Tyrosinase inhibitors lighten skin because they block tyrosinase. Tyrosinase is the enzyme your skin needs to make melanin, the pigment that makes the skin darker. 

 Skin care products that contain these melanin blockers are used in treatments for all kinds of skin hyperpigmentation. 

Many of these skin lightening ingredients that block tyrosinase are of natural origin. They are used in creams and face serums to treat dark spots on the skin.

 They are the best type of skin-lightening ingredients used to treat dark spots, melasma and post-inflammatory hyperpigmentation.  

You can find a list of tyrosinase inhibitors in alphabetical order at the end of this blog. 

Tyrosinase inhibitors work by blocking the enzyme tyrosinase that is needed to produce the 2 kinds of melanin skin pigments: eumelanin and pheomelanin. 

When this enzyme is blocked, neither type of skin melanin can be made. 

Tyrosinase controls the most important step in melanin production which is the conversion of tyrosine to L-DOPA. Melanin cannot be made when these melanin production inhibitors prevent tyrosine from turning into L-DOPA.

Tyrosinase blockers can stop the conversion of tyrosine to L-Dopa in many different ways⁽³⁾ but the end result is the same: the skin produces less melanin pigment than it would have.

How well the production of melanin is blocked depends upon how effective the tyrosinase inhibitor product is. (There are weak ones, medium strength, and strong ones.)

Click on the ingredient name in the list below to learn more about it.

Of the 16 Baumann Skin Types,  eight of these skin types need a tyrosinase inhibitor in their skincare routine. 

I recommend that you use at least one tyrosinase inhibitor product in your skin care routine, but you need to choose wisely and use them properly to get good results.

Combine these with exfoliants, soothing ingredients, and sunscreens for best results.

1. Derma Made Mela-Fade
2. Alastin A-Luminate Brightening Serum
3. Cyspera Intensive Pigment Correcting Serum 
4. Isdinceutics Melaclear Advanced 
5. Skinceuticals Discoloration Defense

Keep reading to learn how to incorporate these products in your routine.

Our favorite medical grade products work best when combined with other products that are made with different types of skin lightening ingredients. These all work faster and have fewer side effects when combined with the correct cleanser, serum, face cream and sunscreen for your Baumann Skin Type.

 We recommend shopping by your skin type for products so you can match the best ingredients to any issues that your skin may have in addition to hyperpigmentation.

Many things need to be considered when choosing the best skin lightening products for your skin.

Take the quiz to see if these products are right for you.

These products do not work well if used incorrectly, so we have some advice to help you get better results.

Here are our dermatologists tips to get your skin lightening products to work faster to treat hyperpigmentation.

Use tyrosinase inhibitors at least once a day every day. Do not skip days. Use them on clean skin after cleansing. Combine them in your routine with exfoliating products , retinoids, PAR-2 blockers and  anti-inflammatory ingredients if these are right for your skin type.  Choose a moisturizer with unsaturated fatty acids and oils that help inhibit tyrosinase. Use the moisturizer after the tyrosinase inhibitor. Use SPF every day- even indoors. Apply the sunscreen after your moisturizer in the am.

Take a 2- 4 week break from using tyrosinase inhibitors every 3-4 months.⁽²⁾

There are many different tyrosinase inhibitors.  Some are very strong like hydroquinone while others like ascorbic acid are weak.

Hydroquinone is the strongest and best ingredient to block the conversion of tyrosine to L-DOPA,  but questions about the safety of hydroquinone and removal of it from the cometic market have led to the development of many different ingredients that block this enzyme.

Here is  a list of tyrosinase blocking ingredients by strength:

The 5 most powerful tyrosinase inhibitors to use topically are (in order of strength):

1. Thiamidol (isobutylamido-thiazolyl-resorcinol) 
2. Hydroquinone
3. Resorcinol
4. Hexylresorcinol
5. Kojic Acid

 These medium strength ingredients also have fewer side effects (in alphabetical order):

• Arbutin
• Artemisia Capillaris
• Ascorbic acid
• Azelaic acid
• Ellagic Acid
• Emblica (Emblican)
• Licorice Extract (Glabridin, Glycyrrhiza glabra)
• Paper Mulberry (Mulberry extract)
• Retinol
• Saururus chinensis also called Asian Lizard's Tail Plant or Chinese Lizard's Tail 

These weak ingredients have very few side effects.  They can be used even when you are taking a tyrosinase inhibitor holiday:

• Aloesin
• Flavonoids (A large family of compounds that includes resveratrol)
• Oils with unsaturated fatty acids (see list below of oils)

Oils with high concentrations of unsaturated fatty acids are also considered natural tyrosinase inhibitors. These can be found in organic and clean skin lighting products.

These skin lightening oils are ideal alone or in moisturizers to layer over skin lightening products.

Look for moisturizers such as Zerafite Skin Brightening Barrier Cream that have unsaturated fatty acids or these unsaturated oils.

These should be combined with stronger tyrosinase inhibitors and PAR-2 blockers for best results.

• Argan oil
• Avocado oil
• Borage seed oil
• Evening primrose oil
• Grapeseed oil
• Marula oil
• Olive oil
• Rosehip oil
• Safflower oil
• Sunflower oil
• Sesame oil
• Soybean oil
• Tsubaki oil

Many different types of ingredients can be used to lighten skin. I will discuss which category these are in and if they are tyrosinase inhibitors.

It is good to have options because tyrosinase inhibitors work best when you use them for 3-4 months and then stop for 2-4 weeks and then restart.  Dermatologists call this a tyrosinase inhibitor holiday.

We can help you find the right lightening for your skin type, if you shop using your Baumann Skin Type.

Vitamin C is a weak tyrosinase inhibitor but it can also help prevent skin pigmentation through its effects on the p53 pathway and it's antioxidant capabilities.

Downsides of using Vitamin C to treat hyperpigmentation are:

• Does not effectively inhibit tyrosinase
• Has difficulty penetrating into the skin
• Unstable
• Reacts with other skin care products
• Has a low pH that can sting skin and affect other products
• Expensive

However, Vitamin C is a great antioxidant and it helps increase skin collagen and prevent aging.

I prefer using Vitamin C serum in my patients when they are taking a tyrosinase inhibitor holiday.

The best Vitamin C serums to use to treat melasma if you have aging skin can be found at this link.

In addition to being a tyrosinase inhibitor, azelaic acid is an exfoliant and is anti-inflammatory

 It has a low pH and can cause stinging in sensitive skin types.

Cysteamine is a tyrosinase inhibitor, but it also has the added benefit of protecting skin from UV radiation.

Cysteine does not effect the conversion of tyrosine to L-DOPA but works later in the pathway to push the melanin production towards pheomelanin and away from eumelanin. 

Pheomelanin is lighter than eumelanin so it makes the skin appear lighter when cysteine is present.

Cysteine is not esy to get into the skin so it is not found in very many skin care products.

Glutathione blocks melanin by directly and indirectly stopping the enzyme tyrosinase, shifting away from producing dark eumelanin to making more of the lighter pheomelanin pigments. While glutathione injections are popular, no proof shows they work or are safe. In fact, side effects made the Philippines FDA warn against using injections for unapproved uses including skin lightening. Currently, three controlled studies support the safe skin-lightening impacts of oral and topical glutathione. However crucial questions remain on aspects like treatment length, lastingness of lightening, and maintenance plans. More high-quality clinical trials tracking patients long-term are necessary to demonstrate if glutathione can treat hyperpigmentation and sustain skin lightening. (17)

Glycolic acid does not inhibit tyrosinase. Instead it lightens dark spots by causing exfoliation. 

Glycolic acid is classified as an alpha hydroxy acid (AHA).

It can be great as a cleanser for some uneven skin types because of it's low pH.

It can also be used in acne skin types with dry skin to help remove the dark spots left by pimples.

Niacinamide is not a tyrosinase inhibitor. It helps gives cell energy to repair themselves and prevents the production of melanin by blocking the PAR-2 receptor and reducing inflammation.

Salicylic acid is not a tyrosinase inhibitor.  It is an exfoliant classified as a beta hydoxyacid (BHA).

It can be a good treatment for hyperpigmentation if combined with other skin lighteners.

It is a great choice to help treat dark spots from acne in oily skin types.

Salicylic acid also has anti-inflammatory effects.

This is a weak tyrosinase inhibitor, but really has effects on plasmin.

Tyrosinase inhibitors begin blocking skin pigment production right away but it takes months to see results. This is because the skin pigment is in the cells of the epidermis called keratinocytes. It takes around 30-50 days for the epidermis to complete the desquamation process and replace all of the skin cells and repopulate the epidermis with cells without melanin.¹

This is why you must use a skin lightening routine with tyrosinase inhibitor skincare products for at least 6 weeks to see a difference in skin color.

In many cases, melanin pigment is also in the dermis which takes even longer to clear.

This is why you should plan to use your tyrosinase inhibitor products for 8 weeks before you begin to tell a difference. Most people require 16 weeks of a tyrosinase inhibitor treatment before they can see results.

Keep in mind that any sun, heat, or light exposure will set you back because sun, heat, and light activate melanocytes to make more pigment. We recommend using tinted sunscreen daily to help your tyrosinase inhibitors work better. The iron oxides in the tint give more protection than an un-tinted sunscreen.

Tips to improve the results of tyrosinase inhibitor products:

•  Combine several tyrosinase inhibitors together
• Use them with antioxidants
• Use them with exfoliants
• Use them consistently in a customized skin care routine designed for your Baumann Skin Type®.
• Make sure you apply in the correct skincare routine step order. 
• Use moisturizers with unsaturated fatty acids
• Use occlusives to "slug" the tyrosinase inhibitors into your skin.
• Stop them for 2-4 weeks every 3-4 months

The other products in the routine will affect how well tyrosinase inhibitors work.

You will waste your money if you do not consider every single step of your skin care regimen.

Keep these tips in mind when buying products and building a skin care routine:

• Use a low pH cleanser to speed exfoliation
• The best cleansers for melasma are discussed here
• Use skin-lightening ingredients that will not irritate your skin type
• Use moisturizers with unsaturated fatty acids that inhibit tyrosinase
• Use moisturizers that help tyrosinase inhibitors absorb into the skin 
• Combine the tyrosinase inhibitors with antioxidants and soothing ingredients to reduce inflammation because inflammation causes pigmentation
• Combine with PAR-2 inhibitors that block the transfer of melanin into skin cells
• Wear a tinted mineral (physical) SPF since iron oxides protect the skin from blue light
• Combine with microdermabrasion or chemical peels
• Consider a supplement or vitamin such as pycnogenol, melatonin, or polypodium leucotomos to block skin pigment production
• Change your lifestyle to get rid of melasma
• There is a prescription pill used to treat melasma - it is not FDA approved but it is often used

Look for moisturizers with unsaturated fatty acids. See the list of oils in this blog that have unsaturated fatty acids.  Choose moisturizers with the oils on that list.

The best moisturizer with unsaturated fatty acids to block tyrosinase is Zerafite Brightening Barrier Repair Moisturizer.

Click on the ingredients below for more information:

• Aloesin
• Arbutin
• Artemisia Capillaris
• Ascorbic acid
• Azelaic acid
• Difluorocyclohexyloxyphenol
• Ellagic Acid
• Emblica (Emblican)
• Flavonoids 
• Gentisic Acid
• Glutathione
• Hydroquinone
• Hexylresorcinol
• Kojic Acid
• Licorice Extract (Glabridin, Glycyrrhiza glabra)
• Paper Mulberry (Mulberry extract)
• Resveratrol
• Resorcinol
• Saururus chinensis also called Asian Lizard's Tail Plant or Chinese Lizard's Tail 
• Thiamidol (isobutylamido-thiazolyl-resorcinol)

Studies on tyrosinase inhibitors are usually not done one animals, but they may be. The research studies on these ingredients  are usually performed first on mushrooms, then on melanocyte cells in culture, and ultimately on human skin.  Obviously, the way an ingredient performs on mushrooms or cells may differ from how it performs on living human skin, so look for evidence-based research trials performed on humans to see which of these ingredients work best.

There is so much to know about treating hyperpigmentation.

Let us guide you!

We will give you a step by step routine and you can choose from a list of products right for your skin type.

Start now!

1. Baumann, L.  Chapters 14, 20, and 41.  Baumann's Cosmetic Dermatology.  3rd Ed. (McGraw-Hill 2022)
2. This statement has never been proven but this is the practice of most dermatologists.  Check back every few months to see if recommendations have changed.
3. Zolghadri, S., Bahrami, A., Hassan Khan, M. T., Munoz-Munoz, J., Garcia-Molina, F., Garcia-Canovas, F., & Saboury, A. A. (2019). A comprehensive review on tyrosinase inhibitors. Journal of enzyme inhibition and medicinal chemistry, 34(1), 279-309.
4. D’Mello, S. A., Finlay, G. J., Baguley, B. C., & Askarian-Amiri, M. E. (2016). Signaling pathways in melanogenesis. International journal of molecular sciences, 17(7), 1144.
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9. Vaezi, M. (2023). Structure and inhibition mechanism of some synthetic compounds and phenolic derivatives as tyrosinase inhibitors: Review and new insight. Journal of Biomolecular Structure and Dynamics, 41(10), 4798-4810.
10. Peng, Z., Wang, G., Zeng, Q. H., Li, Y., Liu, H., Wang, J. J., & Zhao, Y. (2022). A systematic review of synthetic tyrosinase inhibitors and their structure-activity relationship. Critical Reviews in Food Science and Nutrition, 62(15), 4053-4094.
11. Jakimiuk, K., Sari, S., Milewski, R., Supuran, C. T., Şöhretoğlu, D., & Tomczyk, M. (2022). Flavonoids as tyrosinase inhibitors in in silico and in vitro models: Basic framework of SAR using a statistical modelling approach. Journal of Enzyme Inhibition and Medicinal Chemistry, 37(1), 427-436.
12. Mughal, E. U., Ashraf, J., Hussein, E. M., Nazir, Y., Alwuthaynani, A. S., Naeem, N., ... & Ahmed, S. A. (2022). Design, synthesis, and structural characterization of thioflavones and thioflavonols as potential tyrosinase inhibitors: In vitro and in silico studies. ACS omega, 7(20), 17444-17461.
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15. Charoo, N. A. (2022). Hyperpigmentation: Looking beyond hydroquinone. Journal of Cosmetic Dermatology, 21(10), 4133-4145.
16. Arrowitz, C., Schoelermann, A. M., Mann, T., Jiang, L. I., Weber, T., & Kolbe, L. (2019). Effective tyrosinase inhibition by thiamidol results in significant improvement of mild to moderate melasma. Journal of Investigative Dermatology, 139(8), 1691-1698.
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