Also known as TXA, tranexamic is a synthetic derivative of the amino acid lysine, which is an amino acid that is used in the biosynthesis of proteins.

TXA is a versatile ingredient that is relatively new to the skincare market. You can take tranexamic acid orally as a tablet, apply it topically on your skin as a cream or serum, or have it injected into the lower layers of your skin.

Tranexamic acid tablets have actually been around for a long time and are used to reduce bleeding in situations like heavy menstrual periods, nosebleeds and surgery. In the last 5-10 years, dermatologists have also started using tranexamic acid for pigmentation disorders, especially melasma.

How does TXA work?

Most of the studies on tranexamic acid and skin have been on taking it orally for melasma. These studies suggest TXA takes on melasma in a number of different ways:

• It interferes with the interaction of pigment-producing melanocyte cells and regular keratinocyte skin cells
• It could decrease blood vessels in affected skin
• Tranexamic acid also decreases inflammatory mediators that stimulate pigment production after UV exposure
• It decreases the number of mast cells which release inflammatory mediators
• Since it’s structurally similar to tyrosine, it could also potentially slow down the production of melanin by tyrosinase as a competitive antagonist

It does a lot of these by slowing down the production of plasmin, an enzyme in blood that breaks up clotting material – which is also why it’s used to slow down bleeding.

Melasma

Oral tranexamic acid is effective for treating melasma. It’s generally taken at a dose of 250 to 1500 mg daily, for 8 to 12 weeks. It has few side effects which are mostly digestive however, it has the potential to increase the risk of blood clots.

Since it’s relatively new, oral tranexamic acid has fewer studies than other acids. Most of these studies have been on Asian patients and there’s limited data on other ethnicity’s. But it’s generally used when topical, peels and lasers don’t work well enough or aren’t suitable. It can also be used in combination with another melasma treatment.

Other types of pigmentation

Interestingly, oral tranexamic acid doesn’t seem to be as effective for other types of hyperpigmentation – in one study, it had almost no effect on freckles and age spots even though it faded melasma well. In a study where oral and topical tranexamic acid were used together, the skin around melasma patches darkened during treatment, which was thought to be due to increased sun exposure.

Oral tranexamic acid also doesn’t seem to work for preventing post-inflammatory hyperpigmentation after laser treatment.

Topical TXA

There is a lot less evidence for tranexamic acid applied topically on the skin but like for oral tranexamic acid, most of the studies on topical tranexamic acid have been done on melasma. 

A few studies have found that tranexamic acid at 3-5% is as effective at fading melasma as 2-4% hydroquinone, with fewer side effects. Injections of tranexamic acid into the dermal layer of the skin has also been found to work for melasma.

In other types of pigmentation, there’s even less evidence. There are a few studies where tranexamic acid faded hyper pigmentation when combined with other ingredients known to fade pigment (kojic acid, niacinamide, alpha arbutin), but none where tranexamic acid was used alone.

Since tranexamic acid acts on blood vessels as well as pigment to fade melasma (this could partly explain its greater effectiveness compared to ingredients that solely act on pigment), it could potentially help fade redness. But again, there’s only very scant evidence available:

• There’s one report of nightly 5% tranexamic acid reducing post-inflammatory erythema (redness after acne) in 6-8 weeks
• A couple of preliminary studies have also been done using 10% tranexamic acid for erythematotelangiectatic rosacea