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Int J Mol Sci. 2010; 11(7): 2699–2700.
Published online 2010 July 12. doi:  10.3390/ijms11072699
PMCID: PMC2920561

Quasi-Drugs Developed in Japan for the Prevention or Treatment of Hyperpigmentary Disorders. Int. J. Mol. Sci. 2010, 11, 2566–2575

One additional skin lightening or whitening quasi-drug (QD) has been developed and officially approved by the Ministry of Health, Labor and Welfare of Japan. The active ingredient niacinamide should be included in this review [1]. Its mechanism of skin lightening is based on the inhibition of melanosome transfer from melanocytes to keratinocytes. Niacinamide is listed in Table 1, which classifies compounds according to the mechanism of skin lightening QDs registered in Japan.

Table 1.
Mechanistic classification of skin lightening QDs approved by the MHLW of Japan.

2.15. Niacinamide (Obtained by Procter & Gamble Company in 2007)

Niacinamide (also termed nicotinamide), a derivative of vitamin B3, has been shown to act as an anti-inflammatory agent in acne [2]. Niacinamide had no effect on the tyrosinase activity and melanin synthesis of cultured normal human melanocytes, however, it was found that niacinamide significantly decreased hyperpigmentation, such as melasma and solar lentigines, via inhibition of melanosome transfer from melanocytes to keratinocytes [3,4].


1. Ando H, Matsui MS, Ichihashi M. Quasi-drugs developed in Japan for the prevention or treatment of hyperpigmentary disorders. Int. J. Mol. Sci. 2010;11:2566–2575. [PMC free article] [PubMed]
2. Shalita AR, Smith JG, Parish LH, Sofman MS, Chalker DK. Topical nicotinamide compared with clindamycin gel in the treatment of inflammatory acne vulgaris. Int. J. Dermatol. 1995;34:434–437. [PubMed]
3. Hakozaki T, Minwalla L, Zhuang J, Chhoa M, Matsubara A, Miyamoto K, Greatens A, Hillebrand GG, Bissett DL, Boissy RE. The effect of niacinamide on reducing cutaneous pigmentation and suppression of melanosome transfer. Br. J. Dermatol. 2002;147:20–31. [PubMed]
4. Greatens A, Hakozaki T, Koshoffer A, Epstein H, Schwemberger S, Babcock G, Bissett D, Takiwaki H, Arase S, Wickett RR, Boissy RE. Effective inhibition of melanosome transfer to keratinocytes by lectins and niacinamide is reversible. Exp. Dermatol. 2005;14:498–508. [PubMed]

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