 Melanogenesis is a process to synthesize melanin, which is responsible for human skin, eye, and hair pigmentation. The enzymes tyrosinase and TRP-1 and TRP-2 play major roles in melanin synthesis, with tyrosinase being the key enzyme that catalyzes a rate-limiting step of the process. Downregulation of tyrosinase is the most prominent approach for developing melanogenesis inhibitors, and numerous inhibitors targeting tyrosinase have been developed in recent years. The review focuses on recent discoveries of tyrosinase inhibitors that directly target its catalytic activity and functionality from various sources. This article was authored by Thanigymolipoleia, Manosh Manicum, and Vigneshwaranomasivayan.