Purpose <p>This review attempts to compile the most recent information on <i>Bidens pilosa (B. Pilosa)</i>, identify research gaps, and investigate its potential as a source of new natural medicinal compounds in pharmaceuticals and nutraceuticals. This review examines <i>B. pilosa</i>, a plant used in conventional remedies, and its important medicinal benefits.</p> Methods <p>A comprehensive review of the literature was conducted using multiple data sources such as Google Scholar, PubMed, Science Direct, and Scopus to gather relevant information. Keywords such as <i>B. pilosa</i>, traditional medicine, phytochemistry, and pharmacological activity were used for the literature search. Articles were thoroughly reviewed and articles related to Taxonomy, Ethnopharmacological Uses, Phytochemistry of <i>B. pilosa</i>, and Pharmacological Activities, Toxicity and Safety Profile, Clinical Studies and Applications, Current Herbal Formulations and Commercial Products were included and other articles were excluded.</p> Results <p>The plant <i>B. pilosa</i> L. is a crucial plant of the Asteraceae family and has several nutritional and ethnomedicinal uses. Indigenous people in Africa use it widely as a folk medicine for several ailments. Growing throughout tropical regions of the world, <i>B. pilosa</i> is a representative perennial herb with 230–240 species. <i>B. pilosa</i> is a species featuring white flowers, black seeds, and green leaves, and it has a history of treating over 40 ailments. Its bioactive compounds consist of phenolic compounds, terpenoids, alkaloids, polyacetylenes, flavonoids, essential oils, and fatty acids, which are valuable for addressing cancers, inflammation, diabetes, viral infections, and digestive issues. The plant is known for its pharmacological effects, which include anti-inflammatory, antioxidant, immune system-modulating, liver-protecting, diabetes-controlling, antimalarial, and antiviral properties. This review also analyzes the toxicological profile and clinical trials conducted on the plants, which were found to be limited, suggesting future clinical investigation to identify <i>B. pilosa</i> offers a potential source for natural drugs, pharmaceuticals, and nutraceuticals.</p> Conclusion <p>The review explores <i>B. pilosa’s</i> pharmacognostic traits, phytochemical makeup, taxonomical classification, traditional use, global distribution, ethnomedical use, phytochemistry and pharmacology, method of extraction and analysis, regulatory status, clinical studies, and toxicity profile. This review attempts to compile the most recent information on of <i>B. pilosa</i>, identify research gaps, and investigate its potential as a source of new natural medicinal compounds in pharmaceuticals and nutraceuticals.</p> Graphical Abstract <p></p>