What are the Most Effective Ingredients for Treating Melasma?

Posted by Dr. Eiji Ozawa ,27th May 2024
What are the Most Effective Ingredients for Treating Melasma?

What are the Most Effective Ingredients for Treating Melasma?

Melasma, a common skin condition characterized by dark, discolored patches, primarily affects the face. It is often stimulated by female hormones and UV exposure, which activate melanocytes. The excess melanin produced by these cells accumulates in keratinocytes, leading to the visible signs of melasma.

Tranexamic Acid

When keratinocytes are triggered by stimulants such as female hormones and UV rays, they produce plasmin, a melanocyte-activating factor, initiating melanin production. Tranexamic acid, traditionally prescribed in the United States as a hemostatic and anti-inflammatory agent to prevent and treat bleeding, is the first ingredient approved for improving melasma as an OTC drug in Japan, South Korea, and other Asian countries. Tranexamic acid plays a crucial role in the early stages of melasma. It effectively blocks plasmin from reaching melanocytes, preventing the onset of melasma at its source.

L-Cysteine and Vitamin C

Within melanocytes, an amino acid called tyrosine is converted to melanin. When plasmin signals melanocytes, it increases the activity of an enzyme called tyrosinase, which activates tyrosine for conversion to melanin. L-cysteine and vitamin C, your powerful allies in the fight against melasma, step in. They block the production and activation of tyrosinase, providing a reassuring barrier against melanin production. Additionally, vitamin C blocks the activation of tyrosinase. Tyrosine is converted to dopaquinone via a compound called dopa, which eventually becomes melanin. Vitamin C can reverse dopaquinone back to dopa and lighten the color of melanin that has already formed.

Vitamin Bs

Vitamin B6 and nicotinic acid amide (vitamin B3) are not just about melasma. They regulate skin turnover, accelerate melanin elimination, and maintain normal skin function. Vitamin B5 supports the function of vitamin C, enhancing its efficacy in combating melasma. These B vitamins are essential in ensuring that the skin remains healthy and capable of reducing melanin accumulation. It's a comprehensive approach to skincare that goes beyond just treating melasma.


A vital part of any melasma treatment regimen is the regular use of sunscreen. UV exposure is a significant trigger for melasma, so protecting the skin from harmful UV rays can prevent further darkening and worsening of the condition. Broad-spectrum sunscreens with a high SPF are recommended to shield the skin effectively.

Lifestyle Adjustments

Managing stress, maintaining a healthy diet, and avoiding known triggers such as certain medications and cosmetics can also help control melasma. A holistic approach that combines topical treatments, sun protection, and lifestyle changes often yields the best results.

Consult a Medical Professional

It is essential to consult with a medical professional to determine the most appropriate treatment plan for your specific case of melasma. A professional can provide personalized advice and treatment options best suited to your skin type and condition.

These statements have not been evaluated by the Food and Drug Administration. Always consult with a healthcare professional before starting any new treatment regimen.

* These statements have not been evaluated by the Food and Drug Administration. This product is not intended to diagnose, treat, cure, or prevent any disease.