People’s lifestyles are changing from active to sedentary as a result of urbanization; they are replacing organic home-cooked meals with processed fast foods and snacks that are high in sugar, salt, and fat. This increases the risk of metabolic syndromes, including diabetes, obesity, and other noncommunicable illnesses linked to food. Therefore, it is vital to harness the potential of plants like Bidens pilosa L. (BP; Asteraceae) to combat malnutrition, food scarcity, and health issues. About 230–240 varieties of the Bidens genus exist. Bidens pilosa L. is a common perennial plant found throughout tropical and temperate regions. It is an edible medicinal plant with a wide range of bioactivities that may help prevent and treat several illnesses. Historically, BP has been utilized in medicinal therapy, phytoremediation of heavy metal-contaminated soils, and in agriculture as a biopesticide and herbicide, as well as a food flavoring ingredient. Bioactives derived from BP are resurfacing as a promising alternative medicine for drug formulations and herbal therapy to treat over 40 ailments in humans and animals without any evident side effects. Even though phytochemical and biological investigations of BP have advanced significantly in recent years, thorough and critical assessments of this plant are either outdated or have a narrow focus. While there has been some progress, more comprehensive research is needed to fully comprehend and confirm the conventional applications of BP and find therapeutic benefits for the specific chemicals extracted from the substance. In summary, the broad range of its applications for various purposes is undetermined, which is why this book chapter aims to evaluate BP’s pharmacological, metabolomic, and phytochemical features as well as its uses, health advantages, and/or hazards.