Copper-64 was produced in large scales and high specific activities in late 1990s' using compact cyclotrons based by Ni-64(p,n)Cu-64 reaction and many radiopharmaceuticals developed since then by various groups based on interesting physicochemical and nuclear properties of the radionuclide. The unique emission of beta particles as well as positron particles offers a spectacular real therapeutic/diagnostic ("Theranostic") radionuclide in nuclear medicine. Although the development of copper-64 radiopharmaceuticals continued with a slower rate in 2010s' due to availability of Ga-68-tracers, however recent advances in application of therapeutic doses of Cu-64 has emerged a new trend in the radiopharmaceutical development based on coppe-64. In this review, recent advances in the copper-64 theranostic radiopharmaceuticals including introduction of new chelating groups with enhanced stability as well as radiolabelling conditions as well as application of simple (CuCl2)-Cu-64 radiopharmaceutical as areal theranostic agent in human subjects are summarized. A proposed strategy for development of peptide based copper-64 radiopharmaceuticals with high and low dose therapeutic applications has been suggested.