Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy - Université de Rennes Accéder directement au contenu
Article Dans Une Revue Molecules Année : 2020

Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy

Résumé

Identified in 1973, somatostatin (SST) is a cyclic hormone peptide with a short biological half-life. Somatostatin receptors (SSTRs) are widely expressed in the whole body, with five subtypes described. The interaction between SST and its receptors leads to the internalization of the ligand-receptor complex and triggers different cellular signaling pathways. Interestingly, the expression of SSTRs is significantly enhanced in many solid tumors, especially gastro-entero-pancreatic neuroendocrine tumors (GEP-NET). Thus, somatostatin analogs (SSAs) have been developed to improve the stability of the endogenous ligand and so extend its half-life. Radiolabeled analogs have been developed with several radioelements such as indium-111, technetium-99 m, and recently gallium-68, fluorine-18, and copper-64, to visualize the distribution of receptor overexpression in tumors. Internal metabolic radiotherapy is also used as a therapeutic strategy (e.g., using yttrium-90, lutetium-177, and actinium-225). With some radiopharmaceuticals now used in clinical practice, somatostatin analogs developed for imaging and therapy are an example of the concept of personalized medicine with a theranostic approach. Here, we review the development of these analogs, from the well-established and authorized ones to the most recently developed radiotracers, which have better pharmacokinetic properties and demonstrate increased efficacy and safety, as well as the search for new clinical indications.
Fichier principal
Vignette du fichier
molecules-25-04012-v2.pdf (5.06 Mo) Télécharger le fichier
Origine : Fichiers éditeurs autorisés sur une archive ouverte
Loading...

Dates et versions

hal-02957763 , version 1 (05-10-2020)

Licence

Paternité

Identifiants

Citer

Romain Eychenne, Christelle Bouvry, Mickael Bourgeois, Pascal Loyer, Eric Benoist, et al.. Overview of Radiolabeled Somatostatin Analogs for Cancer Imaging and Therapy. Molecules, 2020, 25 (17), pp.4012. ⟨10.3390/molecules25174012⟩. ⟨hal-02957763⟩
146 Consultations
145 Téléchargements

Altmetric

Partager

Gmail Facebook X LinkedIn More