Tranexamic Acid and Azelaic Acid—What’s the Buzz About?

For some of us, the end-of-summer blues has officially kicked in along with some unwelcome changes in our skin (especially if you’ve spent prolonged periods of time outdoors). The result of frequent sun exposure can manifest as pesky dark spots, among other things — even for the most dedicated SPF-wearers. Whether sun-induced, ghosts of acne past, or other, hyperpigmentation can be extremely stubborn. 

For that reason, the conversation around hyperpigmentation and ways to treat it has skyrocketed in recent years, and raged unabated during the pandemic as we had to find solutions at home outside the doctor’s office. Dovetailing with the increased application of science to beauty and the blurred line between cosmetics and drugs, as well as the growing popularity of acids and DTC prescription skincare (think, Curology), actives that were exclusive to the discerning eye of a dermatologist are now part of mainstream beauty products. 

Say hello to ingredients like azelaic acid and tranexamic acid, which are the shining stars of many popular anti-pigmentation products on the market right now. Brands like Skinceuticals, Peter Thomas Roth, Topicals, Good Molecules, The Ordinary, Paula’s Choice, and The Inkey list, to name a few, have recently launched products featuring these new “derm actives,” while promising results we don’t necessarily think possible with most OTC cosmetic products. 

So, what exactly is the buzz about and where does that leave our go-to repertoire of favorite skin renewing and brightening ingredients (e.g., vitamin c, retinoids, AHAs)? Let’s take a deeper look through the lens of two newer OG brands/products. But first, a quick overview of how pigment is produced in the skin and what active ingredients are commonly used to treat hyperpigmentation. 

How pigment is made & actives to treat hyperpigmentation

Pigmentation starts with a pigment producing enzyme called tyrosinase found in specialized skin cells called melanocytes, which reside in the stratum basale (bottom most) layer of our epidermis. Within melanocytes, organelles called melanosomes synthesize the pigment melanin and then transfer it to neighboring skin cells (keratinocytes) and deposit it there.

While it’s important to know how pigment is created, it’s equally worthwhile to know that you can address hyperpigmentation at different levels of the pigment production process (also known as melanogenesis). For example, a retinoid can help alleviate pigmentary issues at all levels — it inhibits tyrosinase, impedes melanosome pigment transfer, and speeds up cell turnover to get rid of pigment already deposited in the skin. Ingredients like hydroquinone, azelaic acid, kojic acid, vitamin c, licorice root, and glutathione work strictly as tyrosinase inhibitors. Hydroquinone, while no longer available OTC and ostensibly taboo, is the gold standard for squashing hyperpigmentation by dermatologists. 

Faded by Topicals & Discoloration vs. Correcting Serum by Good Molecules

Chances are many of you are already familiar with “medicated botanicals” brand Topicals and their infamous gel-serum called Faded, formulated to fade dark marks and acne scars. At an affordable price point ($36) with legit before/afters and a comprehensive formula to boot, they’ve captured the attention of beauty aficionados far and wide. Their unabashed and liberating “Who cares? Looks fade” brand messaging is worthy of praise, too.  

The popularity behind Faded, in part, stems from its power-packed ingredient list. With an all-star lineup including kojic acid, tranexamic acid, azelaic acid, alpha-arbutin (a glycosylated form of hydroquinone that is under the safety radar), niacinamide, glutathione (source of the bad sulfur smell of the product), licorice root, and melatonin, it’s no surprise that this hero product sold out within 45 minutes of hitting sephora.com. Throw in soothing botanicals like centella asiatica (gotu kola), coconut oil, and palm butter, and you definitely have a winning product on paper. But a cosmetic chemist knows that the design of this formula is based on the popular “kitchen sink” approach where a concoction is created by combining different ingredients to target multiple pathways in the skin, all in the hopes that the end product will work. Drug products on the other hand are carefully created one molecule at a time and combinations are only created if they offer a proven benefit.  

For the purpose of this article, we’re going to shed some light on two of the key hero ingredients in the formula — so here goes: 

• Azelaic acid is a dicarboxylic acid derived from grains, but is synthetically produced in a lab for skincare application. 

  • It was first approved as a drug in the form of a topical cream (20%) by the FDA in 1995 for the treatment of acne vulgaris. Later on, it was approved for the treatment of rosacea as a topical gel (15%). 

  • In terms of cosmetic regulation, there is no Scientific Committee on Consumer Safety (SCCS) opinion from the EU on this INCI.

  • It is a potent antioxidant, antibacterial, and anti-inflammatory, as well as a veritable multi-tasker: it exfoliates, alleviates congested pores, and has been shown to reduce the number of melanocytes and inhibit enzyme tyrosinase. 

  • It is a good alternative to Hydroquinone and also shows synergy with retinoic acid. 

• Tranexamic acid is a synthetic derivative of the amino acid lysine and has been used to treat or stop excessive loss of blood in the field of medicine. 

  • It comes from the pharma industry where it is approved topically for treatment of melasma pigmentation.

  • In terms of cosmetic regulation, there is no SCCS opinion from the EU or Cosmetic Ingredient Review on this INCI.

  • It is known to decrease melanin content by blocking the interaction between epidermal melanocytes and skin cells (keratinocytes).

Now that we’ve given you the 411 on those ingredients, let’s take a look at a product like the Discoloration Correcting Serum by brand Good Molecules. It’s more representative of the trend we're seeing in the market in terms of calling out one “derm active” in a formula. First off, the brand was founded by a team of beauty pros at beauty e-tailer Beautylish, and similar to The Ordinary, they’re betting on high volumes as they don’t markup their products. Some of their bestsellers range from a mere $6-$12. 

Aside from tried-and-true niacinamide at 4%, which serves as an anti-inflammatory, barrier restorer, and overall skin health booster, this product features a derivative of tranexamic acid called cetyl tranexamic mesylate at 2%. In the formula, it acts as both an emulsifier and skin brightener for better cost-efficiency. It delivers tranexamic acid into deeper layers of the skin and notably prevents UV-induced activation of melanocytes. However, unlike tranexamic acid, this derivative needs more thorough assessment and study. 

Conclusion

While azelaic acid and tranexamic acid are some of the newer, buzzy skincare ingredients that have made a splash in the beauty scene — and sure pack a punch — they haven’t replaced the more established ingredients like retinoids or vitamin c in our routines, but rather serve as adjunct treatments for hyperpigmentation and the like. Having said that, they do make excellent alternatives if prescription hydroquinone is not your cup of tea, or if you’re not able to tolerate retinoids. Check with your dermatologist to find out if these “derm actives” are right for you and what a good treatment plan may be. And remember: at the end of the day it’s all about what works for you and your skin.