The role of radiolabeling in BNCT tracers for enhanced dosimetry and treatment planning

Abstract

Positron emission tomography (PET) and single photon emission computed tomography (SPECT) are potent technologies for non-invasive imaging of pharmacological and biochemical processes in both preclinical and advanced clinical research settings. In the field of radiation therapy, boron neutron capture therapy (BNCT) stands out because it harnesses biological mechanisms to precisely target tumor cells while preserving the neighboring healthy tissues. To achieve the most favorable therapeutic outcomes, the delivery of boron-enriched tracers to tumors must be selective and efficient, with a substantial concentration of boron atoms meticulously arranged in and around the tumor cells. Although several BNCT tracers have been developed to facilitate the targeted and efficient delivery of boron to tumors, only a few have been labeled with PET or SPECT radionuclides. Such radiolabeling enables comprehensive in vivo examination, encompassing crucial aspects such as pharmacodynamics, pharmacokinetics, tumor selectivity, and accumulation and retention of the tracer within the tumor. This review provides a comprehensive summary of the essential aspects of BNCT tracers, focusing on their radiolabeling with PET or SPECT radioisotopes. This leads to more effective and targeted treatment approaches which ultimately enhance the quality of patient care with respect to cancer treatment.

64Cu-Labeled Boron-Containing Cyclic RGD Peptides for BNCT and PET Imaging

“…Additionally, it should exhibit negligible systemic toxicity and high water solubility. Finally, highly precise thermal neutron irradiation is required when the 10 B concentration peaks inside tumors. , …”

“…Finally, highly precise thermal neutron irradiation is required when the 10 B concentration peaks inside tumors. 3,4 Currently, only two BNCT drugs are in clinical trials: Lboronophenylalanine (L-BPA) and disodium mercaptoundecahydro-closo-dodecaborate (BSH). L-BPA, the most frequently used boronated tyrosine derivative, is taken up by the L-type amino acid transporter-1 (LAT-1), which is upregulated in various cancers.…”