Somatostatin Receptor 2-Targeting Compounds

J Nucl Med. 2017 Sep;58(Suppl 2):54S-60S. doi: 10.2967/jnumed.117.191015.


The molecular imaging and treatment of neuroendocrine tumors (NETs) with radiolabeled somatostatin analogs represent a milestone in the development of theranostic compounds. Whole-body scintigraphy with 111In-pentetreotide has revolutionized the diagnosis and staging of NETs and the evaluation of treatment outcomes. At present, diagnostic accuracy with positron-emitting radionuclides is greater than 90%. Peptide receptor radionuclide therapy (PRRT) has become a well-accepted treatment for patients with well-differentiated inoperable or metastatic NETs and disease progression after first-line treatment. Disease control rates (complete or partial remission or stable disease in patients with formerly progressive disease) of up to 95%, with a low incidence of long-term hematologic and renal toxicity, have been reported. In a recently published randomized trial, compared with intensified treatment of midgut NETs with long-acting and repeatable octreotide, PRRT reduced the hazard of disease progression and death by 79%. Upcoming developments in PRRT include the use of somatostatin receptor antagonists and α-emitting radionuclides, which may further enhance treatment outcomes.

Keywords: neuroendocrine tumors; peptide receptor radionuclide therapy; somatostatin receptor; theranostics.

Publication types

  • Review

MeSH terms

  • Animals
  • Diagnostic Imaging
  • Drug Discovery / methods*
  • Humans
  • Molecular Targeted Therapy*
  • Receptors, Somatostatin / metabolism*
  • Safety


  • Receptors, Somatostatin
  • somatostatin receptor 2