Nuclear Medicine and Cancer Theragnostics: Basic Concepts

Abstract

Cancer theragnostics is a novel approach that combines diagnostic imaging and radionuclide therapy. It is based on the use of a pair of radiopharmaceuticals, one optimized for positron emission tomography imaging through linkage to a proper radionuclide, and the other bearing an alpha- or beta-emitter isotope that can induce significant damage to cancer cells. In recent years, the use of theragnostics in nuclear medicine clinical practice has increased considerably, and thus investigation has focused on the identification of novel radionuclides that can bind to molecular targets that are typically dysregulated in different cancers. The major advantages of the theragnostic approach include the elimination of multi-step procedures, reduced adverse effects to normal tissues, early diagnosis, better predictive responses, and personalized patient care. This review aims to discuss emerging theragnostic molecules that have been investigated in a series of human malignancies, including gliomas, thyroid cancer, neuroendocrine tumors, cholangiocarcinoma, and prostate cancer, as well as potent and recently introduced molecular targets, like cell-surface receptors, kinases, and cell adhesion proteins. Furthermore, special reference has been made to copper radionuclides as theragnostic agents and their radiopharmaceutical applications since they present promising alternatives to the well-studied gallium-68 and lutetium-177.

Editorial for the Special Issue “Molecular Biology in Targeted Radionuclide Therapy Radiopharmaceutical Design”

“…The expression of SSTR (Somato Statin Receptor) by NETs (neuro-endocrine tumors) offers a very specific target for diagnostic imaging and therapy. The search for a more efficient theranostic candidate must take into account several parameters, including (1) the peptide sequence/chelator and its affinity for receptor subtypes; (2) the characteristics of the isotope and its SPECT/PET suitability [ 8 , 9 , 10 , 11 , 12 ]. Poletto and coworkers [contribution 3] performed a systematic review of the existing literature in this field.…”

Comparison of Nuclear Medicine Therapeutics Targeting PSMA among Alpha-Emitting Nuclides

“…However, by fully understanding the principles and properties of nuclear medicine therapeutics, we believe that they are effective. Furthermore, through an investigation of the dynamics and pathological analysis of nuclear medicine, it has been shown that the side effects are not significantly different from those of other drugs [12][13][14][15]. Nuclear medicine therapeutics are expected to become new treatment options for patients for whom existing therapeutic drugs are not suitable.…”

Biodistribution Assessment of a Novel 68Ga-Labeled Radiopharmaceutical in a Cancer Overexpressing CCK2R Mouse Model: Conventional and Radiomics Methods for Analysis

“…Utilizing the same radionuclide or pairs of chemically identical radioisotopes with similar half-lives and complementary emissions has proven to be an efficient strategy for theranostic studies. These shared features ensure the same behavior for both diagnostic and therapeutic radiotracers, a crucial factor contributing to the success of the analysis [ 21 , 22 , 23 , 24 ]. An illustrative example is the utilization of [ 68 Ga]Ga-DOTA-TOC, which extends beyond diagnostic applications and is also investigated in theranostic use, in conjunction with its therapeutic partner [ 177 Lu]Lu-DOTA-TATE (Lutathera ® ), known for its significant binding affinity for somatostatin receptors (SSTR) [ 12 ].…”