Theranostic radiopharmaceuticals: established agents in current use

Br J Radiol. 2018 Nov;91(1091):20170969. doi: 10.1259/bjr.20170969. Epub 2018 Mar 12.

Abstract

Although use of the term "theranostic" is relatively recent, the concept goes back to the earliest days of nuclear medicine, with the use of radioiodine for diagnosis and therapy of benign and malignant thyroid disease being arguably the most successful molecular radiotherapy in history. A diagnostic scan with 123I-, 124I-, or a low activity of 131I-iodide is followed by therapy with high activity 131I-iodide. Similarly, adrenergic tumours such as phaeochromocytoma and neuroblastoma can be imaged with 123I-metaiodobenzylguanidine and treated with 131I-metaiodobenzylguanidine. Bone scintigraphy can be used to select patients with painful bone metastases from prostate cancer who may benefit from treatment with beta- or alpha-particle emitting bone seeking agents, the most recent and successful of which is 223Ra radium chloride. Anti-CD20 monoclonal antibodies can be used to image and treat non-Hodgkins lymphoma, though this has not been as commercially successful as initially predicted. More recently established theranostics include somatostatin receptor targeting peptides for diagnosis and treatment of neuroendocrine tumours with agents such as 68Ga-DOTATATE and 177Lu-DOTATATE, respectively. Finally, agents which target prostate-specific membrane antigen are becoming increasingly widely available, despite the current lack of a commercial product. With the recent licensing of the somatostatin peptides and the rapid adoption of 68Ga- and 177Lu-labelled prostate-specific membrane antigen targeting agents, we have built upon the experience of radioiodine and are already seeing a great expansion in the availability of widely accepted theranostic radiopharmaceuticals.

Publication types

  • Review

MeSH terms

  • 3-Iodobenzylguanidine
  • Antigens, CD20 / radiation effects
  • Bone Neoplasms / diagnostic imaging
  • Bone Neoplasms / radiotherapy
  • Dipeptides / therapeutic use
  • Diphosphonates / therapeutic use
  • Drug Approval / economics
  • Forecasting
  • Heterocyclic Compounds, 1-Ring / therapeutic use
  • Hodgkin Disease / radiotherapy
  • Humans
  • Iodine Radioisotopes / therapeutic use
  • Lutetium
  • Octreotide / analogs & derivatives
  • Organometallic Compounds
  • Prostate-Specific Antigen
  • Radiopharmaceuticals*
  • Somatostatin / analogs & derivatives
  • Somatostatin / therapeutic use
  • Theranostic Nanomedicine / economics
  • Theranostic Nanomedicine / methods*
  • Theranostic Nanomedicine / trends
  • Thyroid Diseases / diagnostic imaging
  • Thyroid Diseases / radiotherapy

Substances

  • 177Lu-PSMA-617
  • Antigens, CD20
  • Dipeptides
  • Diphosphonates
  • Heterocyclic Compounds, 1-Ring
  • Iodine Radioisotopes
  • Organometallic Compounds
  • Radiopharmaceuticals
  • 3-Iodobenzylguanidine
  • Somatostatin
  • Lutetium
  • gallium Ga 68 dotatate
  • lutetium Lu 177 dotatate
  • Prostate-Specific Antigen
  • Octreotide