Results | |
|---|---|---|---|---|---|
| Text to translate here | 33 subjects | Melasma or freckles | Skin emulsion with tranexamic acid for 5 to 18 weeks | / | Improvement in pigmentation in 80% of subjects with melasma and 75% with freckles (visual assessment) |
| 2 groups of 30 individuals (n = 60) | Melasma | (1) Micro-injection of tranexamic acid (4 mg/mL) or (2) topical application of a tranexamic acid solution combined with microneedling, 3 times a month for 8 weeks | / | Improvement of 35.72% in the MASI score in the "micro-injection" group compared to 44.41% in the "microneedling" group | |
| NAEINI F. F. & al. (2014) | 50 Iranian women | Melasma | 3% tranexamic acid topical solution on one side of the face and 3% hydroquinone topical solution on the other side, twice daily for 12 weeks | / | Significant decrease in MASI score in both groups; No significant difference between the two treatments |
| HEYDARIAN A. & al. (2017) | 2 groups of 30 individuals (n = 60) | Melasma | (1) Solution with 5% tranexamic acid or (2) 2% hydroquinone solution, twice daily for 12 weeks | / | Reduction in melanin content and MASI score in both groups; No significant difference between the two treatments |
| 84 Chinese individuals (primarily phototypes III or IV) | Moderate to severe facial melasma | Topical application of a poultice containing 2.5% tranexamic acid for about 7 hours once a day for 8 weeks | / | Significant reduction in the MASI score compared to the control group (poultice without TXA) | |
| ZHENG Q. & al. (2019) | 55 Brazilian individuals | Mild to moderate melasma and/or mild to moderate post-inflammatory hyperpigmentation (PIH) | Topical serum containing 3% tranexamic acid, 1% kojic acid, and 5% niacinamide, twice daily for 12 weeks | In combination with a broad-spectrum sunscreen (preventive care) | Reduction of melanin content by 9% in subjects with melasma and 9.5% in those with PIH |
| and | 3 groups of 20 patients (n = 60) | Melasma | (1) Oral administration of 250 mg of TXA twice daily; (2) topical application of TXA; (3) use of the modified Kligman therapeutic solution (2% hydroquinone, 0.05% tretinoin, 0.01% fluocinolone) for 8 weeks | In combination with a broad-spectrum sunscreen (preventive care) | 30% reduction in MASI score with the modified Kligman therapeutic solution, 25% with oral TXA, and 5% with topical TXA |
| 40 individuals (predominantly phototypes IV and V) | Melasma | Topical solution with 10% tranexamic acid (4 sessions spaced 2 weeks apart) | In combination with microneedling + daily application of sunscreen (preventive care) | 65.9% improvement in the mMASI score on the tranexamic acid-treated side compared to 20.7% on the control side (distilled water) | |
| 25 subjects | Post-inflammatory hyperpigmentation related to acne | (1) Micro-injection of tranexamic acid (every 2 weeks for 3 months) or (2) fractional CO2 laser (every 4 weeks for 3 months) | / | Significant reduction in HPI for both treatments, with better results from the fractional CO2 laser | |
| WINN D. & al. (2021) | 35 subjects | Sun damage-related pigment spots | Topical serum with 2% cetyl tranexamate mesylate (ester of tranexamic acid), applied twice daily for 8 weeks | / | Continuous and significant improvement in pigmentation from 2 weeks, reaching a −16.9% change in the melanin index by 8 weeks |
| POOSTIYAN E. & al. (2023) | Two groups of 30 subjects with acne vulgaris (n = 60) | Post-inflammatory hyperpigmentation related to acne | (1) Topical cream with 20% azelaic acid or (2) Topical solution with 5% tranexamic acid, twice daily for 12 weeks | / | Decrease in HPI observed in both groups; No significant difference between the two treatments |
| LAURENT A. & al. (2024) | 22 Caucasian patients | Facial Hyperpigmentation | Serum with 3% tranexamic acid, 5% niacinamide, and 2% vitamin C derivative + cream with 3% tranexamic acid and 5% niacinamide, twice a day for 8 weeks | / | Significant reduction of 13% in pigmentation intensity and 6% in the size of dark spots |
Summary of some studies on the effect of tranexamic acid in pigmentary disorders.
The MASI score (Melasma Area and Severity Index) is a clinical scale used to evaluate melasma severity by considering the affected area, pigmentation intensity, and border uniformity across different facial regions.
The tranexamic acid is regarded as a brightening agent rather than a lightening one. It is intended to reduce unwanted pigmentation spots.
In 2019, it was demonstrated in a double-blind clinical trial published in the Journal of Research in Medical Sciences that the topical application of a 5% tranexamic acid solution is just as effective as a 3% hydroquinonesolution, the absolute benchmark in hyperpigmentation treatment, for reducing the appearance of melasma but with a better safety profile. After 12 weeks of treatment, melasma severity decreased by 27% in the tranexamic acid group, a result comparable to the hydroquinone group, without the adverse effects.
Of course, it's not necessary to have melasma to use tranexamic acid. It may also help to reduce sunspots from UV exposure, which can occur even with diligent sunscreen use, or the appearance of brown marks that can appear after a blemish resolves (post-inflammatory hyperpigmentation).
The tranexamic acid can be used all year round, including in summer. It does not increase skin sensitivity to the sun, although daily application of a sunscreen remains essential to prevent the appearance of new spots.
However, due to its hydrophilic nature and strong affinity for hydrogen bonds, its penetration into the skin is limited. This is why complementary techniques like intradermal injections, microneedling, or optimized formulations are often explored to enhance its effectiveness.
What is the mechanism of action by which tranexamic acid evens skin tone?
The dark spots result from a localized overproduction of melanin. Reducing this synthesis is thus a key lever for unifying the complexion. Unlike AHAs or other well-known skin-brightening agents (such as kojic acid or arbutin), tranexamic acid has a unique mechanism of action by working at multiple complementary levels to unify the complexion:
When applied topically, tranexamic acid acts as a competitive inhibitor by binding to lysine sites on plasminogen, preventing its conversion into plasmin within keratinocytes—a process triggered primarily by UV exposure or inflammation. This inhibition limits the production of arachidonic acid, an increase of which activates tyrosinase (a key enzyme in melanogenesis) and stimulates melanin synthesis through its metabolite, prostaglandin E2. By curbing these signals, tranexamic acid slows the activation of melanocytes and thus helps mitigate pigmentary disorders.
By inhibiting the conversion of plasminogen to plasmin, tranexamic acid also reduces the release of basic fibroblast growth factor (bFGF), a potent growth factor for melanocytes.
Tranexamic acid also blocks the Sc-uPA pathway (Single-chain urokinase Plasminogen Activator), thereby reducing the increase in size and number of dendrites in melanocytes as well as tyrosinase activity.
Data in vitro have also shown that tranexamic acid inhibits the activation of vascular endothelial growth factor receptors (VEGFR-1 and VEGFR-2) in melanocytes, thereby reducing the subsequent expression of key proteins involved in melanogenesis like tyrosinase. This mechanism also helps to decrease melanin production.
Due to its structure analogous to tyrosine, tranexamic acid might also directly inhibit tyrosinase activity through a competitive mechanism.
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Volunteers find their complexion more even after twice-daily application of our hyperpigmentation and firmness loss emulsion serum (A33).
Benefit No. 2: Tranexamic acid for a stronger skin barrier?
We understand how vital an intact skin barrier is: it limits water loss, protects the skin from external aggressors, and prevents the entry of unwanted agents. However, certain conditions such as rosacea are associated with a compromised barrier, which may contribute to the onset or worsening of symptoms. Interestingly, tranexamic acid, primarily known for its anti-hemorrhagic properties, could also play an unexpected role: supporting the repair of the skin barrier when applied topically.
Studies have shown that when the skin barrier is damaged, it can lead to increased production of pro-inflammatory molecules, infiltration of immune cells, and elevated expression of factors involved in vascularization, all mechanisms frequently observed in rosacea.
A 2015 pilot study (n = 30) highlighted that a topical solution containing 3% tranexamic acid, applied for two weeks, significantly reduced the clinical signs of rosacea compared to the control group. Another study published in 2022 reached similar conclusions in patients with steroid-induced erythematotelangiectatic rosacea. Researchers attributed this improvement to the restoration of the skin's barrier function, although the exact mechanisms of rosacea remain poorly understood.
But how would tranexamic acid work to strengthen the skin barrier?
Available data suggest that tranexamic acid may work by reducing the activity of serine proteases, enzymes involved in inflammation and the breakdown of the skin barrier. This inhibition limits the activation of the PAR-2 receptor, thereby reducing intracellular calcium mobilization in keratinocytes. This cascade slows the secretion of lamellar bodies, which are essential for the formation of epidermal lipids, and promotes the restoration of E-cadherin function, a protein crucial for cell cohesion, thereby helping to restore skin barrier homeostasis.
Furthermore, a study conducted in 2014 by WU P-L. and colleagues demonstrated that tranexamic acid accumulates in the stratum corneum, where it enhances the cohesion between epidermal cells by increasing the expression of occludin, a key protein in tight junctions, speeding up the regeneration of the skin barrier and thereby improving skin appearance and health.
Benefit No. 3: Reducing redness and inflammation with tranexamic acid?
Tranexamic acid is not limited to a depigmenting role: its anti-inflammatory properties also make it an interesting ally to soothe skin prone to redness, particularly in cases of rosacea, inflammatory acne, or skin sensitivity.
A pilot study conducted by KONTOCHRISTOPOULOS et al. (n = 20) evaluated the effectiveness of topical tranexamic acid in erythematotelangiectatic rosacea. Two application methods were compared: a simple damp dressing impregnated with TXA and a combination of microneedling and a tranexamic acid-soaked dressing. After four sessions, all participants showed improvement, with better outcomes observed in the group receiving the combined treatment.
Another study (2023) explored the efficacy of micro-injections of tranexamic acid in treating post-inflammatory erythema in acne-prone skin. Two injections were administered 15 days apart on one side of the face, with the other side serving as a control. At the conclusion of the protocol, a significant reduction in erythema intensity was observed, with no adverse effects reported.
Despite promising results, available studies remain limited and are conducted on small samples. Further research on a larger scale is necessary to establish solid recommendations.
By what mechanisms might tranexamic acid exert its anti-inflammatory and vascular effects?
The anti-inflammatory and vasomodulating properties of tranexamic acid are based on two molecular mechanisms:
Inhibition of the plasminogen/plasmin pathway.
Tranexamic acid acts as a competitive inhibitor by binding to the lysine sites of plasminogen, preventing its conversion to plasmin. Plasmin is involved in the release of pro-inflammatory factors such as IL-6 and TNF-α, two key cytokines in skin inflammatory processes.Regulation of skin angiogenesis.
Plasmin also activates the release of VEGF, a key factor in the formation of new blood vessels. Tranexamic acid inhibits this pathway by reducing the activation of VEGF and the expression of its receptor VEGFR-2, and by decreasing the expression of endothelin-1, another pro-angiogenic mediator involved in the persistent vasodilation observed in rosacea.
Benefit No. 4: Tranexamic acid for inflammatory acne?
Although primarily studied for its effects on pigmentation or the skin barrier, tranexamic acid may also be of interest in the management of inflammatory acne. A preliminary randomized, double-blind, placebo-controlled clinical study evaluated the efficacy of a serum containing 10% tranexamic acid in 18 patients with mild to moderate acne. After eight weeks of twice-daily application to one side of the face (with the other side receiving a placebo), a significant reduction in the number of inflammatory lesions was observed on the treated side. The authors suggest that this improvement may be related to tranexamic acid's modulatory effect on the skin's inflammatory response, although the precise mechanisms remain to be clarified. Further studies are needed to confirm this therapeutic potential.
Sources
TOMITA Y & al. Clinical study of effect of tranexamic acid emulsion on melasma and freckles. Skin Research (2007).
PRABHU N. & al. A randomised, open-label, comparative study of tranexamic acid microinjections and tranexamic acid with microneedling in patients with melasma. Journal of Cutaneous and Aesthetic Surgery (2013).
NAEINI F. F. & al. Topical tranexamic acid as a promising treatment for melasma. Journal of Research in Medical Sciences (2014).
WU P-L. & al. Tranexamic acid accelerates skin barrier recovery and upregulates occludin in damaged skin. International Journal of Dermatology (2014).
ZHONG S. & al. Topical tranexamic acid improves the permeability barrier in rosacea. Dermatologica Sinica (2015).
HEYDARIAN A. & al. Therapeutic effects of topical tranexamic acid in comparison with hydroquinone in treatment of women with melasma. Dermatology and Therapy (2017).
WANG X-W. & al. Tranexamic acid for adults with melasma: A systematic review and meta-analysis. BioMed Research International (2018).
JANNEY M. S. & al. A randomized controlled study comparing the efficacy of topical 5% tranexamic acid solution versus 3% hydroquinone cream in melasma. Journal of Cutaneous and Aesthetic Surgery (2019).
LI J. & al. Tranexamic acid ameliorates rosacea symptoms through regulating immune response and angiogenesis. International Immunopharmacology (2019).
WANG J. V. & al. Tranexamic acid for melasma: Evaluating the various formulations. Journal of Clinical and Aesthetic Dermatology (2019).
WU X-P. & al. Activation of VEGF receptors in response to UVB promotes cell proliferation
and melanogenesis of normal human melanocytes. Experimental Cell Research (2019).ZHENG Q. & al. Effect of a tranexamic acid, kojic acid, and niacinamide containing serum on facial dyschromia: A clinical evaluation. Journal of Drugs in Dermatology (2019).
JAWADE S. & al. Study of oral tranexamic acid, topical tranexamic acid, and modified Kligman's regimen in treatment of melasma. Journal of Cosmetic Dermatology (2020).
SANDHU J. & al. Clinical efficacy of topical Tranexamic acid with microneedling in melasma. Dermatologic Surgery (2020).
CHAICHALOTORNKUL M. D. & al. Adjunctive treatment for acne vulgaris by tranexamic acid. Journal of Cosmetic Dermatology (2022).
MISRI R. & al. Topical 10% tranexamic acid for erythematotelangiectatic steroid-induced rosacea. Journal of the American Academy of Dermatology (2022).
POOSTIYAN E. & al. A comparative study of 20% azelaic acid cream versus 5% tranexamic acid solution for the treatment of postinflammatory hyperpigmentation in patients with acne vulgaris: A single-blinded randomized clinical trial. Journal of Research in Medical Sciences (2023).
LAURENT A. & al. Pilot clinical safety and efficacy evaluation of a topical 3% tranexamic acid cream and serum protocol for managing facial hyperpigmentation in caucasian patients. Cosmetics (2024).
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