tranexamic acid for melasma and skin lightening

Tranexamic Acid: A New Frontier in Compounded Uses and Opportunities

When our team is asked what the newest cosmetic ingredient has been at our pharmacy in 2018, we can answer pretty unanimously: tranexamic acid. It isn’t new (studies about its use as a treatment for melasma date back to 1979)1, and it isn’t even particularly groundbreaking, but for an industry eager to meet new cosmetic demands across the nation, we can safely say that tranexamic acid is having a new renaissance in cosmetic medicine.

What is tranexamic acid?

Tranexamic acid (trans-4-aminomethyl cyclohexane carboxylic acid) is a known blood clotting antifibrinolytic drug. It’s widely used in the medical field as a safe hemostatic agent during surgery, after major blood loss from a traumatic injury or postpartum and has been commonly used during denture procedures in patients with hemophilia.

Since the early ’80s, however, studies have demonstrated its role in plasmin inhibitor activation making it an effective treatment for melasma – an alternative to hydroquinone with low side effects and high patient satisfaction.2 The largest study conducted on tranexamic acid for skin conditions, so far, has been the 2016 retroactive analysis conducted in Singapore on a population of 561 patients, examining the use of oral tranexamic acid (TA) for the treatment of melasma.3 Published in the Journal of American Academy of Dermatology (JAAD), the conclusion was that TA posed an effective adjunct therapy for refractory melasma as long as there was careful screening for personal and familial risk factors and thromboembolism.

New uses for tranexamic acid and what’s next:

Today, we see tranexamic acid being used by dermatology practices and aesthetic centers as a more general depigmenting agent for not just hormone-induced and ultra-violet related pigmentation but post-inflammatory hyperpigmentation. Because of its flexible stability as a compounded oral, topical and IV formulation, we have seen requests for it skyrocket as its use expands across cosmetic indications. Some practices see its use beyond fading spots and unwanted pigmentation but also for redness seen in rosacea patients. VLS Pharmacy is also seeing it combined with other popular ingredients such as niacinamide (vitamin B3) and kojic acid for added potency in skin lightening products and treatments.

Most of all, topical tranexamic acid is becoming a popular solution in conjunction with in-office aesthetic procedures such as micro needling and microdermabrasion to amplify skin brightening results. As more and more practices seek an edge to make their non-invasive in-office treatments more efficacious and competitive, tranexamic acid has become the new go-to ingredient that can truly deliver results for patients.

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VLS Pharmacy’s most popular compounded formulations with tranexamic acid:


Glutathione, Vitamin C, Tranexamic acid


TRANEXAMIC 5% TOPICAL SOLUTION Used after microneedling or microdermabrasion

TRANEXAMIC TOPICAL CREAM with KOJIC ACID and NIACINAMIDE Used as a skin brightening formulation and safe alternative to hydroquinone


Sadako N, Treatment of melasma with tranexamic acid, The Clin Rep 1979; 13: 3129-3.

  1. Ebrahimi, B., & Naeini, F. F. (2014). Topical tranexamic acid as a promising treatment for melasma. Journal of Research in Medical Sciences: The Official Journal of Isfahan University of Medical Sciences, 19(8), 753–757.
  2. Lee HC, Thng TG, Goh CL. Oral tranexamic acid (TA) in the treatment of melasma: a retrospective analysis. J Am Acad Dermatol. 2016;75:385-392.


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