Tranexamic Acid
Originally an oral medication for heavy menstrual bleeding, tranexamic acid (TXA) has emerged as one of the most effective treatments for melasma and stubborn hyperpigmentation that does not respond to conventional treatments. It works through a unique mechanism — blocking plasmin-mediated stimulation of melanocytes — that is different from tyrosinase inhibitors, making it an excellent combination partner.
Concentration & Usage
Topical: 2-5% in serum or cream, applied twice daily. Oral (off-label for melasma): 250 mg twice daily — requires medical supervision. Can be combined with other brightening agents. Results visible at 8-12 weeks. Especially effective for melasma.
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Mechanism of Action
Tranexamic acid (TXA) is a lysine analogue that competitively inhibits plasminogen activation—binding lysine-binding sites and preventing conversion to plasmin by tPA and uPA. Plasmin normally activates multiple pathways: converts latent TGF-beta to active form, stimulates keratinocyte release of arachidonic acid and prostaglandins (PGE2, PGF2-alpha), and increases SCF and bFGF—all stimulating melanocyte proliferation and melanogenesis. By blocking plasmin, TXA interrupts this paracrine cascade, reducing melanin through a mechanism independent of tyrosinase. TXA also inhibits VEGF and reduces angiogenesis—addressing melasma's vascular component. May reduce UV-induced plasmin in keratinocytes. This unique mechanism makes TXA synergistic with tyrosinase inhibitors for stubborn melasma.
Ingredient Interactions
Tranexamic acid blocks plasmin (reducing melanocyte stimulation) while niacinamide blocks melanosome transfer. Different mechanisms, additive brightening, no conflicts.
See our full Ingredient Interactions Guide for more combinations and timing strategies.
Regulatory Status
Oral tranexamic acid is a prescription medication (Lysteda, Cyklokapron). Topical forms are available as cosmetic ingredients OTC.
Risks & Safety
Rare
Topical form has minimal systemic absorption and low risk.
Compare Tranexamic Acid With
Research Papers
10Published: October 10, 2023
AI Summary
We found that TXA reduced IMQ-induced psoriasis-like erythema, thickness, scaling, and cumulative scores (erythema plus thickness plus scaling) on the back skin of BALB/c mice. Results further confirmed that in the ear skin of IMQ-induced mice, psoriasis biomarkers such as NLRP3, IL1β, Nrf2, and keratin 17 expression were downregulated by ...
Published: August 15, 2023
AI Summary
Tranexamic acid can be used by various routes of administration including oral, topical and intradermal injection, and in combination with other treatment methods. This review article presents evidence for the effectiveness of tranexamic acid in the treatment of various skin disorders.
Published: June 20, 2018
AI Summary
Melasma is a common acquired disorder of hyperpigmentation that commonly affects those with skin of color. Tranexamic acid (TXA) is a novel treatment for melasma that has a multimodal mechanism of action.
Published: September 24, 2024
AI Summary
Based on its good hemostatic efficacy, it is mainly used clinically for bleeding in trauma, various types of surgical and dental procedures and prevention of bleeding in patients with hemophilia. We review the clinical use of TXA in hyperpigmentation and telangiectatic disorders other than melasma, such as post-inflammatory hyperpigmentation, Ri...
Published: June 22, 2022
AI Summary
Therapeutic management of melasma is challenging, with high recurrence rates which significant impacts on the quality of life. Combination therapies, either in double or triple combinations yielded the best results when compared to single terapies.
Published: July 5, 2017
AI Summary
Side-effects were minor, with a few cases reporting hypo-menorrhoea, mild abdominal discomfort, and transient skin irritation. These results support the efficacy and safety of tranexamic acid, either alone or as an adjuvant to routine treatment modalities for melasma.
Published: March 29, 2019
AI Summary
We found that cancer development was ameliorated by administration of tranexamic acid. These results indicated that the nonmelanoma skin cancer induced by DMBA+UVA long-term irradiation is ameliorated by tranexamic acid through regulation of the plasmin/macrophage/IL-6/STAT3/cyclin D signal transmission pathway.
Published: September 6, 2024
AI Summary
Papulopustular rosacea (PPR) is a chronic inflammatory disease with a significant impact on facial aesthetics. An impaired skin barrier is an important factor in the development and exacerbation of PPR.
Published: September 18, 2024
AI Summary
Melasma is a chronic, acquired disorder of focal hypermelanosis that carries significant psychosocial impact and is challenging for both the patient and the treating practitioner to manage in the medium to long term.
Published: August 10, 2023
AI Summary
Tranexamic acid is a cost-effective intervention for the prevention of postpartum hemorrhage among women who undergo cesarean delivery, but the evidence to support its use is conflicting. We conducted this meta-analysis to evaluate the efficacy and safety of tranexamic acid in low- and high-risk ces
Frequently Asked Questions
What is Tranexamic Acid used for?
Originally an oral medication for heavy menstrual bleeding, tranexamic acid (TXA) has emerged as one of the most effective treatments for melasma and stubborn hyperpigmentation that does not respond to conventional treatments. It works through a unique mechanism — blocking plasmin-mediated stimulation of melanocytes — that is different from tyrosinase inhibitors, making it an excellent combination partner.
What are the side effects of Tranexamic Acid?
Common (topical): Well-tolerated. Mild dryness or irritation. Serious (oral): Increased risk of blood clots (thromboembolism) — contraindicated in people with clotting disorders or on hormonal contraceptives. Rare: Topical form has minimal systemic absorption and low risk.
How is Tranexamic Acid administered?
Tranexamic Acid is administered via topical (serum, cream) or oral (tablets, off-label). topical preferred for safety. oral is more effective but carries systemic risks..
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Hydroquinone
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