Expanding the Role of Oral Tranexamic Acid in Dermatology: Anti-Pigment, Anti-Inflammatory, and Barrier Repair

During his presentation on the first day of Dermatology Week, Dr Lal, director of cosmetic dermatology at Affiliated Dermatology in Scottsdale, AZ, provided an in-depth review of oral tranexamic acid (TXA) as a versatile and underutilized treatment in dermatology. The talk outlined TXA’s mechanisms of action, clinical evidence, and prescribing guidance for dermatologic indications beyond its traditional use.

Originally approved for heavy menstrual bleeding and surgical hemostasis in hemophilia, TXA is a synthetic amino acid that competitively inhibits plasminogen activation, reducing fibrinolysis. In dermatology, it is gaining attention for its impact on pigmentation, inflammation, angiogenesis, and skin barrier recovery.

Dr Lal highlighted TXA’s mechanistic parallels with tyrosine, suggesting its potential in melanin pathway modulation. “It’s a very similar molecule to tyrosine,” he explained, “and so there’s some role as to this synthetic amino acid and how it pertains to pigment production.”

TXA has shown an ability to reduce tyrosinase activity, particularly in keratinocyte-melanocyte cocultures, implicating it in the treatment of melasma and post-inflammatory hyperpigmentation (PIH). Importantly, TXA also demonstrated anti-angiogenic effects. In vivo studies revealed reduced CD31-positive vascular structures and HMB-45-positive melanocytes following treatment. Additionally, in a rosacea mouse model, TXA downregulated inflammatory markers, including IL-6, TNF-α, and MMP-9.

“We often don’t think of tranexamic acid as being an anti-inflammatory medication,” said Dr Lal, “but it does reduce inflammation.”

TXA’s ability to accelerate skin barrier recovery further expands its utility. In models using UVB and sodium lauryl sulfate to disrupt the skin, TXA improved occludin density and decreased transepidermal water loss, suggesting therapeutic value in conditions with compromised barrier function.

Dr Lal provided multiple clinical examples of oral TXA in action—most notably for melasma, rosacea, PIH, and lichen planus pigmentosus. He emphasized the importance of treatment duration and combination therapy.

“Typically, when I’m treating patients, I’m using it for 3 months and I’m using it with other agents—we’re using hydroquinone, we’re using sunscreen,” he noted.

For dermatologists managing complex pigmentary disorders or rosacea with vascular and inflammatory components, oral TXA offers a compelling adjunct—one supported by a growing body of translational and clinical data.

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Reference
Lal K. Oral tranexamic acid in dermatology. Presented at: Dermatology Week; May 14–16, 2025; Virtual.