Provided herein are methods of treating prostate cancer using radiopharmaceuticals. The radiopharmaceuticals compositions can comprise a prostate specific membrane antigen (PSMA) targeting moiety, a metal chelator, and a radionuclide chelated to the metal chelator.

The present invention relates to a compound according to formula (V):

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or a pharmaceutically acceptable salt thereof, optionally containing a chelated radioactive cation and wherein F is optionally .sup.18F.

The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of PSMA-expressing cancers, especially prostate cancer, and metastases thereof. In particular, the present invention relates to a PSMA binding ligand or a pharmaceutically acceptable salt or solvate thereof comprising a PSMA binding motif Q and a chelator residue A linked via at least one linker L.sup.AQ, the linker comprising at least one N-alkylated, preferably N-methylated amino acid.

The present disclosure relates to compounds of Formula (1a), (1b), (1c) or (1d) and pharmaceutically acceptable salts thereof, wherein X, Z, L, CM and R.sup.1 are defined herein, and their use as cancer diagnostic or imaging agents.

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