Long Tingting, Liu Geru, Zhou Ming, Zhang Zhen, Xiao Yao, Chen Huizhu, Peng Ning, Jin Yuzhen, He Yao, Gan Yu, Chen Zhi, Luo Min, Li Chun, Xiao Yuan, Liu Zehao, Guo Min, Xia Zhuying, Wang Min, Wang Jing, Liu Longfei, Luo Xianghang, Jiang Tiejian, Hu Shuo
Departments of Nuclear Medicine.
Endocrinology.
Clin Nucl Med. 2025 Sep 1;50(9):847-855. doi: 10.1097/RLU.0000000000006014. Epub 2025 Jun 4.
Aldosterone synthase (CYP11B2) is overexpressed in primary aldosteronism (PA), making it a promising target for imaging. This first-in-human study evaluates the safety and feasibility of [ 18 F]AldoView, a highly selective PET tracer targeting CYP11B2, for PA subtyping.
Biodistribution and dosimetry of [ 18 F]AldoView were assessed in 3 healthy volunteers using whole-body PET/CT. Fifteen patients with adrenal lesions (13 with PA, 1 with Cushing's syndrome, and 1 with a nonfunctional adenoma) were enrolled. PET/CT scans were performed 60 minutes postinjection. Lesions were considered positive if tracer uptake exceeded normal adrenal tissue. Semi-quantitative analyses included maximum standardized uptake value (SUVmax), lesion-to-liver ratio (LLR), and lesion-to-adrenal ratio (LAR). Ten PA patients with positive imaging findings and 1 with Cushing's syndrome underwent adrenalectomy, and resected specimens were analyzed for CYP11B2 expression. This ongoing study is registered with the Chinese Clinical Trial Registry (ChiCTR2400093214).
[ 18 F]AldoView was well-tolerated, with no adverse events. The effective dose was 0.012±0.0022 mSv/MBq. PET/CT identified positive lesions in all 10 PA patients, with a mean SUVmax of 15.73±8.57, LAR of 8.02±4.06, and LLR of 10.24±1.48. No positive lesions were observed in patients with idiopathic hyperaldosteronism, Cushing's syndrome, or nonfunctional adenomas. Positive lesions showed strong CYP11B2 staining on pathology, confirming aldosterone-producing adenomas (APA) or nodules (APN).
[ 18 F]AldoView PET/CT is safe and feasible for the imaging of APAs and APNs in PA patients. These results highlight its potential for noninvasive in vivo detection of CYP11B2, supporting its use in PA subtyping.
醛固酮合酶（CYP11B2）在原发性醛固酮增多症（PA）中过表达，使其成为一个有前景的成像靶点。这项首次人体研究评估了[¹⁸F]AldoView（一种靶向CYP11B2的高选择性PET示踪剂）用于PA亚型分型的安全性和可行性。
使用全身PET/CT在3名健康志愿者中评估[¹⁸F]AldoView的生物分布和剂量学。纳入了15例肾上腺病变患者（13例PA患者、1例库欣综合征患者和1例无功能腺瘤患者）。注射后60分钟进行PET/CT扫描。如果示踪剂摄取超过正常肾上腺组织，则病变被视为阳性。半定量分析包括最大标准化摄取值（SUVmax）、病变与肝脏比值（LLR）和病变与肾上腺比值（LAR）。10例影像学检查结果阳性的PA患者和1例库欣综合征患者接受了肾上腺切除术，并对切除标本进行CYP11B2表达分析。这项正在进行的研究已在中国临床试验注册中心注册（ChiCTR2400093214）。
[¹⁸F]AldoView耐受性良好，未发生不良事件。有效剂量为0.012±0.0022 mSv/MBq。PET/CT在所有10例PA患者中均发现了阳性病变，平均SUVmax为15.73±8.57，LAR为8.0²±4.06，LLR为10.24±1.48。在特发性醛固酮增多症、库欣综合征或无功能腺瘤患者中未观察到阳性病变。阳性病变在病理上显示CYP11B2强染色，证实为醛固酮分泌性腺瘤（APA）或结节（APN）。
[¹⁸F]AldoView PET/CT对PA患者的APA和APN成像安全可行。这些结果突出了其在体内无创检测CYP11B2的潜力，支持其在PA亚型分型中的应用。
