Background:
People have 4 parathyroid glands near the thyroid gland in the neck. Surgery is needed to remove a parathyroid gland that is too large or has a tumor. These glands can be in different places, so doctors use an imaging scan with contrast dye to help find them before surgery. Researchers want to know if a different type of scan and a new tracer can make it easier to find the tumors in the parathyroid glands.
Objective:
To see if PET/MRI and NeuroEXPLORER PET-CT scans with a 18F-FCH tracer are better than existing methods for finding the parathyroid glands.
Eligibility:
People aged 18 years or older who are scheduled for surgery to remove a parathyroid gland.
Design:
Participants will have up to 4 clinic or hospital visits. They will be screened. They will have a physical exam and give blood samples.
Participants will have a 4-dimensional computed tomography (4D-CT) scan. This is the current way doctors look for parathyroid glands. They will be injected with an iodine-based dye for the 4D-CT scan. They will lie on a padded table that slides into a donut-shaped machine.
Participants will have a positron emission tomography (PET)-magnetic resonance imaging (MRI) and NeuroEXPLORER PET-CT scan. For these scans, they will be injected with a radioactive tracer (18F-FCH). They will wait about 30 to 60 minutes for their body to absorb the tracer. They will lie on a padded table that slides into a tube. Their vital signs will be monitored during the scan.
Participants will have surgery to remove the target gland. They may need to stay in the hospital for up to 3 nights.
Participants will have a follow-up visit 6 months after the surgery. This may be done remotely....

开始日期2026-04-16

申办/合作机构

National Institute of Diabetes & Digestive & Kidney Diseases

ACTRN12625000509460

/ RecruitingN/AIIT

PARA-PET: a randomised diagnostic imaging trial of [18F]FCH PET/CT vs conventional imaging (4D-CT and sestamibi SPECT/CT) for primary hyperparathyroidism

开始日期2025-06-23

申办/合作机构-

NCT05891769

/ Recruiting临床2/3期IIT

Evaluation of Patients With Suspected Parathyroid Adenoma and Negative or Equivocal 99mTc Sestamibi SPECT/CT Using 18F Fluorocholine PET/CT

This study proposes the use of a well-established PET isotope, Fluorine-18 (18F), bound to Choline, for a prospective single-center, single-arm study for participants with suspected parathyroid adenoma and negative or equivocal standard of care 99mTc Sestamibi SPECT/CT

开始日期2023-09-27

申办/合作机构

Stanford University

100 项与 18F-Fluorocholine 相关的临床结果

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100 项与 18F-Fluorocholine 相关的转化医学

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100 项与 18F-Fluorocholine 相关的专利（医药）

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项与 18F-Fluorocholine 相关的文献（医药）

2025-12-01·The French journal of urology

A multidisciplinary approach to managing non-metastatic castration resistant prostate cancer: Insights from a national practice survey

Article

作者: Supiot, Stéphane ; Pignot, Géraldine ; Le Clanche, Solenn ; Chebbah, Myriam ; Merlin, Charles ; Sargos, Paul ; Rozet, François ; Neuzillet, Yann

INTRODUCTION:

Non-metastatic castration-resistant prostate cancer (nmCRPC) progresses despite androgen-deprivation therapy (ADT) however metastases remain undetectable on conventional imaging. PSMA PET/CT may enable earlier metastasis detection, but its clinical use remains limited. This study assessed the alignment of French clinical practices with nmCRPC management guidelines.

MATERIAL AND METHODS:

A two-part survey was conducted among 61 healthcare professionals, including urologists, oncologists, and radiation oncologists, to assess their imaging and treatment approaches for nmCRPC. The survey explored diagnostic imaging strategies, treatment decisions, and responses to two clinical case scenarios reflecting different PSA doubling times.

RESULTS:

Results showed variation, with 65% of respondents initiating enzalutamide only after conventional imaging confirmed metastases, while 57% would do so after molecular imaging detection. PSMA PET/CT was used by 41% for patients with a 6-month PSA doubling time. Treatment decisions were influenced by both imaging modality and PSA kinetics. In clinical case 1 (6-month PSA doubling time), 41% chose TAP CT or bone scan as initial imaging, 35% used [18 F] fluorocholine/[18 F] fluciclovine PET/CT, and 24% used PSMA PET/CT. In clinical case 2 (12-month PSA doubling time), 66% ordered imaging, while 29% favored monitoring without imaging. Imaging delays varied from 3 to 4 weeks, reflecting regional disparities in access.

DISCUSSION/CONCLUSION:

This study highlights variability between guideline recommendations and clinical practice in nmCRPC management in France. Although PSMA PET/CT is crucial for detecting metastases, its cost and accessibility remain suboptimal and require further improvement, despite recent advancements. Clearer guidelines and improved training are needed to reduce inconsistencies and avoid loss of therapeutic opportunity for patients.

LEVEL OF EVIDENCE:

6 as per Melnyk and Fineout-Overholt 2023.

2024-09-06·MEDICINE

Risk of malignancy in thyroid nodules with increased 11C-Choline uptake detected incidentally on PET/CT: A diagnostic accuracy study

Article

作者: Ryder, Mabel ; Johnson, Geoffrey ; Gharib, Hossein ; Durski, Jolanta ; Frota Lima, Livia Maria ; Bogsrud, Trond Velde

Purpose::

The purpose was to evaluate the pathological nature of focal thyroid uptake seen in 11C-Choline PET/CT performed for prostate cancer.

Material and methods::

The study was IRB-approved. All 11C-Choline PET/CT exam reports for studies performed between January 01, 2018, and July 30, 2021, in male patients with prostate cancer in our institution were retrospectively reviewed. Exams with “focal thyroid uptake” on their final report were selected. Patients with surgery or ablation in the thyroid prior to the PET/CT, proven parathyroid adenomas or absent thyroid ultrasound were excluded. Repeated PET/CT exams of same patient were excluded. PET images were analyzed visually and semi-quantitatively by measuring the maximum standardized uptake value (SUVmax) of the focal thyroid uptake. Available thyroid ultrasound images, cytology and pathology reports were reviewed. Statistical analyses were performed.

Results::

Out of 10,047 sequential 11C-Choline PET/CT studies, 318 reports included “focal thyroid uptake.” About 128 of these studies were repeat exams and were excluded. Additional 87 patients were excluded, because the uptake was determined to be adjacent, rather than confined to the thyroid gland. Out of the remaining 103 patients, 74 patients had focal thyroid uptake and concurrent thyroid sonographic evaluation. Out of the 74 focal uptakes evaluated with ultrasound, 21 were presumed benign thyroid nodules based on the ultrasound and 53 had further evaluation with biopsy. Sixty three nodules were benign (21 presumed benign on ultrasound and 42 cytology or surgical pathology-proven), 9 nodules were malignant and 2 remained indeterminate. There was no significant difference between the SUVs of the benign and malignant groups (P > .3).

Conclusion::

In this retrospective study of patients with prostate cancer who underwent 11C-Choline PET/CT, we identified a group of patients who underwent thyroid ultrasound for incidental finding of focal 11C-Choline thyroid uptake. Incidence of malignancy in this group was 12%. Therefore, further investigation with ultrasound and possibly ultrasound-guided biopsy may be warranted when a choline avid thyroid nodule is found incidentally on choline PET.

2024-03-01·Current pharmaceutical design

Challenging Axillary Lymph Nodes on PET/CT in Cancer Patients throughout COVID-19 Vaccination Era

Article

作者: Storto, Giovanni ; Nappi, Antonio ; Milella, Mariarita ; Storto, Rebecca ; Pellegrino, Teresa ; Di Cosola, Michele ; Giordano, Alessia ; Nardelli, Anna ; Gallicchio, Rosj

Background::

The unexpected detection of axillary lymphadenopathy (AxL) in cancer patients (pts) represents a real concern during the COVID-19 vaccination era. Benign reactions may take place after vaccine inoculation, which can mislead image interpretation in patients undergoing F-18-FDG, F-18-Choline, and Ga-68-DOTATOC PET/CT. They may also mimic loco-regional metastases or disease. We assessed PET/CT findings after COVID-19 first dose vaccination in cancer patients and the impact on their disease course management.

Methods::

We evaluated 333 patients undergoing PET/CT (257 F-18-FDG, 54 F-18-Choline, and 23 Ga-68 DOTATOC) scans after the first vaccination with mRNA vaccine (Pfizer-BioNTech) (study group; SG). The uptake index (SUVmax) of suspected AxL was defined as significant when the ratio was > 1.5 as compared to the contralateral lymph nodes. Besides, co-registered CT (Co-CT) features of target lymph nodes were evaluated. Nodes with aggregate imaging positivity were further investigated.

Results::

Overall, the prevalence of apparently positive lymph nodes on PET scans was 17.1% during the vaccination period. 107 pts of the same setting, who had undergone PET/CT before the COVID-19 pandemic, represented the control group (CG). Only 3 patients of CG showed reactive lymph nodes with a prevalence of 2.8% (p < 0.001 as compared to the vaccination period). 84.2% of SG patients exhibited benign characteristics on co-CT images and only 9 pts needed thorough appraisal.

Conclusion::

The correct interpretation of images is crucial to avoid unnecessary treatments and invasive procedures in vaccinated cancer pts. A detailed anamnestic interview and the analysis of lymph nodes’ CT characteristics, after performing PET/CT, may help to clear any misleading diagnosis.

项与 18F-Fluorocholine 相关的新闻（医药）

2026-03-22

·核联盛

肿瘤PET显像剂全链条研发：一篇读懂从原理、设计到临床转化的底层逻辑

标题：Insight into the Development of PET Radiopharmaceuticals for Oncology 作者：Joseph Lau,Etienne Rousseau,Daniel Kwon,Kuo-Shyan Lin,François Bénard,XiaoyuanChen 正电子发射断层显像（PET）早已不是实验室里的冷门技术，而是现代肿瘤精准诊疗的标配基础设施。从¹⁸F‑FDG一统天下，到⁶⁸Ga‑PSMA、⁶⁸Ga‑FAPI掀起“诊疗一体化”革命，再到PD‑L1、CD8免疫PET打开精准免疫治疗的大门，PET放射性药物正在重新定义肿瘤的诊断、分期、疗效预测与全程管理。但绝大多数人只看到一张张清晰的影像，却很少有人理解：一款能走向临床的PET药物，究竟是如何被设计、合成、验证并最终转化落地的？这篇发表在《Cancers》的系统性综述，没有停留在案例罗列，而是搭建了一套完整、自洽、可落地的PET药物研发逻辑体系——从问题提出、机制拆解、技术路径到临床转化，把整个行业的底层规律讲得透彻清晰。它既是新手入门的教科书，也是资深研究者的路线图，更是普通读者理解“核医学为什么厉害”的最佳入口。一、PET药物为什么重要？因为传统成像解决不了精准问题肿瘤诊疗最大的痛点之一，是“看不见、分不清、测不准”。 CT和MRI看的是解剖结构，只能判断“有没有长东西”；而PET看的是分子层面的功能信息，能直接回答：是不是肿瘤？是什么类型？活跃程度如何？靶点表达多少？治疗有没有效果？ PET的核心原理并不复杂：将一种能发出正电子的放射性核素，标记在能精准“找到”肿瘤的分子上，注入人体后，它会像“导航弹”一样聚集在病灶，再通过探测器“点亮”肿瘤，实现定量可视化。但长期以来，临床最依赖的依旧是¹⁸F‑FDG——一种反映葡萄糖高代谢的“广谱探针”。它好用，却不完美：炎症会假阳性、部分肿瘤不摄取、无法区分分型、更不能指导靶向治疗。这就带来一个全行业的核心命题：如何开发出更特异、更灵敏、更稳定、更能落地的新型PET显像剂？这不是简单的“标记一个核素”，而是一套横跨分子设计、放射化学、药代动力学、临床前评价和法规监管的系统工程。二、好的PET药物，必须满足五条“铁律” 一款能成功临床转化的PET探针，不是越复杂越好，而是要在设计之初就遵循严格的内在规律。第一，高特异性。只结合肿瘤或特定靶点，不与正常组织乱结合，这是避免假阳性的基础。很多药物失败，不是不灵敏，而是“爱乱贴”。第二，高亲和力。对靶点的结合能力要强，通常要求Kd值低于50nM，才能在靶点低表达时也被检出。第三，非靶组织快速清除。探针进入人体后，正常器官代谢得越快，肿瘤对比就越清晰，同时降低患者辐射剂量。第四，体内高度稳定。不能还没到肿瘤就被酶剪断、代谢掉，也不能在血液里分解释放游离核素，造成干扰。第五，制备简单、成本可控、符合GMP。实验室做得出来不算成功，医院能自动化合成、稳定放行，才具备真正价值。这五条铁律，决定了PET药物从源头设计就必须“带着临床思维做研发”，而不是单纯追求学术上的新颖。图1：前列腺癌免疫PET成像［⁸⁹Zr］Zr‑11B6 直观呈现了理想PET药物的核心特征：肿瘤持续高摄取，肝脏等正常器官快速清除，并且只在目标阳性肿瘤中聚集，完美诠释“特异性+药代匹配”两大关键。三、四大主流路线，决定一款核药的成败在PET药物研发中，靶向分子（药效团）的选择，决定天花板。目前全球最成功的路线，基本都集中在四大类型，每一类都有清晰的适用场景与优劣。表 1 临床已评估的肿瘤 PET 放射性药物生物学过程 / 靶点放射性药物载体类型适应症 A33 [¹²⁴I]I-huA33 抗体结直肠癌乙酰辅酶 A 合成酶 [¹¹C]acetate 盐泛肿瘤氨基酸转运 [¹¹C]methionine、[¹⁸F]FDOPA、[¹⁸F]FGln、[¹⁸F]FSPG、[¹⁸F]FACBC、[¹⁸F]FACPC、[¹⁸F]FET 氨基酸脑胶质瘤、神经内分泌肿瘤、前列腺癌雄激素受体 (AR) [¹⁸F]FDHT 激素前列腺癌凋亡 [¹⁸F]ML-10、[¹⁸F]ICMT-11 小分子胶质母细胞瘤、乳腺癌、肺癌骨重塑 [¹⁸F]NaF 盐骨病变 CA19.9 [⁸⁹Zr]Zr-DFO-HuMab-5B1 抗体胰腺癌、膀胱癌碳酸酐酶 IX (CA-IX) [¹²⁴I]I-girentuximab、[⁸⁹Zr]Zr-girentuximab 抗体肾透明细胞癌癌胚抗原 (CEA) [⁸⁹Zr]Zr-AMG 211 双特异性抗体胃肠道腺癌 CD8 [⁸⁹Zr]Zr-Df-IAB22M2C 小抗体黑色素瘤、肺癌、肝癌 CD20 [⁸⁹Zr]Zr-rituximab、[⁸⁹Zr]Zr-obinutuzumab 抗体 B 细胞淋巴瘤 CD44v6 [⁸⁹Zr]Zr-U36 抗体头颈部肿瘤 CXCR4 [⁶⁴Cu]Cu-plerixafor、[⁶⁸Ga]Ga-pentixafor、[⁶⁸Ga]Ga-NOTA-NFB 小分子、肽血液肿瘤、实体瘤 CTLA-4 [⁸⁹Zr]Zr-ipilimumab 抗体黑色素瘤 EGFR [¹¹C]erlotinib、[¹¹C]PD153035、[¹⁸F]afatinib、[⁸⁹Zr]Zr-cetuximab、[⁸⁹Zr]Zr-panitumumab 小分子、抗体非小细胞肺癌、结直肠癌 ERBB2(HER2) [⁶⁸Ga]Ga-ABY-025、[⁶⁸Ga]Ga-HER2-Nanobody、[⁸⁹Zr]Zr-trastuzumab、[⁸⁹Zr]Zr-pertuzumab 抗体模拟物、纳米抗体、抗体乳腺癌 ERBB3 [⁸⁹Zr]Zr-GSK2849330、[⁸⁹Zr]Zr-lumretuzumab 抗体实体瘤雌激素受体 (ER) [¹⁸F]FES、[¹⁸F]4FMFES 激素乳腺癌、妇科肿瘤成纤维细胞活化蛋白 α(FAP) [⁶⁸Ga]Ga-FAPI-04、[⁶⁸Ga]Ga-FAPI-21、[⁶⁸Ga]Ga-FAPI-46 小分子泛实体瘤半乳糖代谢 [¹⁸F]FDGal 小分子肝细胞癌胃泌素释放肽受体 (GRPR) [⁶⁴Cu]Cu-CB-TE2A-AR06、[¹⁸F]BAY 864367、[⁶⁸Ga]Ga-RM2、[⁶⁸Ga]Ga-SB3、[⁶⁸Ga]Ga-RM26、[⁶⁸Ga]Ga-BBN-RGD、[⁶⁸Ga]Ga-NOTA-Aca-BBN、[⁶⁸Ga]Ga-NeoBOMB1 肽前列腺癌、乳腺癌、胶质瘤 GLP-1R [⁶⁸Ga]Ga-NOTA-exendin-4 肽胰岛素瘤葡萄糖代谢 [¹⁸F]FDG 小分子泛肿瘤磷脂酰肌醇蛋白聚糖 3 [¹²⁴I]I-codrituzumab 抗体肝细胞癌乏氧 [¹⁸F]EF5、[¹⁸F]FMISO、[¹⁸F]FAZA、[¹⁸F]HX4、[⁶⁴Cu]Cu-ATSM 小分子实体瘤整合素 α4β1 [⁶⁴Cu]Cu-LLP2A 肽模拟物多发性骨髓瘤整合素 αvβ3 [¹⁸F]F-Galacto-RGD、[¹⁸F]F-FPP(RGD)2、[¹⁸F]F-RGD-K5、[¹⁸F]F-fluciclatide、Al[¹⁸F]F-alfatide-I、Al[¹⁸F]F-alfatide-II、[⁶⁸Ga]Ga-NOTA-PRGD2 肽实体瘤整合素 αvβ6 [¹⁸F]F-αvβ6-BP、[⁶⁸Ga]Ga-DOTA-SFITGv6、[¹⁸F]FP-R01-MG-F2、[⁶⁸Ga]Ga-NODAGA-R01-MG 肽、胱氨酸结头颈部肿瘤、肺癌、结直肠癌、乳腺癌、胰腺癌黑皮质素 1 受体 (MC1R) [⁶⁸Ga]Ga-DOTA-GGNle-CycMSHhex 肽黑色素瘤间皮素 [⁸⁹Zr]Zr-MMOT0530A 抗体胰腺癌、卵巢癌神经激肽 1 受体 (NK1R) [⁶⁸Ga]Ga-DOTA-SP 肽胶质瘤神经降压素 1 受体 (NTS1R) Al[¹⁸F]F-NOTA-neurotensin 肽前列腺癌磷脂合成 [¹¹C]choline、[¹⁸F]F-choline 盐前列腺癌 PARP1 [¹⁸F]PARPi 小分子头颈部肿瘤前列腺特异性膜抗原 (PSMA) [¹⁸F]PSMA-1007、[¹⁸F]DCFPyL、[¹⁸F]DCFBC、[¹⁸F]rhPSMA-7、[⁶⁸Ga]Ga-PSMA-11、[⁶⁸Ga]Ga-PSMA-617、[⁶⁸Ga]Ga-PSMA-I&T、[⁸⁹Zr]Zr-HuJ591 拟肽、抗体前列腺癌 PD-1 [⁸⁹Zr]Zr-durvalumab、[⁸⁹Zr]Zr-nivolumab、[⁸⁹Zr]Zr-pembrolizumab 抗体非小细胞肺癌 PD-L1 [¹⁸F]BMS-986192、[⁸⁹Zr]Zr-atezolizumab 小分子、抗体非小细胞肺癌、膀胱癌、乳腺癌 STEAP1 [⁸⁹Zr]Zr-DFO-MSTP2109A 抗体前列腺癌钠 / 碘转运体 Na[¹²⁴I]I 盐甲状腺癌胸腺激酶 (DNA 增殖) [¹⁸F]FLT 核苷实体瘤生长抑素受体 2 (SSTR2) [⁶⁸Ga]Ga-DOTA-NOC、[⁶⁸Ga]Ga-NODAGA-JR11、[⁶⁴Cu]Cu-SARTATE、[⁶⁸Ga]Ga-DOTA-TATE、[⁶⁸Ga]Ga-DOTA-TOC 肽神经内分泌肿瘤 TGF-β [⁸⁹Zr]Zr-fresolimumab 抗体胶质瘤 VEGFR [⁸⁹Zr]Zr-bevacizumab 抗体第一类是生物活性分子探针，也就是模仿人体本身的物质，比如葡萄糖、氨基酸、核苷酸、胆碱。这类探针最贴近生理，安全性高、代谢路径清晰。¹⁸F‑FDG、¹¹C‑胆碱、¹⁸F‑FET、¹⁸F‑FLT都属于这一类。它们的优势是通用性强，但缺点也明显：特异性有限，难以区分更精细的肿瘤分型。图2：基于生物活性分子的PET药物示例图中展示的FDG、FDOPA、胆碱等结构，是目前全球临床用量最大的PET分子，它们的成功证明：“越贴近生理，越容易转化”。第二类是多肽与拟肽探针，也是近十年最成功的类别。多肽分子量小、组织穿透快、清除快、易于标记，尤其适合靶向肿瘤高表达的GPCR受体。最经典的代表就是生长抑素受体多肽，用于神经内分泌肿瘤；以及PSMA靶向多肽，彻底改变了前列腺癌诊疗格局。这类探针的核心优势是“快进快出、高靶本比”，非常适合⁶⁸Ga、¹⁸F等短半衰期核素。图4：生长抑素受体成像多肽类核药成功的本质：受体表达谱清晰、肿瘤高表达、正常组织低表达，让PET/CT能检出传统影像看不见的微小转移灶。第三类是药物衍生探针，直接把已经成熟的靶向药、抑制剂标记成核素。比如把厄洛替尼、阿法替尼标记用于EGFR显像，把PSMA抑制剂标记成⁶⁸Ga‑PSMA‑11。这种思路的最大优势是机制明确、靶点确证、转化风险低。但难点在于：放射性标记不能破坏药物的结合活性。这也是为什么PSMA、FAPI抑制剂类探针能快速爆发——它们本身就是高效配体，稍作改造就能变成显像剂。图5：PSMA靶向成像药物所有PSMA探针共享一个核心结合基序Glu‑urea‑Lys，这是它们能高特异性结合的关键，也是诊疗一体化药物能成功的结构基础。图6：FAP靶向成像 FAPI探针之所以能“横扫28种癌”，正是因为它靶向肿瘤微环境里的癌相关成纤维细胞，而不是局限于某一种肿瘤抗原，这种“泛肿瘤”能力让它迅速成为爆款。第四类是抗体及大分子探针，也就是免疫PET。抗体的特异性极高、亲和力极强，适合HER2、EGFR、PD‑1、PD‑L1、CD8等靶点。但抗体分子量大、代谢慢，必须搭配⁸⁹Zr、¹²⁴I这类长半衰期核素。它的价值不在于常规诊断，而在于指导免疫治疗、抗体药、ADC患者筛选——先显像看靶点表达，再决定用药，真正实现“先测后治”。图7：PD‑1/PD‑L1成像免疫PET的革命性意义，在于能看到全身病灶的靶点异质性，解决穿刺活检“以点代面”的局限，让免疫治疗不再盲目。除此之外，还有通过高通量化合物筛选得到的高亲和力探针，比如LLP2A这类靶向整合素的分子，它们往往亲和力达到皮摩尔级，为难以成药的靶点提供新可能。图8：LLP2A靶向整合素α₄β₁ 这类分子来自超大文库的迭代筛选，代表了“从随机筛选到精准设计”的研发趋势。四、放射化学：核素怎么选、怎么标，是技术核心很多人以为PET药物就是“随便贴个放射性原子”，真相是：核素选择与标记策略，直接决定药物能不能用、好不好用。核素选择有一条黄金法则：核素的物理半衰期，必须和分子的生物半衰期匹配。表 2 PET 常用核素关键参数核素半衰期衰变模式平均 β+ 能量 (MeV) 水中正电子平均射程 (mm) 制备方式 ¹¹C 20.4 min β+(99.8%) 0.386 1.2 ¹⁴N(p,α)¹¹C ¹³N 10.0 min β+(99.8%) 0.492 1.8 ¹⁶O(p,α)¹³N ¹⁵O 2.0 min β+(99.9%) 0.735 3.0 ¹⁵N(p,n)¹⁵O ¹⁸F 109.7 min β+(96.7%) 0.250 0.6 ¹⁸O(p,n)¹⁸F ⁴⁴Sc 4.0 h β+(94.3%) 0.632 2.4 ⁴⁴Ti/⁴⁴Sc 发生器 ⁶⁴Cu 12.7 h β+(17.6%) 0.278 0.7 ⁶⁴Ni(p,n)⁶⁴Cu ⁶⁸Ga 67.7 min β+(88.9%) 0.836 3.5 ⁶⁸Ge/⁶⁸Ga 发生器 ⁸²Rb 1.3 min β+(81.8%) 1.535 7.1 ⁸²Sr/⁸²Rb 发生器 ⁸⁶Y 14.7 h β+(11.9%) 0.535 1.9 ⁸⁶Sr(p,n)⁸⁶Y ⁸⁹Zr 78.4 h β+(22.7%) 0.396 1.3 ⁸⁹Y(p,n)⁸⁹Zr ¹²⁴I 100.2 h β+(11.7%) 0.687 2.8 124Te(p,n)124I 小分子、多肽代谢快，用¹⁸F、⁶⁸Ga；抗体代谢慢，用⁸⁹Zr、¹²⁴I；不匹配，要么核素衰变完了药物还没到肿瘤，要么药物清完了核素还在辐射。同时还要考虑：正电子射程越短，图像分辨率越高；摩尔比活度越高，探针用量越少，安全性越好；制备越简单，越容易临床落地。标记方法主要分三类：直接标记、辅基标记、金属螯合。其中金属螯合因为稳定、高效、易于自动化，成为诊疗一体化药物的首选——DOTA、NOTA、DFO这些螯合剂，既能标诊断核素⁶⁸Ga、⁸⁹Zr，也能标治疗核素¹⁷⁷Lu、²²⁵Ac，实现“同一分子，既可显像，又可治疗”。图9：放射性药物自动化合成模块临床落地的最后一关，是自动化合成与质控。只有能在热室内全自动、稳定、高产率制备，并通过无菌、内毒素、放射化学纯度等严格质控，才算真正走完研发闭环。五、一套完整的“闯关体系”，决定能否上临床实验室做得漂亮，不代表动物有效；动物有效，不代表人体安全。PET药物临床前必须完成一套严谨评价：首先在体外测结合亲和力、内吞、稳定性、血浆蛋白结合；然后在动物身上做PET成像、活体分布、阻断实验，验证特异性与药代；接着计算辐射剂量，确保人体安全；最后做急性毒性，因为PET药物是“微量给药”，毒理评价可以简化，但不能省略。这套体系不是为了走流程，而是为了回答一个终极问题：这个探针，在人体内是否安全、是否有效、是否可重复？六、监管与转化，PET药物的最大优势，是“微剂量、快通道” 对创新药来说，最难的往往是临床转化。但PET药物拥有天然优势：给药量极低（微量）、无药理作用、辐射剂量低。因此全球监管机构（FDA、EMA、ICH）都为PET核药开通简化评价路径：非临床要求更宽松、探索性IND（eIND）更快获批，让优秀探针能快速进入人体试验。这也是为什么最近十年，新型PET药物获批速度明显加快——研发逻辑顺、技术路径成熟、监管政策友好，三者共振。七、终极洞察：未来PET药物的决胜点，不是“新”，而是“准、简、能用” 纵观整个研发体系，真正的行业洞察藏在最后：能成功的PET药物，从来不是结构最复杂、文章最亮眼的，而是满足三点：靶点真有用、分子够简单、临床能落地。未来的趋势早已清晰：第一，诊疗一体化：一个分子，既能显像，又能治疗；第二，免疫PET：指导免疫治疗，解决“谁有效、谁无效”；第三，泛肿瘤探针：如FAPI，覆盖更多癌种；第四，自动化、试剂盒化：让基层医院也能轻松制备。 PET不只是一种影像，它是肿瘤精准医疗的入口。从分子设计到核素选择，从动物实验到临床转化，每一步都在回答同一个问题：如何让肿瘤无处遁形，让治疗有的放矢。在精准医疗的时代，谁掌握了更好的PET显像剂，谁就掌握了肿瘤诊疗的未来。声明本文为作者基于公开文献、公开报道及行业资料整理形成的观点性内容，仅用于学术与产业交流。文中若涉及相关研究团队、机构或个人成果，如存在引用不当、理解偏差或可能影响相关权益的情况，欢迎及时联系作者，我们将第一时间核实并做出修订或删除处理。

放射疗法

2022-06-27

·GlobeNewswire-Health Care

Curium Announces the Submission of its Marketing Authorization Application for [18F]-DCFPyL to the European Medicines Agency

PARIS, June 27, 2022 (GLOBE NEWSWIRE) -- Curium the world’s leading nuclear medicine company, today announced the submission of its Marketing Authorization Application for [18F]-DCFPyL to the European Medicines Agency. The submission comes two months after completing its Phase III PYTHON trial of [18F]-DCFPyL and follows two US pivotal trials – OSPREY and CONDOR by Progenics Pharmaceuticals, Inc., a Lantheus company. In the U.S., [18F]-DCFPyL was approved by the FDA in May of 2021 and is commercially available as PYLARIFY® (Piflufolastat F 18 Injection) and sold by Lantheus. Sakir Mutevelic, MD, MSc, Chief Medical Officer at Curium commented: “The positive results of our Phase III PYTHON clinical trial conducted in Europe reinforce the diagnostic performance of [18F]-DCFPyL in the pivotal OSPREY and CONDOR clinical trials in multiple stages of prostate cancer disease, confirming our belief in [18F]-DCFPyL and the role it will play in helping Curium to redefine the experience of cancer.” Benoit Woessmer, PET Europe Chief Executive Officer at Curium added: “With the completion of the PYTHON clinical trial and the submission of our Marketing Authorization Application to the European Medicines Agency, Curium demonstrates its continued dedication and commitment to developing life-saving diagnostic solutions for cancer patients around the world. With our state-of-the-art PET radiopharmacy network – the largest in Europe, Curium will be ready to make the product available across Europe post approval in order to make an everyday impact on patients and people.” PYTHON Study The PYTHON Study (NCT04734184) was a Phase III, European, multicenter, prospective cross-over comparison trial, to evaluate and compare the detection rates, impact on patient management and safety proﬁles between [18F]-DCFPyL and [18F]-Fluorocholine (the current approved and established gold standard for PET/CT imaging of prostate cancer in Europe), in patients with first biochemical recurrence (BCR) after initial definitive therapy with curative intent. This study successfully met the primary endpoint. The details of the PYTHON study and the clinical results will be presented at the 35th Annual Congress of the European Association of Nuclear Medicine, October 15-19, 2022 in Barcelona, Spain. PYLARIFY® (piflufolastat F 18) Injection In the U.S., [18F]-DCFPyL was approved by the FDA in May of 2021 and is commercially available as PYLARIFY® (Piflufolastat F 18 Injection) and sold by Lantheus. U.S. Indication PYLARIFY® (piflufolastat F 18) Injection is a radioactive diagnostic agent indicated for positron emission tomography (PET) of prostate-specific membrane antigen (PSMA) positive lesions in men with prostate cancer: with suspected metastasis who are candidates for initial definitive therapy with suspected recurrence based on elevated serum prostate-specific antigen (PSA) level Important Safety Information Contraindications None. Warnings and Precautions Risk of Image Misinterpretation Imaging interpretation errors can occur with PYLARIFY imaging. A negative image does not rule out the presence of prostate cancer and a positive image does not confirm the presence of prostate cancer. The performance of PYLARIFY for imaging of patients with biochemical evidence of recurrence of prostate cancer seems to be affected by serum PSA levels. The performance of PYLARIFY for imaging of metastatic pelvic lymph nodes prior to initial definitive therapy seems to be affected by risk factors such as Gleason score and tumor stage. PYLARIFY uptake is not specific for prostate cancer and may occur with other types of cancer as well as non-malignant processes and in normal tissues. Clinical correlation, which may include histopathological evaluation of the suspected prostate cancer site, is recommended. Hypersensitivity Reactions Monitor patients for hypersensitivity reactions, particularly patients with a history of allergy to other drugs and foods. Reactions may be delayed. Always have trained staff and resuscitation equipment available. Radiation Risks Diagnostic radiopharmaceuticals, including PYLARIFY, expose patients to radiation. Radiation exposure is associated with a dose-dependent increased risk of cancer. Ensure safe handling and preparation procedures to protect patients and health care workers from unintentional radiation exposure. Advise patients to hydrate before and after administration and to void frequently after administration. Adverse Reactions The most frequently reported adverse reactions were headaches, dysgeusia and fatigue, occurring at rate of ≤2% during clinical studies with PYLARIFY. In addition, a delayed hypersensitivity reaction was reported in one patient (0.2%) with a history of allergic reactions. Drug interactions Androgen deprivation therapy (ADT) and other therapies targeting the androgen pathway, such as androgen receptor antagonists, may result in changes in uptake of PYLARIFY in prostate cancer. The effect of these therapies on performance of PYLARIFY PET has not been established. To report suspected adverse reactions for PYLARIFY, call 1-800-362-2668 or contact FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. For important risk and use information about PYLARIFY Injection, please see Full Prescribing information. About Curium Curium is the world’s largest nuclear medicine company. We develop, manufacture and distribute world-class radiopharmaceutical products to help patients around the globe. Our proven heritage combined with a pioneering approach are the hallmarks to deliver innovation, excellence and unparalleled service. With manufacturing facilities across Europe and the United States, Curium delivers SPECT, PET and therapeutic radiopharmaceutical solutions for life-threatening diseases to over 14 million patients annually. The name ‘Curium’ honors the legacy of pioneering radioactive materials researchers Marie and Pierre Curie, after whom the radioactive element curium was named and emphasizes our focus on nuclear medicine. To learn more, visit curiumpharma.com.

引进/卖出诊断试剂

100 项与 18F-Fluorocholine 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D11254	-	V09	DB15887

研发状态

批准上市

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
肝癌	意大利	-	2014-02-03
前列腺癌	意大利	-	2014-02-03

未上市

10 条进展最快的记录,

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适应症	最高研发状态	国家/地区	公司	日期
局限性前列腺癌	临床3期	法国	ABX advanced biochemical compounds GmbH	2019-03-06
复发性前列腺癌	临床3期	法国	ABX advanced biochemical compounds GmbH	2019-03-06

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临床结果

适应症

分期

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT03764007 (CTgov)	临床2/3期	原发性甲状旁腺功能亢进症 \| 甲状旁腺腺瘤	98	Positron Emission Tomography (PET)+18F-Fluorocholine	窪夢選築顧廠鑰憲壓願 = 築窪簾範簾觸壓蓋壓壓艱構糧網憲範鏇醖衊憲 (鏇蓋夢蓋廠憲鏇膚築齋, 膚網壓窪獵襯糧蓋願鏇 ~ 鹹淵簾範鏇齋鹹醖遞窪) 更多	-	2021-10-19
NCT02397408 (CTgov)	临床2期	前列腺癌	18	Positron Emission Tomography (PET) / Magnetic Resonance Imaging (MRI)+Carbon C 11 Choline+Fluorine F 18 Choline	醖鑰夢膚衊膚範壓蓋醖(簾餘襯觸遞獵鏇顧鬱醖) = 積廠範繭膚廠獵築淵糧範範鏇糧憲壓繭夢鑰夢 (繭鹹鏇膚積願鏇淵鬱繭, 顧願鹹繭夢獵鬱範顧築 ~ 鹽願淵憲鏇襯憲觸壓鹹) 更多	-	2020-11-19
EANM2019	N/A	甲状腺髓样癌 calcitonin \| CEA levels	20	18 F-Fluorocholine PET/CT	觸膚廠網遞壓獵遞鏇窪(構淵壓衊壓夢構膚鹹衊) = 淵鹽獵鬱範齋齋顧觸窪願鹽獵淵餘獵憲艱願膚 (願衊窪築壓鏇繭夢顧襯, 7.3 ~ 35.5) 更多	-	2019-09-18
ACTRN12608000641392 (ASCO_GU2019)	临床2/3期	前列腺癌一线 \| 二线	108	Fluorocholine-PET/CT	窪膚鹹繭繭淵夢襯壓獵(淵鹹衊鹽願築遞夢齋壓) = 鏇蓋積觸願膚窪遞願顧襯觸鹹廠齋壓衊鹹範鏇 (醖網齋鹹構觸淵齋獵積, 2 ~ 68) 更多	积极	2019-02-26
ACTRN12608000641392 (ASCO_GU2019)	临床2/3期	前列腺癌一线 \| 二线	108	fluorocholine-PET/CT (Computed Tomography + 99mTc-Whole Body Bone Scan)	窪膚鹹繭繭淵夢襯壓獵(淵鹹衊鹽願築遞夢齋壓) = 衊艱觸簾壓艱衊壓簾鹽襯觸鹹廠齋壓衊鹹範鏇 (醖網齋鹹構觸淵齋獵積, 1 ~ 16)	积极	2019-02-26
NCT00928174 \| NCT00928252 (Pubmed \| J Nucl Med)	临床1/2期	去势抵抗性前列腺癌	-	Chemotherapy	衊壓願獵鑰願遞餘糧襯(餘願願構構鹹淵蓋簾齋) = 製齋膚膚鬱構構襯簾醖鬱鬱鏇淵製遞製窪網顧 (窪構齋觸鏇簾廠齋襯醖 )	-	2016-07-01
NCT00928174 \| NCT00928252 (Pubmed \| J Nucl Med)	临床1/2期	去势抵抗性前列腺癌	-	<sup>18</sup>F-fluorocholine (Antiandrogens)	衊壓願獵鑰願遞餘糧襯(餘願願構構鹹淵蓋簾齋) = 襯淵築鏇鏇衊窪鹽齋範鬱鬱鏇淵製遞製窪網顧 (窪構齋觸鏇簾廠齋襯醖 )	-	2016-07-01
ASCO_GU2016	N/A	前列腺癌	42	Salvage focal FCH PET+ stereotactic radiation therapy (sf-SRT)	製鏇顧簾積積範膚觸鑰(鏇製網鹹衊夢醖積醖糧) = no difference was observed for GI toxicities between the 2 groups (p = 0.26) 蓋夢築鏇鏇積窪憲憲壓 (獵網衊壓夢窪夢簾憲積 ) 更多	积极	2016-01-10
ASCO_GU2016	N/A	前列腺癌	42	Salvage elective nodal irradiation with a protracted FCH PET+ nodal boost (seni-PRT)		积极	2016-01-10
NCT00928174 (CTgov)	临床1/2期	去势抵抗性前列腺癌	27	IV administration of fluorine-18 fluorocholine followed by PET/CT imaging	觸製範鏇窪觸齋網選膚 = 鹹齋齋襯衊築蓋繭獵簾壓鏇蓋製蓋鏇築製糧願 (網顧夢鹹夢築網鏇顧鏇, 範觸繭壓選廠鹹選築鏇 ~ 艱壓夢廠構衊選簾範糧) 更多	-	2014-11-19