Cysteamine Can Effectively Treat Hyperpigmentation

Cysteamine & Hyperpigmentation

Cysteamine is an aminothiol naturally present in the body that acts as an intrinsic antioxidant and potent skin depigmenting agent. It can be effective treating all disorders of hyperpigmentation, including melasma, post-inflammatory hyperpigmentation, chronic actinic damage and lentigines, and can be especially effective treating hyperpigmentation in darker skin, according to Corey Hartman, M.D., F.A.A.D.

Aminothiol naturally occurs in the body due to the degradation of Coenzyme A. Its physiological levels are well distributed in mammalian tissues, and it is highly concentrated in human milk. In the 1970s, cysteamine was evaluated for the treatment of cystinosis, a rare autosomal-recessive lysosomal storage disease with high morbidity and mortality rates. The disease is caused by mutations in the CTNS gene that encodes the cystine transporter, cystinosin, leading to lysosomal cystine accumulation. Cystine-depleting therapy with cysteamine orally is the only specific targeted therapy available for managing cystinosis, decreasing the frequency and severity of extrarenal complications and extending life expectancy, according to a 2017 study in Pediatric Nephrology.

Antioxidant & Keratolytic Agent

Cysteamine has been compared to hydroquinone and a modified Kligman’s formulation (hydroquinone, tretinoin and steroid), according to Dr. Hartman. Its method of depigmenting action is not yet fully understood, but as a copper and iron ion chelating agent, it is suggested that cysteamine could slow down the conversion of tyrosine into dopaquinone by preventing Fenton-type reactions.

“As a known antioxidant, cysteamine quenches hydroxy free radicals. Antioxidant agents play a key role in the inhibition of the melanogenesis pathway,” Hartman said. “Cysteamine also seems to exhibit a keratolytic effect on the epidermis. Like other keratolytic agents, tretinoin or glycolic acid, cysteamine enhances the removal of superficial epidermal layers containing melanin and accelerate epidermal turnover.”

Potent Hyperpigmentation Treatment

Hartman, along with Seemal R. Desai, M.D., Pearl E. Grimes M.D., and Sana Shah, Pharm.D., published a study in the December 2021 issue of the Journal of Drugs in Dermatology indicating that stabilized cysteamine demonstrated significant effectiveness for the treatment of different types of hyperpigmentation, including senile lentigines, which is typically considered resistant to topical depigmenting agents. The study concluded that “topical stabilized cysteamine can be regarded to as one of the most potent treatments available for hyperpigmentation disorders in humans.”

“Its rapid oxidation and offensive odor have made it more difficult to use in the past, but recent innovations have improved both stability and odor making it more palatable for consumer use,” Hartman said. “It is used in skin care as a skin lightening agent that excels at not only lightening the skin but producing an overall evening of the complexion, improvement in tone and small gains in texture as well.”

Along with a strong odor, Cysteamine is an unstable ingredient, which requires formulators to ensure the active ingredient doesn’t break down in a skin care product after prolonged use. According to Dr. Hartman, the ingredient can effectively combine with niacinamide and isobionic amide.

“Cysteamine works well in cream formulations that allow for maximum penetration into the skin during the short contact period of fifteen minutes,” Hartman said. “But when formulated correctly, cysteamine can be beneficial in cleansers, serums, creams, spot treatments and moisturizers.”