Hyperpigmentation is a very common group of conditions with a pronounced negative impact on patients’ quality of life, that requires the necessity of development and search of effective and safe means to control it. Today, the market of depigmentary cosmetics is extremely var-ious, and its global financial turnover continues to grow, that confirms the relevance of whitening products. The article presents the classification and review of modern preparations for hyperpigmentation treatment. The used drugs are divided into different classes depending on the mechanism of action. Conducted studies have shown that inhibitors of tyrosinase, a key enzyme in melanin synthesis, are the most effective group. Till recently, tyrosinase produced by mushrooms due to its commercial availability has been used for the synthesis and study of tyrosinase inhibitors in factories, so many of the released whitening agents are not clinically effective for control of hyperpigmentation in humans. It has been established that isobutylamido-thiazolyl-resorcinol has the most specific action for human’s tyrosinase. The molecule has a higher efficacy and better safety profile than other substances of the group, such as arbutin and hydroquinone, which were once the gold-en standard for skin hyperpigmentation treatment. © 2023, Media Sphera Publishing Group. All rights reserved.