PSMA ligands in prostate cancer - Probe optimization and theranostic applications

Methods. 2017 Nov 1:130:42-50. doi: 10.1016/j.ymeth.2017.06.026. Epub 2017 Jun 28.

Abstract

Due to its selective overexpression in prostate cancer (PCa), the prostate-specific membrane antigen (PSMA) has been recognized as a highly promising target for diagnostic and therapeutic applications. So far, various PSMA ligands have been developed for radiolabeling with radioisotopes such as 68Ga or 18F which can be used for specific visualization and diagnosis of PSMA-expressing PCa. In addition, PSMA ligands suitable for radiolabeling with 131I or 177Lu have become available to the clinics, allowing PSMA-based radioligand therapies. Here, we provide a comprehensive review of the most frequently used PSMA ligands, their structural modifications, and the impact of those on clinical applications.

Keywords: Imaging; PSMA; Prostate cancer; Theranostics.

Publication types

  • Review

MeSH terms

  • Animals
  • Antigens, Surface
  • Binding Sites / physiology
  • Fluorodeoxyglucose F18 / administration & dosage
  • Fluorodeoxyglucose F18 / metabolism
  • Gallium Radioisotopes / administration & dosage
  • Gallium Radioisotopes / metabolism
  • Glutamate Carboxypeptidase II
  • Humans
  • Ligands
  • Male
  • Prostatic Neoplasms / diagnostic imaging*
  • Prostatic Neoplasms / metabolism*
  • Radioisotopes / administration & dosage
  • Radioisotopes / metabolism*
  • Theranostic Nanomedicine / methods*
  • Theranostic Nanomedicine / standards

Substances

  • Antigens, Surface
  • Gallium Radioisotopes
  • Ligands
  • Radioisotopes
  • Fluorodeoxyglucose F18
  • Gallium-68
  • FOLH1 protein, human
  • Glutamate Carboxypeptidase II