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One-Step 18F-Labeling of Estradiol Derivative for PET Imaging of Breast Cancer.

ABSTRACT: Positron emission tomography (PET) imaging is a useful method to evaluate in situ estrogen receptor (ER) status for the early diagnosis of breast cancer and optimization of the appropriate treatment strategy. The 18F-labeled estradiol derivative has been successfully used to clinically assess the ER level of breast cancer. In order to simplify the radiosynthesis process, one-step 18F-19F isotope exchange reaction was employed for the 18F-fluorination of the tracer of [18F]AmBF3-TEG-ES. The radiotracer was obtained with the radiochemical yield (RCY) of ~61% and the radiochemical purity (RCP) of >98% within 40?min. Cell uptake and blocking assays indicated that the tracer could selectively accumulate in the ER-positive human breast cancer cell lines MCF-7 and T47D. In vivo PET imaging on the MCF-7 tumor-bearing mice showed relatively high tumor uptake (1.4~2.3?%D/g) and tumor/muscle uptake ratio (4~6). These results indicated that the tracer is a promising PET imaging agent for ER-positive breast cancers.

SUBMITTER: Huang H

PROVIDER: S-EPMC5859795 | biostudies-literature | 2018

REPOSITORIES: biostudies-literature

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One-Step 18F-Labeling of Estradiol Derivative for PET Imaging of Breast Cancer.

Huang Hongbo H Li Ke K Lv Gaochao G Liu Guiqing G Zhao Xueyu X Liu Qingzhu Q Wang Shanshan S Li Xi X Qiu Ling L Lin Jianguo J

Contrast media & molecular imaging 20180305

Positron emission tomography (PET) imaging is a useful method to evaluate in situ estrogen receptor (ER) status for the early diagnosis of breast cancer and optimization of the appropriate treatment strategy. The 18F-labeled estradiol derivative has been successfully used to clinically assess the ER level of breast cancer. In order to simplify the radiosynthesis process, one-step 18F-19F isotope exchange reaction was employed for the 18F-fluorination o ...[more]

PMID: 29692688

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Project description:BACKGROUND:Elacestrant is an oral selective estrogen receptor (ER) degrader. This phase 1b open-label, non-randomized study (RAD1901-106) was initiated to determine the effect of elacestrant on the availability of ER in lesions from postmenopausal women with ER+ advanced breast cancer (ABC) using 16?-18F-fluoro-17?-estradiol positron emission tomography with low-dose computed tomography (FES-PET/CT). METHODS:Eligible patients were postmenopausal women with ER+, HER2- ABC; tumor progression after ??6?months of 1-3 lines of endocrine treatment for ABC; and measurable or evaluable disease. Two 8-patient cohorts were enrolled: one treated with 400?mg elacestrant once daily (QD) and one treated with 200?mg elacestrant QD with dose escalation to 400?mg QD after 14?days. Elacestrant was dosed continuously until progressive disease, toxicity, or withdrawal. FES-PET/CT was performed pre-dose at baseline and 4?h post-dose on day 14. The primary endpoint was the percentage difference in FES uptake in tumor lesions (maximum 20) after 14?days of treatment compared to baseline. Overall response was investigator-assessed by Response Evaluation Criteria in Solid Tumors [RECIST] version 1.1. RESULTS:Patients (n?=?16; median age, 53.5?years) had ABC with a median 2.5 prior lines of endocrine therapy. Median reduction in tumor FES uptake from baseline to day 14 was 89.1% (Q1, Q3: 75.1%, 94.1%) and was similar in both cohorts (89.1% [Q1, Q3: 67.4%, 94.2%], 200/400?mg and 88.7% [Q1, Q3: 79.5%, 94.1%], 400?mg). Residual ER availability (>?25% persistence in FES uptake) on day 14 was observed in 3 patients receiving 200/400?mg (3/78, 37.5%) and 1 patient receiving 400?mg (1/8, 12.5%). The overall response rate (ORR) was 11.1% (1 partial response), and clinical benefit rate (CBR) was 30.8%. Median percentage change in FES uptake did not correlate with ORR or CBR. Adverse events occurring in >?20% of the patients were nausea (68.8%), fatigue (50.0%), dyspepsia (43.8%), vomiting (37.5%), and decreased appetite, dysphagia, and hot flush (31.3% each). Most events were grade 2 in severity. CONCLUSION:Elacestrant 200?mg and 400?mg QD greatly reduced ER availability measured by FES-PET/CT. In a heavily pretreated population, elacestrant was associated with antitumor activity. TRIAL REGISTRATION:ClinicalTrials.gov, NCT02650817 . Registered on 08 January 2016.

Dataset Information

One-Step 18F-Labeling of Estradiol Derivative for PET Imaging of Breast Cancer.

Publications

One-Step <sup>18</sup>F-Labeling of Estradiol Derivative for PET Imaging of Breast Cancer.

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