Copper chalcogenides have a simple general formula, variable atomic ratios, and complicated crystal structures, which lead to their wealth of optical, electrical, and magnetic properties with great potential for wide applications ranging from energy conversion to the biomedical field. Herein, we summarize the recent advances in (1) the synthesis of size- and morphology tunable nanostructures by different methods; (2) surface modification and functionalization for different purposes; and (3) bioapplications for diagnosis and treatment of tumors by different imaging and therapy methods, as well as antibacterial applications. We also briefly discuss the future directions and challenges of copper chalcogenide nanoparticles in the biomedical field.