Molecular Imaging for Estrogen Receptor-Positive Breast Cancer

Design, Synthesis, and Biological Evaluation of Novel Nonsteroidal 18F-Labeled PET Probes Specifically Targeting Estrogen Receptor α

“…PET probes targeting ERα can detect the expression level of ERα dynamically and visually and provide guidance for the diagnosis and treatment of BC. 18 F-FES being illustrated as a representative, , the majority of PET probes targeting ERα reported in the literatures are steroids with estradiol as the parent nucleus. − In 2020, 18 F-FES was approved by Food and Drug Administration (FDA) as a radiodiagnostic agent for PET imaging to detect ERα + lesions as an auxiliary means for biopsy in patients with recurrent or metastatic BC. − However, the metabolic characteristics of 18 F-FES lead to a high imaging background in the blood, liver, and intestines, hindering the detection of abdomen metastases. ,− Hence, the development of ERα-targeted probes based on the nonsteroidal framework might provide an effective solution to the knotty problem of 18 F-FES and afford novel radioactive probes with better specificity, good metabolic characteristics, and imaging efficacy. Derived from Tamoxifen, Inoue et al reported a nonsteroidal ERα-targeted probe 18 F-FTX , which was featured with poor sensitivity, insufficient specificity, and lack of correlation between the tumor uptake of the probe and the ERα level in 10 ERα + breast cancer patients.…”

“…9 PET probes targeting ERα can detect the expression level of ERα dynamically and visually and provide guidance for the diagnosis and treatment of BC. 18 F-FES being illustrated as a representative, 10,11 the majority of PET probes targeting ERα reported in the literatures are steroids with estradiol as the parent nucleus. 12−15 In 2020, 18 F-FES was approved by Food and Drug Administration (FDA) as a radiodiagnostic agent for PET imaging to detect ERα + lesions as an auxiliary means for biopsy in patients with recurrent or metastatic BC.…”

“…Pharmacokinetic Property Study. Venous blood samples were collected from the tail vein of mice (n = 3) at different time points (1,3,5,7,10,15,20,30,45,60,90, 120 min postinjection) and weighed. The radioactivity of each sample was measured by using a γ counter.…”