Small Molecule to Modulate Skin Pigmentation


Project ID:  D2013-88

Novelty: Use of selective small-molecule to reduce pigmentation in skin cells.

Background: Hyperpigmentation is a common condition in which patches of skin become darker in color than the surrounding skin. Globally, it is estimated that total annual sales of skin lightening and appearance enhancing cosmeceuticals amount to more than $13 billion. Although there are a number of skin lighteners available in the market, they either have serious healthy safety concerns or are not effective enough. Hydroquinone is a common skin lightening agent that is being used widely for a number of years but studies have shown that it causes skin sensitivity and is a potential carcinogen. Arbutin is another commonly used skin lightener but is surrounded by safety concerns. Clearly, there is a need for a safer and more effective skin lightening agent.   

Invention description: Researchers at the University of Toledo have developed a method comprising administering an effective amount of small drug like molecule to reduce pigmentation in the skin cell. Scientists have shown that this molecule suppresses pigmentation/melanin synthesis at the level of transcription. Treatment of melanoblasts and melanocytes with this molecule inhibits proliferation, promotes cell cycle arrest, and inhibits the expression of tyrosinase, which is the rate-limiting enzyme for melanin, as well as two other enzymes (tyrosinase related protein 1 and dopachrome tautomerase) that regulate melanin synthesis. It was observed that tyrosinase expression inhibition occurred at both the protein and mRNA levels.


Further studies revealed that administration of this drug candidate suppresses accumulation of DNA damage in mouse melanoblasts and does not cause apoptosis.

Applications: Treatment of hyperpigmentation disorders including melasma, lentigo senilis, solar lentigo, post-inflammatory hyperpigmentation, and other disorders affecting melanocytes.

IP status: Utility application filed.

Patent Information:
For Information, Contact:
Katherine Pollard
Licensing Associate
The University of Toledo
Ivana de la Serna
Archit Trivedi
Skin Lightening Agent