The Next Generation of Positron Emission Tomography Radiopharmaceuticals in Oncology

Abstract

Although 18F-fluorodeoxyglucose (18F-FDG) is still the most widely used positron emission tomography (PET) radiotracer, there are a few well-known limitations to its use. The last decade has seen the development of new PET probes for in vivo visualization of specific molecular targets, along with important technical advances in the production of positron-emitting radionuclides and their related labeling methods. As such, a broad range of new PET tracers are in preclinical development or have recently entered clinical trials. The topics covered in this review include labeling methods, biological targets, and the most recent preclinical or clinical data of some of the next generation of PET radiopharmaceuticals. This review, which is by no means exhaustive, has been separated into sections related to the PET radionuclide used for radiolabeling: fluorine-18, for the labeling of agents such as FACBC, FDHT, choline, and Galacto-RGD; carbon-11, for the labeling of choline; gallium-68, for the labeling of peptides such as DOTATOC and bombesin analogs; and the long-lived radionuclides iodine-124 and zirconium-89 for the labeling of monoclonal antibodies cG250, and J591 and trastuzumab, respectively.

Paclitaxel-loaded iron platinum stealth immunomicelles are potent MRI imaging agents that prevent prostate cancer growth in a PSMA-dependent manner

“…[44][45][46][47][48][49] Our data show that J591 conjugated to paclitaxel-loaded micelles specifically target the micelles to human prostate cancer cells and prevent tumor growth in a PSMA-dependent manner. PSMA is highly expressed in almost all primary and metastatic prostate cancer tumors.…”

PET/MRI and the revolution of the third eye

“…The value of PET lies in the fact that important biomolecules can be labelled with positron emitters. The most important radiotracers used in clinical practice today [2] include, together with 18 F Fluorodeoxy-glucose (FDG), radiocholine used in restaging of prostate cancer, radioamino acids used to detect cerebral recurrences, radiopeptides used to evaluate neuroendocrine tumours, and 18 F fluoride used for the early detection of bone metastases [3]. Newer applications are entering the clinical field, allowing the evaluation of growth rate using radiolabelled thymidine or the analysis of in vivo distribution of oestrogen receptors.…”

64Cu-DOTATATE for Noninvasive Assessment of Atherosclerosis in Large Arteries and Its Correlation with Risk Factors: Head-to-Head Comparison with 68Ga-DOTATOC in 60 Patients

“…64 Cu, on the other hand, is generated on a cyclotron and has a half-life of 12.7 h. The long half-life of 64 Cu allows for early as well as late PET scanning, even the day after injection. 64 Cu has a substantially shorter positron range than 68 Ga, 1 versus 4 mm, rendering it a much better spatial resolution, but a lower positron abundance (10)(11)(12)(13)(14).…”