68 Ga is a promising emerging radionuclide for positron emission tomography (PET). It is produced using a 68 Ge/ 68 Ga-generator, and thus, would enable the cyclotronindependent distribution of PET. However, new 68 Galabeled radiopharmaceuticals that can replace 18 F-labeled agents like [ 18 F]fluorodeoxyglucose (FDG) are needed. Most of the 68 Ga-labeled derivatives currently used are peptide agents, but the developments of other agents, such as amino acid derivatives, nitroimidazole derivatives, and glycosylated human serum albumin, are being actively pursued in many laboratories. Thus, appearance of new 68 Ga-labeled radiopharmaceuticals with high impact are expected in the near future. Here, we present an overview of 68 Ga-labeled agents in terms of their clinical significances and relevances to the management of certain tumors, and pertinent pre-clinical developments.