Melasma is an acquired pigmentation disorder associated with excessive melanin deposition in the skin, which is characterized by skin discoloration of varying intensity. The presence of hyperpigmentation in melasma is accompanied by reduced quality of life, development of depressive and anxiety disorders. Melasma is the most common disfiguring skin disease, since exactly the localization of lesions on the face has a pronounced negative impact both in aesthetic and socio-economic aspects. Treatment aimed at hyperpigmentation correction is not always successful. This is due to many causes and factors (ignoring the doctor’s recommendations, reference to specialists of incorrect profile, presence of unsuccessful experience of treatment with the side effects development, use of external remedies with questionable effectiveness and safety). Currently, the cosmetic agents market, including the category of depigmenting drugs, is developing rapidly. It has been found that the most promising group of whitening agents are tyrosinase inhibitors, which is a key enzyme in melanin synthesis, and that isobutylamido thiazolyl resorcinol has the highest specific action regarding tyrosinase. The molecule is characterized by greater effectiveness and higher safety profile compared to other group’s representatives, such as arbutin and hydroquinone, which were once the gold standard of skin hyperpigmentation treatment. The article presents epidemiological, topical, clinical, psychosocial aspects of melasma, as well as modern and historical approaches to treatment.