Presented herein are systems, compositions, and methods for immuno-PET/SPECT and/or immuno-fluorescence-guided imaging of tissue for diagnosing, localizing, radiation dose planning, and/or evaluating therapy response (e.g., anti-androgen receptor therapeutics, surgery and external irradiation) in cancer (e.g., androgen receptor (AR) positive breast cancer). In other embodiments, for example, the invention is directed to radio- immunotherapy (RIT) treatment of AR-positive breast cancer by administration (e.g., injection) of a free-PSA and/or free hK2 antibody labelled with a radioisotope after KLK2 and KLK3 induction by progesterone, testosterone, and/or irradiation.
