Tranexamic Acid for Hyperpigmentation Explained

22 June 2022


Is tranexamic acid the next big thing in skincare for fading dark spots? With brands like Skinceuticals and The Inkey List adding tranexamic acid to their product line up, this ingredient is set to get its moment in the spotlight.


Will tranexamic acid be a salve for hyperpigmentation or yet another passing fad (RIP salmon DNA)? Here’s a look at the science and data on tranexamic acid in skincare and for treating dark spots.


How does tranexamic acid work?




Tranexamic acid is an ingredient that is relatively new to the skincare scene. It was discovered incidentally in 1979 by Nijo Sadako who used oral tranexamic acid to treat a patient with urticaria. Serendipitously, the patient’s melasma lightened after 2-3 weeks. This finding paved the way for work treating melasma with oral tranexamic acid.


Despite its name, tranexamic acid is not an acid that some of us might associate with chemical peels like AHAs and BHAs. Tranexamic acid is a synthetic derivative of the amino acid, Lysine. For the purpose of treating hyperpigmentation (more specifically, melasma), tranexamic acid can be consumed orally, applied to skin (skincare) or injected into the skin (microneedling)


Related blogpost:

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Outside of dermatology, tranexamic acid has been used mostly to arrest heavy bleeding. In the US, tranexamic acid has received US FDA approval for heavy menstrual bleeding and in tooth extractions for patients with hemophilia. Needless to say, tranexamic acid should be avoided in patients with clotting disorders.



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Melasma is a specific type of hyperpigmentation characterised by dark patches with irregular borders on the face. Euphemistically known as the “mask of pregnancy”, the triggers for melasma have been linked to pregnancy, use of oral contraceptives and sun exposure.


Of all the types of hyperpigmentation, melasma is one of the most challenging types to treat. The exact pathogenesis of melasma remains unclear; but multiple interactions including melanin synthesis, transfer of melanin, inflammation and blood vessel interaction are thought to be involved.


Related blogposts:

Hyperpigmentation Disorders: Types, Causes & Treatments

How to Treat Hyperpigmentation and Dark Spots with Skincare





Before the discovery of its hyperpigmentation lightening effects, tranexamic acid was used to treat heavy blood loss. In the blood, tranexamic acid blocks the conversion of a protein called plasminogen to plasmin. Plasmin is an enzyme that dissolves blood clots, hence high levels of plasmin cause excessive blood loss. By blocking this step in the formation of plasmin, tranexamic acid stops bleeding.


In the skin, plasminogen is also present. Tranexamic acid blocks the binding of plasminogen to the skin cells, thereby stopping the release of inflammatory mediators (arachidonic acid and prostaglandins) which stimulate pigmentation formation. Secondly, tranexamic acid also inhibits UV induced plasmin activity, inflammation and blood vessel growth; all of which contribute to melasma formation.


Additionally, tranexamic acid’s molecular structure resembles tyrosinase. In the skin, tyrosinase is an enzyme involved in the key step of formation of melanin. Because of this resemblance, tranexamic acid reduces melanin synthesis by tyrosinase through competitive antagonism.




When considering tranexamic acid’s effectiveness in studies, two aspects need to be considered:

1) The specific type of dark spots that were treated; and

2) The route of administration i.e. oral vs topical (skincare)


Tranexamic acid does not work for all types of dark spots

Most of the studies on tranexamic acid’s hyperpigmentation fading effects on the skin were conducted on melasma. One study that looked at tranexamic acid’s effects on post inflammatory hyperpigmentation showed no significant improvement. Another study showed that melasma did not improve freckles.



Route of administration: Oral vs Topical (Skincare)


Oral tranexamic acid and melasma

Most of the data and studies on tranexamic acid have been based on oral tranexamic acid in studies. These studies show that at low doses and short durations (2-3 months), oral tranexamic acid is effective in fading melasma, whether alone or in combination with other treatments such as Q-switch laser. Based on these studies, oral tranexamic acid is recommended for patients with melasma resistant to conventional treatments like skincare, chemical peels and lasers.


Related blogpost:

10 Things to Know Before Getting Laser for Pigmentation


Topical tranexamic acid and melasma

The data of topical tranexamic acid i.e. tranexamic acid however, is less robust. A small few studies that used 3-5% topical tranexamic acid showed efficacies similar to the current “gold standard” for treating melasma, hydroquinone. Side effects from topical tranexamic acid were less than with applying hydroquinone to the skin.


Larger, randomised controlled trials and long term studies are required to ascertain the roles of oral and topical tranexamic acid in the treatment of melasma and other types of hyperpigmentation. More information is also needed to establish optimum dosing, duration, long term effects and relapse rates regarding tranexamic acid therapy.




Despite all the hype and rush for skincare companies to introduce tranexamic acid into their products, here’s what you need to know before getting started- the limitations:

• Most studies show that tranexamic acid is effective for melasma, and not other types of hyperpigmentation. If you belong to the latter category, you might want to use another ingredient instead of tranexamic acid.

• Most of the studies were conducted in Asian patients. For non-Asian patients, the efficacy of oral and tranexamic acid is still unclear although it is likely that the same findings can be extrapolated

• Oral vs topical tranexamic acid in skincare- the efficacy of one over the other has yet to be established. There is no published study (at time of this writing) that compares one route of administration over the other.

• Oral tranexamic acid at low doses and short periods (8-12 weeks) is safe. Long term safety is not known

• There is no consensus on optimum dosing and duration on both oral and topical tranexamic acid for melasma.





First of all, get your dark spots checked out by a doctor to determine the diagnosis. Not all dark spots are melasma. If you have melasma, there may be a role for tranexamic acid for fading your blemishes. Otherwise, you’re better off picking other active ingredients. Please read How to Lighten Hyperpigmentation and Dark Spots with Skincare for more ingredients that treat dark spots.


Oral tranexamic acid is a medication that is used to treat recalcitrant melasma or melasma that is not responding well to conventional treatments. It is not without its risks like blood clots, so if you have a higher tendency to form blood clots; conventional creams like retinoids, hydroquinone and laser treatments will be a safer alternative.


Topical tranexamic acid/ skincare seems to lighten melasma but its role in the treatment protocols is a lot less clear. Here’s what you need to know before purchasing tranexamic acid skincare products



• Choose concentrations of tranexamic acid of 3-5% in the skincare product.

• Tranexamic acid can be used twice a day.

• Look for products that combine tranexamic acid with other hyperpigmentation lighteners (e.g. kojic acid) for synergistic improvement in melasma.

• Combination therapy with laser and chemical peels while using tranexamic acid for faster results.


Related blogposts:

10 Things to Know Before Getting Laser for Your Hyperpigmentation

The Truth About Chemical Peels



My review of Skinceuticals’ Discolouration Defense


Ending off this blogpost with a review of a skincare product review. Keeping this succinct: Skinceuticals’ Discolouration Defense is a dark spot treatment; and it contains 3% tranexamic acid, 5% niacinamide and 1% kojic acid.


Related blogpost:

Niacinamide: A Versatile Skincare Ingredient Your Skincare Will Thank You For


Skinceuticals is US skincare brand founded in 1994. The brand is most well known for being a pioneer in antioxidant formulations with formulations backed by empirical research. In Singapore, Skinceuticals’ products are available in dermatologist and aesthetic clinics.


The Good about Skinceuticals’ Discolouration Defense


The combination of ingredients for correction of hyperpigmentation address different key pathways of hyperpigmentation formation.


The Bad about Skinceuticals’ Discolouration Defense


The proof is in the pudding- and with Skinceuticals’ Discolouration Defense, it was a miss for me. Despite the hype and popularity of this product (bought it cos FOMO), there was no visible reduction in my dark spots despite consistent use. I have melasma, which has responded well to over the counter products like vitamin C; but my melasma remained the same with Skinceuticals’ Discolouration Defense. I honestly wished this product worked for me; it was a disappointment for me as Skinceuticals’ Discolouration Defense cost approximately $150.


Even with the niacinamide in Skinceuticals’ Discoloration Defense; I did not notice any calming/ anti-inflammatory effects or sebum reducing outcomes. Niacinamide has always worked well for me; and The Ordinary’s Niacinamide serum (which costs $10) is more effective on my skin.


All in all, I’ve had better outcomes with more affordable products, so I will not be repurchasing Skinceuticals’ Discolouration Defense.


Conclusion on tranexamic acid for treating hyperpigmentation


In short, tranexamic acid can help to lighten dark spots, but with some caveats. It only seems that oral tranexamic acid works, but for a specific type of hyperpigmentation (melasma). The efficacy of topical tranexamic acid (skincare) remains uncertain.



1. Tranexamic acid in treatment of melasma: A comprehensive review of clinical studies. Taraz et al. Dermatol Ther. 2017 May;30(3).

2. Tranexamic Acid in the Treatment of Melasma: A Review of the Literature. Perper et al. Am J Clin Dermatol. 2017 Jun;18(3):373-381.

3. Oral Tranexamic Acid for the Treatment of Melasma: A Review. Bala et al. Dermatol Surg. 2018 Jun;44(6):814-825

4. The emerging importance of tranexamic acid in dermatology. Forbat el al. Clin Exp Dermatol. 2020 Jun;45(4):445-449.

5. Treatment of melasma with oral administration of tranexamic acid. Wu et al. Aesthetic Plast Surg. 2012 Aug;36(4):964-70.



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