The Theranostic PSMA Ligand PSMA-617 in the Diagnosis of Prostate Cancer by PET/CT: Biodistribution in Humans, Radiation Dosimetry, and First Evaluation of Tumor Lesions

Lutetium 177 PSMA radionuclide therapy for men with prostate cancer: a review of the current literature and discussion of practical aspects of therapy

“…There are a number of different PSMA peptides and antibodies9, 18 that have been labelled with 177 Lu, and which have been utilised in both clinical trials and for clinical use as therapy agents in men with metastatic castrate‐resistant prostate cancer (mCRPC) 4, 19, 20, 21. These include the compound PSMA–DKFZ‐617, with which most patients in the published literature to date have received their therapy.…”

PSMA Ligands for PET Imaging of Prostate Cancer

“…The excellent specificity of PSMA ligands, especially for lymph node metastases, was demonstrated in several studies (21,39,46,(83)(84)(85). Therefore, any focal uptake of the PSMA ligand higher than the surrounding background uptake in morphologically visible lesions and not associated with physiologic uptake should be considered suggestive.…”

Glu-Ureido–Based Inhibitors of Prostate-Specific Membrane Antigen: Lessons Learned During the Development of a Novel Class of Low-Molecular-Weight Theranostic Radiotracers

“…For PSMA inhibitor radiotracers, there is evidence that the internalization of PSMA ligands into tumor cells must be improved to gain optimal uptake in tumor lesions over time-relevant especially for PSMA RLT (lesson 3) (20,40). Moreover, during preclinical evaluations of theranostic radioligands, the physiologic levels of expression of the target must be carefully considered; these levels should be orders of magnitude lower in the normal state than in the diseased state.…”

“…68 Ga-PSMA-11, 18 F-DCFBC, 18 F-DCFPyL, and 18 F-PSMA-1007 are exclusive PET PSMA radioligands. PSMA-617 and PSMA I&T are theranostic PSMA radioligands because they can be radiolabeled with both diagnostic (e.g., 68 Ga and 44 Sc) and therapeutic (e.g., 177 Lu) radiometals (23,39,40). Because PSMA-1007 is derived from PSMA-617, the tracers ( 18 F-PSMA-1007 and 177 Lu-PSMA-617) can be used as a theranostic tandem of PSMA radioligands.…”