Optimized and Automated Production of [18F]FFNP for Progesterone Receptor PET Imaging

IF 3.3 3区化学 Q2 CHEMISTRY, APPLIED

Organic Process Research & Development Pub Date : 2026-10-13 DOI:10.1021/acs.oprd.6c00366

Kang-Po Li,Ephraim E. Parent,Pooja P. Advani,Juno Van Valkenburgh,Yiqian Shen,Hancheng Cai

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Abstract

[18F]FFNP is a promising investigational radiopharmaceutical for PET imaging of progesterone receptor (PR) expression in breast cancer. [18F]FFNP PET imaging enables noninvasive assessment of PR expression and serves as a valuable diagnostic tool for determining the functional endocrine status of ER+ breast tumors to guide endocrine therapy. In this study, we report a robust and fully automated radiosynthesis of [18F]FFNP using a commercially available radiosynthesizer. The ratio of the mesylate precursor to the K2.2.2/K2CO3 complex was found to be critical for optimizing radiochemical yield. The optimized and automated radiosynthesis process was completed within 50 min and successfully passed three consecutive validation runs, producing [18F]FFNP activity in 19.52–23.91% decay-corrected radiochemical yields at the end of synthesis. Approximately 215–265 mCi (7.96–9.81 GBq) of [18F]FFNP activity was obtained with high radiochemical purity (99.65–99.72%) and molar activity (16.83–37.40 Ci/μmol [623–1384 GBq/μmol]) in our cGMP-compliant PET Radiochemistry facility. All drug product specifications passed quality control (QC) testing and met the requirements for clinical investigational use.

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孕激素受体PET成像用[18F]FFNP的优化与自动化生产

[18F]FFNP是一种很有前途的用于乳腺癌孕激素受体（PR）表达的PET成像的放射性药物。[18F]FFNP PET成像可以无创评估PR表达，是确定ER+乳腺肿瘤内分泌功能状态的有价值的诊断工具，可指导内分泌治疗。在本研究中，我们报告了使用市售放射性合成器对[18F]FFNP进行稳健且全自动的放射性合成。甲磺酸前体与K2.2.2/K2CO3络合物的比例是优化放化产率的关键。优化的自动化放射合成过程在50分钟内完成，并成功通过了三次连续验证，合成结束时产生的[18F]FFNP活性为19.52% - 23.91%的衰变校正放射化学产率。在符合cgmp的PET放射化学设备中，获得了大约215-265 mCi （7.96-9.81 GBq）的[18F]FFNP活性，具有高放射化学纯度（99.65-99.72%）和摩尔活性（16.83-37.40 Ci/μmol [623-1384 GBq/μmol]）。所有药品规格均通过质量控制（QC）检测，符合临床研究使用要求。

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来源期刊

Organic Process Research & Development 化学-应用化学

CiteScore

6.90

自引率

14.70%

发文量

251

审稿时长

2 months

期刊介绍： The journal Organic Process Research & Development serves as a communication tool between industrial chemists and chemists working in universities and research institutes. As such, it reports original work from the broad field of industrial process chemistry but also presents academic results that are relevant, or potentially relevant, to industrial applications. Process chemistry is the science that enables the safe, environmentally benign and ultimately economical manufacturing of organic compounds that are required in larger amounts to help address the needs of society. Consequently, the Journal encompasses every aspect of organic chemistry, including all aspects of catalysis, synthetic methodology development and synthetic strategy exploration, but also includes aspects from analytical and solid-state chemistry and chemical engineering, such as work-up tools，process safety, or flow-chemistry. The goal of development and optimization of chemical reactions and processes is their transfer to a larger scale; original work describing such studies and the actual implementation on scale is highly relevant to the journal. However, studies on new developments from either industry, research institutes or academia that have not yet been demonstrated on scale, but where an industrial utility can be expected and where the study has addressed important prerequisites for a scale-up and has given confidence into the reliability and practicality of the chemistry, also serve the mission of OPR&D as a communication tool between the different contributors to the field.