This article details some modest benefits to rosacea symptoms experienced by users of 3% topical tranexamic acid. Trialists of the active topical experienced an improvement in stratum corneum function and in “clinical signs and symptoms of rosacea”.

The authors further detail a suggested pathway of how tranexaminc acid benfits rosacea. See the full text link below for more details.

“The possible pathogenic role of the permeability barrier in rosacea and the mechanisms by which tranexamic acid benefits rosacea. The impaired permeability barrier function can increase serine protease (SP) activity, resulting from the elevation of pH. Activation of SP activates SP-PAR2 and increases the production of active forms of LL-37, which in turn induces inflammatory cell infiltrate and angiogenesis. Activation of SP-PAR2 pathway can cause further damage in the permeability barrier via the inhibition of lamellar body secretion and E-cadherin adhesion. In addition, defective permeability barrier alone could increase LL-37”.

Tranexamic acid is a synthetic analog of the amino acid lysine. Lysine has been associated with rosacea for many years but so far any evidence hasn’t risen above anecdotal level.

Paula’s Choice tells us

TRANEXAMIC ACID A synthetic amino acid that functions as a skin-conditioning agent and astringent. Derived from the amino acid lysine, it is used in during surgery to control bleeding, including from dental surgery. In cosmetics, it functions on skin as a barrier repair ingredient and seems able to help skin recover from damage (Source: International Jounal of Dermatology, August 2013, ePublication). There’s a growing body of research showing that tranexamic acid also has an inhibitory effect on melanin (skin pigment) production, meaning topical applications of effective amounts (5%) may improve brown skin discolorations associated with melasma (Sources: Journal of the European Academy of Dermatology and Venereology, August 2013, pages 1,035-1,039; and Journal of Cosmetic and Laser Therapy, June 2012, pages 150-154).

Article Abstract

Topical tranexamic acid improves the permeability barrier in rosacea DERMATOLOGICA SINICA, 33 (2015) 112-117 Shaomin Zhong, Nan Sun, Huixian Liu, Yueqing Niu, Can Chen, Yan Wu, Department of Dermatology, Peking University First Hospital, Beijing, China Objective: To evaluate the influence of tranexamic acid on epidermal permeability barrier function in rosacea and its potential mechanisms. Methods: A randomized, vehicle controlled, split-face study was performed on 30 rosacea patients. This study involved 2 weeks of 3% tranexamic acid solution treatment and vehicle control treatment. Skin physiological parameters, including skin surface pH, stratum corneum hydration, and transepidermal water loss, were measured. The expression of protease-activated receptor 2 (PAR-2) in rosacea and normal skin samples was assessed with immunohistochemical staining. The expression of PAR-2 in HaCaT keratinocytes was determined using reverse transcription polymerase chain reaction after stimulation with tranexamic acid. Changes of intracellular calcium induced by PAR-2 activation were measured using Fluo-4 NW calcium assay. Results: Individuals with rosacea expressed a higher baseline level of PAR-2 compared with normal skin. Tranexamic acid improved the permeability barrier function in rosacea patients and inhibited calcium mobilization in keratinocytes induced by PAR-2 activation. The PAR-2 expression was not altered by tranexamic acid stimulation. Conclusion: Topical tranexamic acid could improve the epidermal permeability barrier function and clinical signs of rosacea, likely resulting from inhibition of PAR-2 activation and consequent calcium influx. Thus, tranexamic acid could serve as an adjuvant therapy for rosacea.

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