Petiveria alliacea is a perennial Amazonian shrub used in traditional medicine for many purposes worldwide, including as antirheumatic, antispasmodic, antifungal, and analgesic for pain relief. Herein, this review aimed to provide a concise overview of the phytochemistry and antimicrobial, anticancer, and immunomodulatory properties reported in the literature for P. alliacea. The herb is rich in sulfur‑containing compounds that possess a broad‑spectrum of in vitro antimicrobial activity against pathogenic fungi and bacteria at low concentrations. P. alliacea also showed cytotoxicity and antiproliferative activity against cancer cell lines through sophisticated machinery of cellular damage in vitro. Other compounds such as flavonoids, terpenoids, and benzenoids are commonly identified in P. alliacea extracts, and they may also justify these activities. Despite the great pharmacological potential, clinical trials are required to ensure its effectiveness and safety. This review may raise new trends on the studies as well as contribute to the community by offering data for decision‑making with regard to its use in treating diseases.