Acmella oleraceaL. (Asteraceae), commonly known as the toothache plant, is a tropical herb with significant therapeutic potential. Traditionally, it has been used for its analgesic and sialagogue properties, and it is known for its distinctive yellow flower crest. This review addresses current gaps in the understanding of its pharmacological properties and aims to provide a comprehensive analysis of its therapeutic potential. A thorough literature review was conducted using databases such as Google Scholar, ScienceDirect, and PubMed/MedLine. The findings indicate that A. oleraceacontains a variety of phytochemicals, including spilanthol, which exhibit diverse pharmacological activities such as antioxidant, anti-inflammatory, immunomodulatory, antinociceptive, pronociceptive, antibacterial, antifungal, antidiabetic, diuretic, and vasorelaxant effects. The results highlight the significant medicinal potential ofA. oleraceawhile also identifying areas for further research, particularly regarding its toxicological impacts on humans and animals. This review aims to guide future studies on the health benefits and safety of this plant.