Tranexamic Acid: the powerful active for dark spots and uneven skin tone

• Common name: Tranexamic acid

• Category: Synthetic derivative of the amino acid lysine

• Origin: Synthetic (derived from lysine through structural modification)

• Form: White crystalline powder

• INCI Name: Tranexamic Acid

• For: Dull complexions, pigment spots, skin prone to pigmentation disorders (lentigo, melasma, etc.)

• Functions: Skin-evening, brightening, soothing, anti-inflammatory

• Dosage in custom-formulated cosmetics: 1 to 3%, to be incorporated into the aqueous phase at less than 50°C

• Solubility: Water-soluble

Tranexamic acid is a synthetic derivative of lysine, an essential amino acid, naturally present in our bodies. It was initially developed in the 1960s as an antifibrinolytic agent (limiting clot breakdown, or fibrinolysis, which is the final stage of the normal clotting process). In cosmetics, it is valued for its ability to inhibit tyrosinase (a key enzyme in melanin production) and inflammatory factors.

Its mechanism of action is primarily based on:

• Inhibiting activated plasminogen, thereby reducing inflammation and associated hyperpigmentation: In fact, tranexamic acid (TXA) acts by inhibiting the conversion of plasminogen into plasmin, an enzyme involved in inflammatory processes and the production of melanin. By blocking this conversion, TXA reduces skin inflammation and the associated hyperpigmentation, particularly by disrupting the interaction between keratinocytes and melanocytes.

• Indirect inhibition of tyrosinase, thereby limiting melanin production: TXA indirectly inhibits tyrosinase, a key enzyme in melanin synthesis. This activation leads to a decrease in the expression of tyrosinase and proteins associated with melanogenesis, thereby reducing the production of melanin, which is responsible for skin pigmentation. Dark spots result from excessive melanin production in certain areas of the skin; reducing its production helps combat dark spots.

• Local anti-inflammatory action, beneficial for skin prone to redness: TXA has anti-inflammatory properties that make it beneficial for skin prone to redness. It works by inhibiting the activity of plasmin, a proteolytic enzyme (which breaks down proteins) primarily known for its role in the fibrinolytic system (the body’s ability to dissolve blood clots). Plasmin breaks down the extracellular matrix—such as collagen or fibrin—which promotes local inflammation. Inhibiting this enzyme thus reduces the release of inflammatory mediators such as prostaglandins and cytokines, helping to soothe the skin and reduce redness.

Note

There are also modified forms of tranexamic acid, such as encapsulated versions (liposomes, niosomes) or those combined with other active ingredients (kojic acid, niacinamide) to improve their bioavailability.

Given TXA’s main actions, several resulting benefits for the skin can be noted: 

Evens out the complexion

Tranexamic acid works on two complementary levels to even out the complexion:

• Upstream, it inhibits the conversion of plasminogen into plasmin. By limiting these pro-inflammatory signals, it slows down the activation of melanocytes by keratinocytes, thereby preventing inflammation-related overproduction of melanin (particularly in cases of post-inflammatory hyperpigmentation).

• Downstream, it indirectly acts on tyrosinase, the key enzyme in melanogenesis. Studies have shown that TXA activates the ERK pathway and the autophagy process, leading to a reduction in the expression of tyrosinase and pigmentation-associated proteins in melanocytes.

Note

These two combined mechanisms allow tranexamic acid to act both to prevent and correct pigmentation spots, making the complexion visibly more even without compromising the skin barrier.

Reduces pigmentation spots

Tranexamic acid is known for its effectiveness on established hyperpigmentation spots, particularly sunspots, post-acne spots, and hormonal spots (such as melasma). By blocking the cellular signals that activate melanocytes, it helps gradually fade existing spots. Its action is enhanced when combined with other skin-brightening ingredients (kojic acid, niacinamide).

Prevents post-inflammatory hyperpigmentation (PIH)

After skin trauma (acne, hair removal, sun exposure, chemical peels, laser treatments), the skin may develop residual dark spots. Thanks to its anti-inflammatory and anti-melanogenesis effects, tranexamic acid is particularly effective in preventing post-inflammatory hyperpigmentation. It is used for this purpose in aesthetic dermatology in the weeks following invasive procedures.

Brightens dull complexions

Beyond its effect on dark spots, tranexamic acid revitalises tired or dull complexions. It works indirectly by improving pigment regulation and underlying micro-inflammation, which can make the skin appear brighter. When combined with active ingredients like niacinamide or azelaic acid, it delivers a natural “glow” without irritating sensitive skin.

Soothes sensitive skin

The anti-inflammatory effect of tranexamic acid isn’t just beneficial for pigmentation. By limiting the production of cytokines and inflammatory mediators, it helps soothe reactive or redness-prone skin. This makes it a valuable ingredient in skincare for sensitive or rosacea-prone skin, working in tandem with other soothing active ingredients such as centella asiatica or licorice.

In cosmetics

1. Skin-evening or anti-dark spot serums: Used to target pigmentation spots (sunspots, post-acne marks, mild melasma), tranexamic acid regulates melanin production and helps prevent pigmentation from recurring.

2. Post-acne or post-laser care: It helps prevent or reduce post-inflammatory hyperpigmentation by soothing the skin and blocking inflammatory signals that stimulate melanocytes.

3. Anti-dullness day creams: By improving skin tone evenness and reducing pigmentation irregularities, it restores the face’s radiance.

4. Radiance masks: Incorporated into hydrating or smoothing masks, it acts on the surface to fade shadows and dark areas, providing a brightening effect in just a few applications!

5. Eye contour care: Useful in treatments targeting melanin-based pigmented dark circles (so-called "brown" dark circles), as it reduces localised melanin production. Note: not suitable for bluish dark circles related to microcirculation, as this active ingredient would have no effect on this issue!

In aesthetic medicine

1. Mesotherapy or microneedling injections: When administered intradermally or combined with microneedling techniques, tranexamic acid penetrates deeper to reduce moderate to severe melasma or pigment spots resistant to topical treatments. Its targeted action is faster but requires strict medical supervision to avoid side effects.

We do not yet offer pure tranexamic acid in our catalogue. However, you can find alternatives with similar benefits in:

Licorice Extract: soothes and evens out skin tone; it’s found in our Hordatine and Licorice Extract Anti-Dark Spot Serum. This clinically proven serum, specially formulated for all skin tones, offers a triple action: anti-dark spot, anti-ageing, and radiance. Its formula combines Hordatine, Niacinamide, and Licorice Extract to target dark spots on all skin types. For a luminous, even complexion.

Niacinamide: regulates melanin production and strengthens the skin barrier. You can find niacinamide in our 10% Niacinamide, Copper, and Zinc Concentrated Serum or as an active ingredient for your custom formulations. Our proven-effective serum tightens pores, regulates sebum production, prevents blemishes, and reduces redness and dark spots. Enriched with hydrating hyaluronic acid, it evens out skin tone and refines skin texture. When used as a hair care product, Niacinamide stimulates keratin production, strengthens hair, restores volume, and balances the scalp. For flawless skin and beautiful hair!

Retinal: comprehensive anti-ageing with anti-inflammatory action. Check out our Optimised Retinal Concentrated Face Serum. This serum is concentrated in retinal, an essential multi-targeted active ingredient against the signs of ageing. It firms the skin, reduces wrinkles and fine lines, fades dark spots, and brightens the complexion. Well-known for its effectiveness against blemishes, it has anti-inflammatory properties, reduces impurities, purifies, evens out skin tone, and helps regulate oily skin.

According to scientific studies, TXA is compatible with:

• Niacinamide (vitamin B3)

• Kojic acid

• Stabilised vitamin C (ascorbyl glucoside)

Avoid combining with (risk of irritation):

• Exfoliating acids that are too potent with a low pH (such as strong AHAs)

• High-concentration retinoids without supervision

Away from light, moisture and heat: It is recommended to store tranexamic acid in a dry place, away from moisture, heat and light.

Room temperature < 25°C: Although specific recommendations for tranexamic acid are limited, it is generally recommended to store sensitive cosmetic ingredients at a room temperature below 25°C to preserve their stability.

To prevent contamination or degradation, it is important to store tranexamic acid in a tightly closed container.

• Do not use undiluted on the skin

• Not recommended for direct application on sensitive, irritated skin, or skin with open wounds.

• Do not exceed 3% in your custom cosmetic formulations

• For external use only.

• Always perform a patch test on the inner elbow 24 hours before use

• Introduce gradually into your routine, especially for sensitive skin (start at 1% or 2%).

• If a reaction occurs (redness, itching, discomfort), space out applications or discontinue use.

• Daily sun protection is essential while using tranexamic acid skincare products, as they may increase skin sensitivity to UV rays.

I'm Delphine Duc, a biological engineer specialising in cosmetology, and I've been passionate about the field of cosmetics for almost 10 years. I started making my own homemade cosmetics using Aroma Zone products to tackle my skin problems. Eventually, I decided to train as a cosmetologist and ultimately to create a bespoke cosmetics brand to address everyone’s individual skin concerns.