Long reserved for the medical field as an oral fibrinolytic agent intended to limit bleeding during surgical procedures, tranexamic acid (TXA) now generates growing interest in skincare. This transition began following the incidental observation of its positive effects on skin tone uniformity in some individuals. However, its skin benefits extend beyond this. Continue reading to uncover all its properties.
Tranexamic Acid: What are the benefits for the skin?
Summary
Published on July 21, 2025, by Stéphanie, PhD, Doctorate in Life and Health Sciences — 18 min of reading
Themes:
Benefit No. 1: Tranexamic acid, a promising active ingredient for addressing dark spots.
In 1979, a dermatologist accidentally discovered that tranexamic acid could affect the skin in an unusual way. He noticed that the complexion of one of his patients treated for chronic hives was becoming clearer and more even. This observation paved the way for studying this active ingredient in skin pigmentation disorders.
Although its initial use was medical as an antifibrinolytic agent to reduce bleeding, tranexamic acid (TXA) is now garnering increased interest for its targeted action on pigment irregularities, whether caused by sun exposure, hormonal changes, or inflammation, for a brighter and more even complexion.
Several studies have confirmed the efficacy of tranexamic acid in managing hyperpigmentation, particularly when administered orally, yielding more pronounced results. However, its topical application, usually between 2 and 5%, offers a significantly more favourable safety profile, removing the potential risks of thrombosis associated with oral use. Research has shown that at these concentrations, no detectable systemic absorption occurs, thereby limiting concerns regarding the pro-coagulant properties of the compound.
| Sample size | Type of hyperpigmentation | Protocols | Combination Therapy | ||
|---|---|---|---|---|---|
| TOMITA Y. & al. (2007) | 33 subjects | Melasma or freckles | Topical tranexamic acid emulsion for five to eighteen weeks | / | Improvement in pigmentation observed in 80% of subjects with melasma and 75% with freckles (visual assessment) |
| Two groups of 30 individuals (n = 60) | Melasma | (1) Microinjection of tranexamic acid (4 mg/mL) or (2) topical application of a tranexamic acid solution combined with microneedling, three times a month for eight weeks | / | Improvement of 35.72% in MASI score in the "micro-injection" group compared to 44.41% in the "microneedling" group | |
| NAEINI F. F. & al. (2014) | 50 Iranian women | Melasma | Topical solution with 3% tranexamic acid on one side of the face and a 3% hydroquinone topical solution on the other side, twice daily for 12 weeks | / | Significant decrease in the MASI score in both groups; No significant difference between the two treatments |
| Heydarian A. & al. (2017) | Two groups of 30 individuals (n = 60) | Melasma | (1) Solution with 5% tranexamic acid or (2) solution with 2% hydroquinone, 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 poultice containing 2.5% tranexamic acid for about 7 hours once a day for 8 weeks | / | Significant reduction in MASI score compared to the control group (poultice without ATX) | |
| 55 Brazilian women | 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, applied twice daily for 12 weeks | In conjunction with a broad-spectrum sunscreen (preventive care) | Reduction in melanin content by 9% in subjects with melasma and by 9.5% in those with PIH | |
| Three groups of 20 participants (n = 60) | Melasma | (1) Oral administration of 250 mg ATX twice daily; (2) topical application of ATX; (3) use of the modified Kligman therapeutic solution (hydroquinone 2%, tretinoin 0.05%, fluocinolone 0.01%) for eight weeks | In conjunction with a broad-spectrum sunscreen (preventive care) | Reduction of the MASI score by 30% with the modified Kligman therapeutic solution, by 25% with oral ATX, and by 5% with topical ATX | |
| 40 people (mainly phototypes IV and V) | Melasma | 10% Tranexamic Acid Topical Solution (4 sessions spaced 2 weeks apart) | In combination with microneedling + daily application of a sunscreen (preventive care) | Improvement of 65.9% in the mMASI score on the tranexamic acid-treated side compared to 20.7% on the control side (distilled water) | |
| Post-inflammatory hyperpigmentation related to acne | (1) Micro-injection of tranexamic acid (every 2 weeks for 3 months) or (2) fractionated CO2 laser (every 4 weeks for 3 months) | / | Significant reduction of HPI for both treatments, with better results from the fractional CO2 laser | ||
| 35 subjects | Pigment spots related to sun damage | Topical serum with 2% cetyl tranexamate mesylate (ester of tranexamic acid), twice daily for 8 weeks | / | Continual and significant improvement in pigmentation observed after 2 weeks, reaching a −16.9% reduction in the melanin index at 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 | / | Reduction of IOP observed in both groups; No significant difference between the two treatments |
| " and " | 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 daily for 8 weeks | / | Significant reduction of 13% in pigmentation intensity and 6% in the size of dark spots |
Summary of part of the studies on the effect of tranexamic acid in pigmentary disorders.
The MASI score (Melasma Area and Severity Index) is a clinical scale used to assess melasma severity by considering the affected area, pigmentation intensity, and edge uniformity on different facial zones.
The tranexamic acid is considered a brightening agent, not a whitening agent. It is intended to reduce unwanted pigmentation spots.
In 2019, a double-blind clinical trial published in the Journal of Research in Medical Sciences demonstrated that the topical application of a 5% tranexamic acid solution is as effective as a 3% hydroquinone solution, the absolute standard in hyperpigmentation treatment, in reducing the appearance of melasma, but with a better safety profile. After 12 weeks of treatment, the severity of melasma decreased by 27% in the tranexamic acid group, a result comparable to the hydroquinone group, without adverse effects.
Obviously, it is not necessary to have melasma to use tranexamic acid. It could also help reduce sunspots caused by UV exposure, which can occur even to those meticulous with sunscreen application, or the appearance of brown marks that can form after a spot has healed (post-inflammatory hyperpigmentation).
The tranexamic acid can be used all year round, including in summer. It does not make the skin sensitive to the sun, though the daily application of sunscreen remains essential to prevent the appearance of new spots.
However, due to its hydrophilic nature and strong affinity for hydrogen bonds, its skin penetration is limited. This is why complementary techniques such as intradermal injections, microneedling, or optimized formulations are often explored to enhance its effectiveness.
By what mechanism does tranexamic acid even out the complexion?
Brown spots result from a localized overproduction of melanin. Reducing this synthesis is therefore a key factor for unifying the complexion. Unlike AHAs or other well-known brightening agents (such as kojic acid or arbutin), tranexamic acid has a unique mechanism of action by working at several complementary levels to unify the complexion:
When applied topically, tranexamic acid acts as a competitive inhibitor by binding to the lysine sites of plasminogen, preventing its conversion into plasmin in keratinocytes—a process triggered mainly by UV exposure or inflammation. This inhibition limits the production of arachidonic acid, whose increase activates tyrosinase (a key enzyme in melanogenesis) and stimulates melanin synthesis via its metabolite, prostaglandin E2. By limiting these signals, tranexamic acid reduces the activation of melanocytes and thus helps to alleviate pigmentation 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 melanocyte dendrites as well as the activity of tyrosinase.
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 such as tyrosinase. This mechanism also helps to decrease melanin production.
Due to its structure similar to tyrosine, tranexamic acid could also directly inhibit the activity of tyrosinase through a competitive mechanism.
Benefit No. 2: Tranexamic acid for a stronger skin barrier?
We understand how crucial an intact skin barrier is: it limits water loss, protects the skin from external aggressors, and prevents the entry of unwanted substances. However, certain conditions like 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-haemorrhagic properties, may also have an unexpected role: promoting 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 heightened expression of factors involved in vascularisation—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 are still not fully understood.
But how would tranexamic acid work to strengthen the skin barrier?
Available data suggest that tranexamic acid primarily functions by reducing the activity of serine proteases, enzymes involved in inflammation and the degradation of the skin barrier. This inhibition limits the activation of the PAR-2 receptor, thereby reducing intracellular calcium mobilisation in keratinocytes. This cascade slows the secretion of lamellar bodies, which are crucial for the formation of epidermal lipids, and supports the restoration of E-cadherin function, a protein essential for cell cohesion, thus contributing to the re-establishment of skin barrier homeostasis.
Furthermore, a study conducted in 2014 by WU P-L. and collaborators demonstrated that tranexamic acid accumulates in the stratum corneum, where it strengthens the cohesion between epidermal cells by increasing the expression of occludin, a key protein in tight junctions, accelerating the regeneration of the skin barrier and thus enhancing the appearance and health of the skin.
Benefit number three: Reduce redness and inflammation with tranexamic acid?
Tranexamic acid is not limited to a depigmenting role: its anti-inflammatory properties make it a useful ally for soothing 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 wet dressing soaked in TXA and a combination of microneedling and tranexamic acid-soaked dressing. After four sessions, all participants showed improvement, with better results observed in the group receiving the combined treatment.
Another study (2023) explored the efficacy of tranexamic acid micro-injections in the treatment of post-inflammatory erythema in individuals with 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 end of the protocol, a significant reduction in erythema intensity was observed, with no reported adverse effects.
Despite promising results, available studies remain limited and are conducted on small samples. Further research on a larger scale is necessary to establish robust recommendations.
By which mechanisms does tranexamic acid potentially exert its anti-inflammatory and vascular effects?
The anti-inflammatory and vasomodulatory properties of tranexamic acid are supported by 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, which are central cytokines in skin inflammatory processes.Regulation of cutaneous 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: Is Tranexamic Acid Effective Against Inflammatory Acne?
While mainly studied for its effects on pigmentation or the skin barrier, tranexamic acid could also be of interest in managing inflammatory acne. A preliminary randomized, double-blind, placebo-controlled clinical study evaluated the effectiveness of a serum containing 10% tranexamic acid in 18 patients with mild to moderate acne. After eight weeks of twice-daily application on one side of the face (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 could 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 required to confirm this therapeutic potential.
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