Provided is a class of radiolabeled
androgen receptor targeting agents (ARTA), useful for
prostate cancer imaging and in treating or preventing
prostate cancer. The agents define a new-subclass of radiolabeled compounds, which are selective
androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a
nonsteroidal ligand for the
androgen receptor, and / or which bind irreversibly to the
androgen receptor. The present invention further provides methods for a) imaging of
cancer in a subject, b) imaging an
androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from
prostate cancer, e) delaying the progression of
prostate cancer in a subject suffering from
prostate cancer, f) preventing the recurrence of
prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention. The present invention further provides a method of producing the radiolabeled SARM compounds, and precursor compounds useful in the preparation of the radiolabeled SARM compounds.