This reviewcontains the analysis data on phytochemical composition ofthree-part beggarticks(Bidens tripartitaL.) and full biological activity spectrum of themedicinalraw material. Flavonoids, essentialoils, phenolcarboxylic acids, polysaccharides, aromatic hydroxy aldehydes, coumarins, tannins, and polyacetylenes are biologically active substances (BAS)ofB. tripartita.Various BAS cause multiple pharmacological and biological effects of theplant. Extracts possess antimycotic, antiinflammatory, antithrombotic, antiradical, antioxidant, antibacterial, antidiabetic, antiulcerogenic, and antitumor effects. The extracts are also ofanalgesic, antipyretic, antiallergic, hepatoprotective, immunostimulating,and hypotensive pharmacological effects. There is also a possibility to inhibit the main enzymes as well as to protect DNA. The B. tripartita medicinal raw material is of great importance for development and making of new drugs.