Clinically modifying skin pigmentation is a valuable approach that can treat pigmentation and photosensitivity disorders and provide a degree of protection from skin cancers. Skin pigmentation is due to the presence of eumelanin, a biological pigment that is generated by the highly regulated melanogenesis pathway. Proteins within this pathway, including the melanocortin 1 receptor (MC1R), microphthalmia-associated transcription factor (MITF), and tyrosinase, can be activated or deactivated in order to bring about the desired change in eumelanin content, and thus pigmentation.A novel platform to modulate skin pigmentation is the use of oligopeptides designed with affinity towards the active sites in molecules of the melanogenesis pathway. A useful approach developing such peptides is to imitate active sites of existing hormones and signaling molecules with melanogenesis modulating properties. This platform is especially useful since oligopeptides can be designed to increase activity, prolong in vivo stability, promote penetration into cells and minimize side effects when compared to the molecules they mimic, or other drugs.