Targeted therapies are applied to increase the efficiency of antitumor treatment by simultaneously decreasing side effects. This can be achieved using carrier molecules which specifically bind to target structures or areas with remodeling activity. These carrier molecules may be coupled to chemotherapeutic drugs or to radioactive isotopes. In most cases, these carrier molecules are antibodies against tumor antigens, peptides, or small molecules which are binders for overexpressed receptors on tumor cells. The paradigm of endoradiotherapy is exemplified by the peptidic tracer DOTATOC which binds to somatostatin receptors and recently also small molecule inhibitors with high affinity for the prostate-specific membrane antigen.