Tranexamic Acid: Which Active Ingredients Should It Be Combined With?

The peptides belong to a broad family of small chains of amino acids, whose effects vary according to their structure and biological function. In cosmetics, signal peptides, which stimulate the synthesis of collagen and elastin, inhibitory neurotransmitter peptides used to smooth the appearance of expression lines, and carrier peptides capable of delivering essential trace elements to skin metabolism. Their growing popularity is due to their good tolerability, versatility, and ability to act on various markers of skin aging, from loss of firmness to lack of radiance.

Combining peptides with tranexamic acid is beneficial for improving skin tone uniformity and overall skin quality.

Depending on the peptide used, the combination can help reinforce barrier function, smooth wrinkles, or improve skin radiance, while the tranexamic acid acts more specifically on the mechanisms involved in hyperpigmentation. For example, at Typology, we decided to combine tranexamic acid with tetrapeptide-2 in our wrinkle and firmness-loss serum. This combination not only fades brown spots but also alleviates signs of skin aging.

The arbutin acid, and more specifically alpha-arbutin, is an active ingredient recognized for its targeted action on hyperpigmentation. A natural derivative of hydroquinone, it primarily works by inhibiting tyrosinase activity, a key enzyme in melanogenesis, thereby limiting the excessive production of melanin. Appreciated for its gradual effectiveness and good tolerability, the arbutin acid is often used to fade pigmentation spots, melasma, and uneven skin tone, even on sensitive skin.

In this context, it may be appropriate to combine alpha-arbutin with tranexamic acid to target different mechanisms involved in hyperpigmentation.

A clinical study conducted in Indonesia on 66 female patients with melasma thus evaluated a formulation combining 3% tranexamic acid, 2% arbutin, 4% niacinamide, and 2% ferment of Galactomyces, known for its soothing properties. Participants applied a serum followed by a cream containing these actives for four weeks. The progression of melasma was monitored using a clinical severity score (MSS) and image analysis tools to assess epidermal and dermal pigmentation. The results showed a overall improvement in hyperpigmentation, detectable as early as the second week of use, suggesting a clinical benefit for this combination of actives.

It should be noted, however, that the study examined a multi-active formulation that did not consist solely of tranexamic acid and alpha-arbutin.

The hydroquinone has long remained the reference molecule in managing hyperpigmentation. Its mechanism relies on potent tyrosinase inhibition and, at higher doses or with prolonged use, on a direct cytotoxic action against melanocytes. However, this marked efficacy is accompanied by numerous controversies: risks of irritation, contact dermatitis, post-inflammatory hyperpigmentation... These adverse effects have led to strict regulation of hydroquinone, and even its ban in cosmetic products in several countries, restricting its use to medical contexts under dermatological supervision.

Some evidence suggests that it is possible to combine hydroquinone and tranexamic acid to act on pigmentary spots at different levels.

However, in practice, this combination is most often used in the form of tranexamic acid orally, combined with topical hydroquinone, although some publications also report the topical use of tranexamic acid. These protocols are generally reserved for severe or resistant forms of melasma and are part of a strictly medical management.

The vitamin C, or ascorbic acid, is a key active ingredient in cosmetics prized for its antioxidant properties and its role in regulating pigmentation. It neutralizes free radicals, notably those induced by UV rays and pollution, limits the oxidation of existing melanin, and indirectly contributes to tyrosinase inhibition. At the same time, it supports collagen synthesis, making it an exceptionally versatile ingredient.

In this context, combining vitamin C and tranexamic acid may seem appropriate.

This complementarity was specifically explored in a clinical study conducted in patients with resistant melasma. The trial enrolled ten women who were followed for eight weeks. Each evening, participants applied a topical formulation containing 2% tranexamic acid and 2% vitamin C. Efficacy was assessed using the MASI score and the MelasQoL questionnaire, which measures the impact of the condition on quality of life. The results showed a progressive and significant reduction in MASI score over the weeks, accompanied by an improvement in quality of life reported by the patients. Notably, no adverse reactions were observed during the study, suggesting that this combination was well tolerated.

The kojic acid is a historically widely used active ingredient for targeting hyperpigmentation. Of fungal origin, it primarily functions by chelating the copper ions required for tyrosinase activity, thereby slowing melanin production. Despite this well-documented efficacy, its use in cosmetics is debated. Kojic acid is indeed suspected of being irritating and sensitizing, with a significant allergenic potential. Concerns have also been raised about a possible endocrine-disrupting effect, as well as signals of carcinogenicity or mutagenicity observed in certain experimental models, leading to strict regulation of its permissible concentrations.

Nevertheless, kojic acid continues to be combined with other depigmenting agents, such as tranexamic acid, to enhance its overall effect on pigmented spots.

This combination was evaluated in a 12-week clinical study involving 55 women with melasma. The serum tested contained 3% tranexamic acid, 1% kojic acid, and 5% niacinamide, and was applied daily. Efficacy was monitored using a mexameter, a device that quantifies the melanin index. The results showed a significant improvement in the appearance of brown spots.

As a precautionary measure, at Typology, we have excluded kojic acid from our formulations.

The azelaic acid is a naturally derived active ingredient that exhibits anti-inflammatory, antibacterial, and depigmenting properties. Versatile, it is incorporated into various skincare formulations, for example intended for individuals prone to blemishes or rosacea.

The benefit of combining azelaic acid with tranexamic acid was explored in a study involving 33 women with moderate to severe skin hyperpigmentation. Participants applied a cream formulated with these two actives daily for six weeks, although their exact concentrations were not specified. Efficacy was assessed using standardized photography, clinical dermatological evaluation, and software-assisted analysis. By the end of the study, a global and visible improvement in skin pigmentation was observed, suggesting that the tranexamic acid–azelaic acid combination may be of interest for pigmentary disorders, even though the absence of concentration data and quantified outcomes calls for caution in interpreting these findings.

The glycolic acid is a widely used alpha-hydroxy acid (AHA) in cosmetics and dermatology for its exfoliating action. Thanks to its low molecular weight (76.05 g/mol), it penetrates the stratum corneum easily and promotes cellular renewal, which helps gradually fade pigmentation spots and soften wrinkles.

Some studies have examined the combination of tranexamic acid and glycolic acid, hypothesizing a complementary effect between melanogenesis inhibition and the removal of superficial skin cells. However, the results did not show any significant benefit compared to using glycolic acid alone. Moreover, in practice, this combination can prove too aggressive for the skin barrier. Therefore, despite its theoretical interest, we do not recommend combining glycolic acid and tranexamic acid within the same skincare routine.

The benzoyl peroxide is a reference active ingredient in the acne management, notably for its antibacterial properties against Cutibacterium acnes. It also exerts a mild keratolytic and anti-inflammatory effect, which helps limit pore obstruction. On the other hand, it is a potent agent often associated with significant skin dryness, irritation, and a transient impairment of the skin barrier, particularly during the first weeks of use.

Although the idea of combining benzoyl peroxide with tranexamic acid may seem pertinent for simultaneously targeting acne and post-inflammatory hyperpigmentation, to date no study has evaluated this combination.

In practice, it is generally preferable to avoid using benzoyl peroxide and tranexamic acid together. Indeed, benzoyl peroxide is already highly drying and potentially irritating, and it is most often recommended to use it alone, pairing it only with hydrating, nourishing, and soothing agents to preserve skin tolerance. Adding another pigment-targeting active, such as tranexamic acid, could increase the risk of discomfort without a clearly demonstrated benefit.

The lactic acid belongs to the AHA family and is naturally present in the skin’s natural moisturizing factor (NMF). In cosmetics, it is valued for its dual action: gentle exfoliation and hydration. By promoting corneocyte shedding, it helps improve skin radiance and evenness, while supporting hydration through its humectant properties. Compared to other AHAs, such as glycolic acid, lactic acid is generally well tolerated, making it a compelling active ingredient for sensitive skin.

To date, no study has demonstrated a synergistic effect between lactic acid and tranexamic acid.

Nevertheless, there is no known contraindication to their combined use. Because lactic acid is generally well tolerated, it can be incorporated into a regimen that includes tranexamic acid—particularly to enhance skin texture and radiance while targeting hyperpigmentation.

The salicylic acid is a beta-hydroxy acid (BHA) primarily used for its keratolytic, comedolytic, and anti-inflammatory properties. Lipophilic, it easily penetrates pores, where it promotes the removal of excess sebum and dead skin cells, making it a reference ingredient in the management of acne-prone skin. By limiting inflammation and the persistence of lesions, salicylic acid can indirectly contribute to reducing the risk of post-inflammatory hyperpigmentation. It can be assumed that salicylic acid and tranexamic acid could act synergistically to prevent or reduce post-inflammatory hyperpigmentation or brown spots in general.

In the absence of clinical studies on the subject, the potential synergy between salicylic acid and tranexamic acid remains hypothetical.

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• WANG J. V. & al. Tranexamic acid for melasma: Evaluating the various formulations. Journal of Clinical and Aesthetic Dermatology (2019).

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• ANWAR A. I. & al. Effectiveness of application of serum and cream containing combination of tranexamic acid, galactomyces ferment filtrate, niacinamide, and alpha arbutin using layering technique in melasma. Hong Kong Journal of Dermatology and Venereology (2020).

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• TENG G. & al. Oral tranexamic acid, low-fluence intense pulsed light, and glycolic acid for the treatment of mixed melasma: An observational study. Medicine (2025).