In the last several decades, researchers have focused on developing suitable drug carriers to deliver pharmaceutical agents to treat cancer diseases. PAMAM dendrimers have been studied as potential delivery systems for targeting, imaging, and/or delivering therapeutic agents specifically to diseased tissues because of their unique properties, such as: multiple functionalities at the periphery or in the cavity, biocompatibility, tunable size, and monodispersity. Anti-cancer agents may be incorporated into the interior void space or conjugated to the surface of PAMAM to enhance the delivery of cytotoxic drugs. In addition, targeting ligands can also be attached to the dendrimer surface to allow active targeting and minimize harm to normal cells. In summary, this review highlights the contributions of PAMAM dendrimers to the field of nanotechnology with the intent to aid researchers in exploring dendrimers for targeted drug delivery, contrasting and bio-imaging agents.