Tranexamic Acid
Synthetic lysine derivative. Suppresses plasminogen activation in keratinocytes, reducing prostaglandin synthesis and melanocyte activity.
Evidence by route
Topical application
Small RCTs show improvement in melasma with 2–5% tranexamic acid. Effect is weaker than the oral route. Independent large studies are limited.
- Ebrahimi B et al. J Res Med Sci. 2014;19(8):753-757. PMID 25422661
Oral intake
Oral tranexamic acid is one of the most evidence-based treatments for melasma. A 2020 meta-analysis of 10 RCTs confirmed significant reductions in MASI and mMASI indices. Risk of thrombosis with prolonged use requires assessment in at-risk patients.
- Colferai MMT et al. J Cosmet Dermatol. 2019;18(6):1583-1589. PMID 30536592
How to read tiers A–F
- BLimited evidence. One RCT or several controlled studies with limitations
Tolerability and safety
- Working concentrations
- 2–5% topically; 500–750 mg/day orally (prescription only)
- Irritation potential
- Low
- Allergen risk
- Low
- Pregnancy
- Unknown
- Suitable for
- Normal, Dry, Sensitive, Combination, Oily
Combinations with other ingredients
About this ingredient
Tranexamic Acid (TXA) is a synthetic lysine derivative. In medicine it is used orally and injectably to stop bleeding (antifibrinolytic). Since the 2010s it has been used in dermatology for melasma and post-acne pigmentation. Mechanism. Suppresses plasminogen activation in keratinocytes. Reduces prostaglandin (PGE2) and arachidonic-acid synthesis – key inflammation mediators. Suppresses melanocyte signalling via the TYR pathway. Effective in post-inflammatory hyperpigmentation (PIH) and melasma. Where applied. Serums and creams for melasma and PIH (2-5%). Oral by prescription – 250-500 mg twice daily for 8-12 weeks. In Spain – Sesderma Azelac Ru, Mesoestetic Cumlaude Mela Stop, La Roche-Posay Mela B3. Evidence base. Bala 2018 meta-analysis in 1267 patients confirmed TXA efficacy in melasma (MASI reduction 30-40% over 8-12 weeks). Comparable to 4% hydroquinone with better tolerance and no depigmentation of healthy skin. The topical form is weaker than oral but systemically safer. Safety. CIR confirmed topical safety up to 5%. Non-sensitizing, non-comedogenic. Systemic absorption through intact skin is low. Thrombosis controversy. Oral TXA raises thromboembolism risk in patients with risk factors (V-Leiden, prothrombin 20210, contraceptives, smoking, obesity). Topical use does not carry this risk, but the beauty segment imports from pharma and cosmetic doctors sometimes prescribe high oral doses without screening. Pregnancy and lactation – use with caution. For topical cosmetic-range concentrations (up to 3%) safety data in pregnancy are limited, so AAD 2024 recommends avoidance. For gestational melasma first line is niacinamide, azelaic acid, adenosine, SPF 50+. Postpartum – TXA in standard regimens. Suitable for. Melasma, post-acne hyperpigmentation, post-procedure inflammatory pigmentation (laser, peels). Not first choice – usually after or alongside niacinamide and hydroquinone.
Frequently asked questions
Is Tranexamic Acid safe during pregnancy?
Safety data for Tranexamic Acid during pregnancy is insufficient. Best avoided when in doubt.
What skin types is Tranexamic Acid for?
Tranexamic Acid suits: normal, dry, sensitive, combination, oily.
What is Tranexamic Acid and what does it do in cosmetics?
Synthetic lysine derivative.
What's the INCI name for Tranexamic Acid?
The INCI name is Tranexamic Acid. It may also appear as: Trans-4-Aminomethylcyclohexane Carboxylic Acid.
What concentration of Tranexamic Acid is effective?
2–5% topically; 500–750 mg/day orally (prescription only)
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