In recent times, there has been a resurgence of interest in V. negundo, with numerous ongoing clinical investigations exploring its therapeutic potential and the development of formulations derived from its bioactive constituents. Moreover, the market availability of homoeopathic medicines containing V. negundo highlights its enduring popularity. This review article provides a comprehensive analysis of V. negundo, encompassing its phytochemical composition, traditional uses, ethnomedicinal practices, and pharmacological properties. It explores the wealth of knowledge passed down through generations and the potential relevance of this traditional wisdom in modern healthcare. Additionally, the review presents findings from recent clinical trials, shedding light on the efficacy and safety of V. negundo‐based formulations in various therapeutic contexts. Furthermore, the review delves into the emerging application of nanoparticles in V. negundo‐based pharmaceutics, considering their potential to revolutionize drug delivery and formulation techniques. The incorporation of nanotechnology may enhance the bioavailability and targeted delivery of V. negundo's active compounds, further amplifying its medicinal potency. The amalgamation of traditional knowledge and contemporary scientific evidence underscores the relevance of V. negundo in the field of chemistry and biodiversity, paving the way for its continued exploration as a promising source of health‐promoting compounds.