In this review, wWe present the latest studies regarding peptides and related compounds that may be useful in artificially increasing or reducing skin melanin levels. Certain analogs of a-melanocyte stimulating hormone (MSH) and peptides with the sequences derived from the hormone were shown to promote or suppress melanin synthesis in cells and in vivo models. Various amino acids, peptides, their analogs, and their hybrid compounds with other chemical moieties were shown to inhibit tyrosinase (TYR) catalytic activity or downregulate TYR gene expression. Certain peptides were shown to inhibit melanosome biogenesis or induce autophagy, leading to decreased pigmentation. In vivo and clinical evidence are available for some compounds, including [Nle⁴-_D-Phe⁷]-a-MSH, glutathione disulfide, and glycinamide hydrochloride.