预约演示

更新于：2025-05-10

Fluciclovine 18F

更新于：2025-05-10

概要

概要

基本信息

药物类型

小分子化药、诊断用放射药物

别名

(18F)FACBC、(1R,3R)-1-amino-3(18F)fluorocyclobutane-1-carboxylic acid、18F fluciclovine

+ [27]

靶点

KLK3

作用方式

抑制剂

作用机制

KLK3抑制剂(前列腺特异性抗原抑制剂)

治疗领域

肿瘤神经系统疾病泌尿生殖系统疾病+ [4]

在研适应症

复发性恶性胶质瘤诊断试剂前列腺癌+ [21]

非在研适应症

骨转移癌头颈部肿瘤高级别胶质瘤+ [7]

原研机构

Emory University

在研机构

Emory University

Blue Earth Diagnostics Ltd.

National Institutes of Health

+ [5]

非在研机构

GE Healthcare Holdings, Inc.

Memorial Sloan Kettering Cancer Center

权益机构

Nihon Medi-Physics Co., Ltd.

Seibersdorf Labor GmbH

Winship Cancer Institute of Emory University

+ [3]

最高研发阶段批准上市

首次获批日期

美国 (2016-05-27),

前列腺癌

最高研发阶段(中国)-

特殊审评孤儿药 (美国)、孤儿药 (欧盟)

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结构/序列

分子式C5H8FNO2

InChIKeyNTEDWGYJNHZKQW-DGMDOPGDSA-N

CAS号222727-39-1

关联

项与 Fluciclovine 18F 相关的临床试验

NCT06613841

/ Recruiting早期临床1期IIT

Pilot Study to Evaluate Multitracer [18F]Fluciclovine and 18F-FDG PET, and Advanced MRI Methods at 7Tesla Metabolic Profiling of Glioblastoma

* To perform metabolic phenotyping of treatment naïve and recurrent GBM by multitracer [18F]Fluciclovine and 18F-FDG PET.
* To compare uptake measures of 18F-Fluciclovine and 18F-FDG and MRI quantification of glutamate and lactate levels to tumor tissue laboratory assays (RNA seq and proteomics) of glutamine/glutamate, glucose, and lactate metabolism.
* To perform metabolic phenotyping of treatment naïve and recurrent GBM by advanced MRI methods at 7 Tesla

开始日期2025-05-01

申办/合作机构

Abramson Cancer Center

NCT05555550

/ Recruiting早期临床1期

Evaluation of 18F-Fluciclovine PET-MRI as a Biomarker of Response in Pediatric and Young Adult Patients With Low Grade Gliomas (LGG)

The purpose of this study is to see if 18F-Fluciclovine (Axumin®) is useful and safe in the management of children with Low Grade Gliomas (LGG). Imaging with 18F-Fluciclovine PET-MRI will be performed prior to initiation of therapy for LGG, and then 3 months, and 1 year after starting therapy. Changes in 18F-Fluciclovine uptake will be compared to changes in MRI measurements at 3 months and 1 year as compared to baseline.

开始日期2025-03-03

申办/合作机构

The Children's Hospital of Philadelphia

[+1]

NCT06706921

/ Recruiting临床4期IIT

Usefulness of Tumor Heterogeneity Assessment in Patients With MCRPC Undergoing Radioligand Therapy With 177LU-PSMA-617 Using Serial 18F-DCFPYL, 18F-FDG and 18F-Fluciclovine PET/CT Predicting Clinical Outcome

This a single-center, prospective, exploratory study. Patients with metastatic castration-resistant prostate cancer (mCRPC) scheduled to undergo Lutetium labelled prostate-specific membrane antigen radioligand therapy (LuPSMA RLT) at the West Los Angeles VA (WLA-VA) will be imaged with a baseline F-18 fluorodeoxyglucose positron emission tomography/computed tomography 18F-FDG PET/CT and a 18F-DCFPyL PET/CT (18F-DCFPyL (2-(3-{1-carboxy-5-[(6-18F-fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-pentanedioic acid)positron emission tomography/computed tomography , as per standard of care in our institution. All patients further undergo eventual follow-up prostate-specific membrane antigen positron emission tomography (PSMA PET) after the 2nd, 4th, and 6th LuPSMA RLT cycle. In this prospective study, an18F-Fluciclovine positron emission tomography/computed tomography ( Axumin PET/CT )will be additionally obtained at baseline (pre-LuPSMA RLT), and after the 2nd, 4th, 6th LuPSMA RLT cycles. Axumin PET/CT will be acquired within 7 days from the PSMA PET.
This study is open to Veterans only.

开始日期2024-12-15

申办/合作机构-

100 项与 Fluciclovine 18F 相关的临床结果

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100 项与 Fluciclovine 18F 相关的转化医学

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100 项与 Fluciclovine 18F 相关的专利（医药）

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192

项与 Fluciclovine 18F 相关的文献（医药）

2025-03-01·Therapeutic Advances in Urology

The expanding role of next-generation imaging in prostate cancer management: a cross-sectional survey exploring the clinical practice of uro-oncologists in North-Eastern Italy; on behalf of GUONE (Gruppo Uro-Oncologico del Nord-Est)

Article

作者: Antonelli, Alessandro ; Matrone, Fabio ; Guttilla, Andrea ; Campo, Irene ; Brunelli, Matteo ; Andrea Signor, Marco ; Artioli, Paolo ; Girometti, Rossano ; Bortolus, Roberto ; Urso, Luca ; Caliò, Anna ; Gardi, Mario ; De Vivo, Rocco ; Caffo, Orazio ; Zattoni, Fabio ; Veccia, Alessandro ; Montesi, Giampaolo ; Evangelista, Laura ; Basso, Umberto ; Polesel, Jerry ; Pierantoni, Francesco ; Cimadamore, Alessia ; Giannarini, Gianluca ; Salgarello, Matteo ; Orlando, Valentina ; Sepulcri, Matteo ; Ongaro, Luca ; Sachs, Camilla ; Munari, Enrico ; Alongi, Filippo

Background::

Next-generation imaging (NGI) technologies such as multiparametric magnetic resonance imaging (mpMRI) and total-body NGI (tbNGI) methodologies including choline, fluciclovine or PSMA positron emission tomography/computed tomography (PET/CT), whole-body MRI (wbMRI), and PET/MRI are becoming increasingly available, but their use in different prostate cancer (PCa) settings is under debate. The Gruppo Uro-Oncologico del Nord-Est (GUONE) designed a survey to explore the current clinical practice of NGI utilization in a specific macro-region in North-Eastern Italy.

Methods::

A cross-sectional survey was conducted by administering an anonymous online multiple-choice questionnaire to uro-oncologists practicing in North-Eastern Italy, using the Google Forms ® platform. The use of NGI was investigated in the following settings: primary staging of PCa; management of biochemical (BCR) and local recurrence (LR); re-staging in metastatic hormone-sensitive PCa (mHSPC), metastatic castration-resistant PCa (mCRPC), non-metastatic CRPC (nmCRPC), and oligometastatic PCa (OMPC).

Results::

In all, 100 uro-oncologists accessed and completed the survey. In primary N/M staging, the use of tbNGI increases in accordance with NCCN risk groups. Re-staging with choline and PSMA PET/CT is the prevalent choice in the case of BCR after radical prostatectomy. Moreover, when the PSA value rises, there is a parallel increased use of tbNGI. When an LR is suspected, PSMA PET/CT plus mpMRI is the most selected option. Re-staging with tbNGI (PSMA PET/CT) is preferred in mHSPC, mCRPC, and nmCRPC patients in case of progression of disease. Overall, there is a limited use of wbMRI and PET/MRI in all the settings investigated.

Conclusion::

Our survey describes the expanding role of NGI modalities in the management of PCa patients, from primary staging and re-staging to management of advanced PCa and assessment of treatment response. Several controversial issues have emerged, which need to be addressed in prospective studies to develop a standardized and cost-effective NGI utilization.

2025-01-25·Cureus Journal of Medical Science

Timing and Patterns of Potentially Salvageable Recurrences Following Stereotactic Body Radiosurgery for Clinically Localized Prostate Cancer Assessed by Preferential Amino Acid Uptake

Article

作者: Kearney, Tim ; Danner, Malika ; Esposito, Giuseppe ; Zwart, Alan L ; Collins, Sean ; Suy, Simeng ; Carrasquilla, Michael ; Kumar, Deepak ; Nagel, Lauren ; Bourne, Matthew

PURPOSE:

18F-fluciclovine is a radiolabeled amino acid analog that is preferentially taken up by prostate cancer cells. 18F-fluciclovine PET/CT scans are approved for the detection of biochemically recurrent prostate cancer. Stereotactic body radiation therapy (SBRT) is increasingly offered for the treatment of localized prostate cancer. Limited data exist on the patterns of failure following prostate SBRT. The impact of scan timing before or after meeting the Phoenix criteria is unknown. Here, we characterize 18F-fluciclovine-defined recurrences for patients with rising prostate-specific antigens (PSAs) following SBRT.

METHODS:

Between 2017 and 2022, 50 consecutive patients underwent an 18F-fluciclovine scan for suspected recurrence. All patients were treated on an institutional protocol with either SBRT (35-36.25 Gy) or SBRT boost (19.5 Gy) with intensity-modulated radiotherapy (IMRT). A total of 38% of the patients were high-risk, and 46% received androgen deprivation therapy (ADT) as part of their initial treatment. Patterns of failure were classified as PSA-only, local (prostate), lymph node (LN), bone, visceral, or combined. Patients were considered salvageable if all evidence of disease could be safely treated with local therapy (radiation, surgery, or interventional radiology (IR) ablation).

RESULTS:

The median time from treatment was 39 months, and the median pre-scan PSA was 2.8 ng/mL. The overall scan positivity rate in our cohort was 34/51 (67%). The most common sites for initial disease recurrence were the prostate (22%), pelvic and para-aortic lymph node basins (40%), and bone (6%). A total of 21/51 scans (41%) were performed prior to reaching the Phoenix definition (nadir + 2) at a median PSA of 1.14 ng/mL. Of these patients, 12 (57%) had evidence of disease recurrence, all of which were potentially salvageable local or LN recurrences. The remaining 30/51 (59%) scans were performed after meeting the Phoenix definition (median PSA = 5.65 ng/mL). Of these, 22/30 (73%) had disease recurrence and 82% were potentially salvageable.

CONCLUSIONS:

The diagnosis and management of recurrence following prostate SBRT continues to evolve. Approximately 50% of patients in our cohort who had yet to meet the Phoenix definition had scan evidence of disease recurrence, all of which were potentially salvageable with additional local therapy. Additional research is needed to identify factors predictive of disease recurrence on 18F-fluciclovine scans prior to reaching the Phoenix definition when they may be most curable.

2025-01-01·ANNALS OF NUCLEAR MEDICINE

Phantom test procedures for a new neuro-oncological amino acid PET tracer: [18F]fluciclovine

Article

作者: Kamitaka, Yuto ; Wagatsuma, Kei ; Yokotsuka, Noriyo ; Tsuzura, Kaede ; Kamiya, Takashi ; Ishii, Kenji ; Miwa, Kenta ; Miyaji, Noriaki

OBJECTIVE:

Amino acid positron emission tomography (PET) examinations using anti-1-amino-3-[¹⁸F]-fluorocyclobutane-1-carboxylic acid ([¹⁸F]FACBC) were allowed for routine clinical use in July 2024. However, phantom test procedures for [¹⁸F]FACBC reconstruction parameters have not yet been established. The present study aimed to establish new phantom test procedures for [¹⁸F]FACBC brain PET imaging to determine optimal reconstruction parameters.

METHODS:

Background (BG) activity as well as hot sphere and target-to-background ratios (TBRs) of [¹⁸F]FACBC were estimated based on brain activity and tumor-to-normal tissue ratios (TNR) in a Japanese clinical trial of [¹⁸F]FACBC. Phantom experiments proceeded under [¹⁸F]FACBC or L-[methyl-¹¹C]-methionine ([¹¹C]MET) conditions. The number of iterations and the Gaussian filter parameters were determined from the reconstruction parameters %contrast_mean and coefficients of variation (CVs) in ordered subset expectation maximization (OSEM) and time-of-flight (TOF) with or without point-spread-function (PSF) correction.

RESULTS:

The amounts of activity in the hot spheres and BG were 1.1 and 5.5 kBq/mL, respectively, and the TBR was 5.0 at the start of acquisition. The %contrast_mean of all hot spheres was higher with [¹⁸F]FACBC than [¹¹C]MET, and %contrast_mean converged between 4 and 6 iterations in hot spheres with diameters < 10 mm. We used four iterations for OSEM + TOF and five for OSEM + TOF + PSF correction for [¹⁸F]FACBC and [¹¹C]MET images. The CV was higher for [¹⁸F]FACBC than [¹¹C]MET. The optimal sizes of Gaussian filters for OSEM + TOF and OSEM + TOF + PSF correction of image reconstruction were 5 mm for [¹⁸F]FACBC, and 4 and 3 mm, respectively, for [¹¹C]MET images.

CONCLUSIONS:

We estimated phantom activity and TBR based on brain activity in a Japanese clinical trial and established new phantom test procedures for [¹⁸F]FACBC. We recommend that the optimal reconstruction parameters for [¹⁸F]FACBC should be set to the same number of iterations as [¹¹C]MET and that the FWHM of Gaussian filter should have a few mm higher than [¹¹C]MET to reduce image noise from brain normal tissue.

项与 Fluciclovine 18F 相关的新闻（医药）

2024-11-04

·Business Wire

Blue Earth Diagnostics, a Bracco Company, Applauds New CMS Rule to Support Patient Access Through Improved Payment for Specialized Diagnostic Radiopharmaceuticals

MONROE TOWNSHIP, N.J., & OXFORD, England--( BUSINESS WIRE )--Blue Earth Diagnostics, a Bracco company and recognized leader in the development and commercialization of innovative PET radiopharmaceuticals, welcomes changes announced by the Centers for Medicare & Medicaid Services (CMS) for the Hospital Outpatient Prospective Payment System (OPPS) Rule on November 1, 2024. The rule, which goes into effect January 1, 2025, is designed to improve payments for diagnostic radiopharmaceuticals for U.S. Medicare patients, and has the potential to increase sustained access to innovative radiopharmaceuticals. “ We are very pleased that CMS has updated this rule, which will increase patient access to advanced diagnostic imaging products to inform patient management and treatment,” said Marco Campione, Chief Executive Officer of Blue Earth Diagnostics. “ This action will foster additional innovation and sustainability in nuclear medicine and molecular imaging, aligning with our company commitment to deliver leading-edge radiopharmaceutical solutions for improved patient care.” “ Since its inception, Blue Earth Diagnostics has championed the need for reimbursement reform around CMS payment methodology for diagnostic radiopharmaceuticals. This rule corrects a significant reimbursement gap that previously hampered the adoption of innovative radiopharmaceutical products, and patient access,” said Terri Wilson, President, Blue Earth Diagnostics. “ It supports Blue Earth Diagnostics’ entire portfolio of diagnostic imaging agents. POSLUMA ® (flotufolastat F 18) maintains its current Pass-Through payment status until September 30, 2026. Axumin ® (fluciclovine F 18), which previously lost Pass-Through status in January 2020, will regain separate payment under this new rule. Although the updated payment methodology provides for separate payment for diagnostic radiopharmaceuticals, payment will differ for Pass-Through and non-Pass-Through diagnostic radiopharmaceuticals. Our field reimbursement team continues to work with hospitals to ensure they understand the new rule and its implications.” Indication and Important Safety Information About Axumin INDICATION Axumin ® (fluciclovine F 18) injection is indicated for positron emission tomography (PET) imaging in men with suspected prostate cancer recurrence based on elevated blood prostate specific antigen (PSA) levels following prior treatment. IMPORTANT SAFETY INFORMATION Image interpretation errors can occur with Axumin PET imaging. A negative image does not rule out recurrent prostate cancer and a positive image does not confirm its presence. The performance of Axumin seems to be affected by PSA levels. Axumin uptake may occur with other cancers and benign prostatic hypertrophy in primary prostate cancer. Clinical correlation, which may include histopathological evaluation, is recommended. Hypersensitivity reactions, including anaphylaxis, may occur in patients who receive Axumin. Emergency resuscitation equipment and personnel should be immediately available. Axumin use contributes to a patient’s overall long-term cumulative radiation exposure, which is associated with an increased risk of cancer. Safe handling practices should be used to minimize radiation exposure to the patient and health care providers. Adverse reactions were reported in ≤ 1% of subjects during clinical studies with Axumin. The most common adverse reactions were injection site pain, injection site erythema and dysgeusia. To report suspected adverse reactions to Axumin, call 1-855-AXUMIN1 (1-855-298-6461) or contact FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . Full Axumin prescribing information is available at https://www.axumin.com/prescribing-information.pdf . Indication and Important Safety Information About POSLUMA INDICATION POSLUMA ® (flotufolastat F 18) injection is 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 Image interpretation errors can occur with POSLUMA PET. 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 POSLUMA for imaging metastatic pelvic lymph nodes in patients prior to initial definitive therapy seems to be affected by serum PSA levels and risk grouping. The performance of POSLUMA for imaging patients with biochemical evidence of recurrence of prostate cancer seems to be affected by serum PSA levels. Flotufolastat F 18 uptake is not specific for prostate cancer and may occur in other types of cancer, in non-malignant processes, and in normal tissues. Clinical correlation, which may include histopathological evaluation, is recommended. Risk of Image Misinterpretation in Patients with Suspected Prostate Cancer Recurrence: The interpretation of POSLUMA PET may differ depending on imaging readers, particularly in the prostate/prostate bed region. Because of the associated risk of false positive interpretation, consider multidisciplinary consultation and histopathological confirmation when clinical decision-making hinges on flotufolastat F 18 uptake only in the prostate/prostate bed region or only on uptake interpreted as borderline. POSLUMA use contributes to a patient’s overall long-term cumulative radiation exposure. Long-term cumulative radiation exposure is associated with an increased risk for cancer. Advise patients to hydrate before and after administration and to void frequently after administration. Ensure safe handling to minimize radiation exposure to the patient and health care providers. The adverse reactions reported in ≥0.4% of patients in clinical studies were diarrhea, blood pressure increase and injection site pain. 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 flotufolastat F 18 in prostate cancer. The effect of these therapies on performance of POSLUMA PET has not been established. To report suspected adverse reactions to POSLUMA, call 1-844-POSLUMA (1-844-767-5862) or contact FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . Full POSLUMA prescribing information is available at www.posluma.com/prescribing-information.pdf . About Blue Earth Diagnostics Blue Earth Diagnostics, an indirect subsidiary of Bracco Imaging S.p.A., is a growing international molecular imaging company focused on delivering innovative, well-differentiated diagnostic solutions that inform patient care. Formed in 2014, the Company’s success is driven by its management expertise and supported by a demonstrated track record of rapid development and commercialization of positron emission tomography (PET) radiopharmaceuticals. Blue Earth Diagnostics’ expanding oncology portfolio encompasses a variety of disease states, including prostate cancer and neuro-oncology. Blue Earth Diagnostics is committed to the timely development and commercialization of precision radiopharmaceuticals for potential use in imaging and therapy. For more information, please visit: www.blueearthdiagnostics.com . About Bracco Imaging Bracco Imaging S.p.A., part of the Bracco Group, is a world-leading diagnostic imaging provider. Headquartered in Milan, Italy, Bracco Imaging develops, manufactures and markets diagnostic imaging agents and solutions. It offers a product and solution portfolio for all key diagnostic imaging modalities: X-ray imaging (including Computed Tomography-CT, Interventional Radiology, and Cardiac Catheterization), Magnetic Resonance Imaging (MRI), Contrast Enhanced Ultrasound (CEUS), and Nuclear Medicine through radioactive tracers and novel PET imaging agents to inform clinical management and guide care for cancer patients in areas of unmet medical need. Our continually evolving portfolio is completed by a range of medical devices, advanced administration systems and dose-management software. In 2019 Bracco Imaging enriched its product portfolio by expanding the range of oncology nuclear imaging solutions in the urology segment and other specialties with the acquisition of Blue Earth Diagnostics. In 2021, Bracco Imaging established Blue Earth Therapeutics as a separate, cutting-edge biotechnology vehicle to develop radiopharmaceutical therapies. Visit: www.braccoimaging.com . PP-rh-US-0581 This press release is for U.S. audiences only

放射疗法诊断试剂并购

2024-10-31

·ioncology

Nat Rev Cancer丨前列腺癌的PSMA表达、调控和异质性分析

点击上方蓝字关注我们编者按：近年来，去势抵抗性前列腺癌（CRPC）的治疗取得了显著进步；同时，前列腺特异性膜抗原（PSMA）作为前列腺癌分子成像和治疗靶点，也已经取得了突破性进展，如：PSMA-PET成像可显著提高前列腺癌定位精确程度，177Lu-PSMA-617为前列腺癌患者带来全新治疗策略等等。近期，Nature子刊发表了一篇综述，总结了当前PSMA表达、调控及其异质性的研究，并分析了临床应用前景。本刊特别整理，以期为精准治疗提供更多思路。前列腺中的PSMA表达前列腺是由上皮组织和纤维肌肉基质组成的外分泌腺（图1）。在微观层面上，PSMA主要在腔上皮的分泌细胞中表达，尤其是在AR阳性的腔上皮细胞中；而基质细胞和少量神经内分泌细胞几乎不表达PSMA。尽管PSMA不在正常血管的内皮细胞中表达，但在多种实体肿瘤的血管生成过程中可以上调，包括乳腺癌、肾癌和前列腺癌等。图1 前列腺腔上皮中的PSMA表达靶向PSMA的诊断和治疗方案通过放射性标记，PSMA-PET/CT可将PSMA表达可视化。但应注意，PSMA假阳性可能出现于软组织病变、异常血管增生、创伤或胸腺瘤等。此外，良性前列腺病变中的PSMA，特别是良性前列腺增生和前列腺上皮内瘤变，需要进一步分析。而通过对PSMA-PET/CT成像进行仔细分析，可提高诊断精度。同时，目前也正在开发多种PSMA放射性配体疗法，如表1所示。表1 基于GUL的PSMA放射性配体明确PSMA阳性，改善肿瘤诊断与治疗对PSMA阳性和同质性的界定，对于筛选合适患者进行PSMA靶向治疗至关重要。研究表明，超过95%的原发性前列腺癌具有中高水平的PSMA表达，但这种PSMA高表达情况仅存在于71%的CRPC患者，而神经内分泌型前列腺癌（NEPC）患者中的比例则下降至32%（图2）。图2 前列腺癌发展过程中的PSMA表达抑制分析目前尚无统一的免疫组织化学（IHC）评分系统，临床上主要依赖PSMA-PET成像确定PSMA阳性状态。PSMA-PET/CT图像基于miTNM分类系统中的miPSMA评分（图3），即按照与血液、肝脏和腮腺的摄取量对比进行分级，miPSMA评分为2和3的肿瘤被认为适合PSMA-RLT治疗。图3 确定PSMA阳性对于选择合适患者至关重要在PET成像领域，放射性示踪剂的摄取量使用标准摄取值（SUV）进行半定量评估，不同研究使用的SUV标准不同。此外，骨转移在前列腺癌中很常见，SUVmax比值大于2.2通常用于区分恶性和良性病灶。神经内分泌型前列腺癌（NEPC）通常PSMA表达较低，因此在成像中挑战较大，不同的前列腺癌组织学变异也可能影响成像特征。 PSMA影像筛选PSMA-RLT治疗人群 PSMA阴性病灶无法保留PSMA放射性配体，因此PSMA阴性或同时存在PSMA阳性和阴性病灶的患者通常被排除在PSMA-RLT试验之外。虽然基于PSMA-PET识别PSMA阴性病灶的概念较为简单，但实际操作较为复杂，miPSMA评分为0的病灶可能难以识别。为了增强检测，部分试验使用氟脱氧葡萄糖（FDG）PET作为辅助影像方法，因为其可进一步增强筛选精确程度。此外，也有试验数据表明，放射组学与转录组学结果相符，显示RNA-seq数据具有分析PSMA调控的潜力。区分PSMA异质性与经典肿瘤异质性最新数据显示，PSMA阳性患者且SUVmean高于10时，177Lu-PSMA-617治疗出现缓解的几率更高。SUVmean用于衡量PSMA异质性，包括细胞、肿瘤、患者个体、空间和时间维度差异（图4）。肿瘤异质性通常是指在原发或转移性肿瘤中存在不同的细胞群，这些细胞具有不同的遗传和表型特征。PSMA的异质性可以通过免疫染色和单细胞RNA测序显示，细胞和肿瘤层面均存在PSMA表达的范围差异。2023年一项研究对52例患者的339个CRPC样本的PSMA表达进行了分类，发现存在低/阴性、异质性和均匀高表达三种模式，部分NEPC亚群也存在PSMA高表达。PSMA在CRPC中表达的谱系内时间异质性也很明显，如雄激素剥夺疗法和AR抑制剂（如恩扎卢胺）可提高AR+肿瘤的PSMA表达水平，表明CRPC在不同时间PSMA异质性的细微差别。图4 PSMA异质性的复杂性表明需要采用更细致的方案 PSMA异质性在PSMA诊疗中的表现 PSMA-PET/CT结合了核医学与CT影像，其空间分辨率极限通常在4~5 mm，这意味着限制了肿瘤内部PSMA阳性和阴性只有距离＞4~5 mm才有可能进行明确区分。放射学结果称为“影像学层面的PSMA”，而免疫组织化学识别的PSMA称为“病理学层面的PSMA”，分辨率的差异可能导致二者异质性的产生。临床前研究显示，PSMA表达程度和PSMA+细胞比例，与肿瘤摄取与177Lu-/225Ac-PSMA-617相关的DNA损伤有关。因此，评估PSMA-PET放射配体摄取的均一性可能会改善纳入标准。应承认，目前缺乏对“PSMA阴性”病灶的统一定义。为了提高前列腺癌转移的诊断准确性，PSMA-PET与相应的CT或MRI使用也至关重要，这会直接影响到纳入标准。未来的最佳患者选择可能会受到PSMA成像异质性及其强度的影响。结合其他生物标志物参数，如肿瘤特征、循环肿瘤细胞和循环肿瘤DNA，以及互补的PET成像数据和深度学习图像处理算法，可能有助于进一步改进。 PSMA低表达的分子特征有研究评估了LuCaP系列PDX模型以及UW-TAN和SU2C-PCF患者队列，发现相比PSMA高表达患者，PSMA低表达患者具有显著的全局表达变化，患者的炎症反应、缺氧、上皮-间质转化以及代谢和糖酵解通路增加。 CRPC中PSMA抑制的出现凸显了寻找PSMA以外靶点的需求。目前已经开发了替代放射性配体以识别靶抗原或改进现有临床配体，包括18F-FDG、胆碱、GRPR、DHT放射性标记物和18F-fluciclovine，以及Zr-DFO-DLL3-scFv和Zr-DFO-MSTP2109A等。成纤维细胞活化蛋白（FAP）也因在CRPC基质中的过表达而成为潜在成像靶点。 PSMA相关的精准医疗未来方向 PSMA作为一种细胞表面蛋白，除了PSMA-RLT之外，还被用作其他治疗的靶点，如PSMA靶向T细胞激活剂、CAR-T细胞治疗和抗体偶联药物。为了优化这些治疗方案，需要深入研究PSMA表达水平和反应、耐药的生物标志物。结合PET成像和液体活检，可评估PSMA表达的动态变化，进行个性化治疗计划，并提前检测耐药。新兴技术如3D组织学、空间转录组学和人工智能，也有助于提高对PSMA在前列腺癌中的生物学理解，并推动更多疗法的开发。结论 PSMA是前列腺癌的重要生物标志物和治疗靶点，广泛应用于癌症诊断和治疗。PSMA受多重基因组和表观遗传网络调控，尤其是雄激素受体（AR）的影响。然而，部分晚期前列腺癌患者因PSMA表达丧失，影响了PSMA-RLT的疗效。PSMA表达的异质性及其在转移部位以及耐药机制的复杂性，进一步增加了治疗挑战。应探索放射性同位素以外的PSMA靶向治疗途径，以提升前列腺癌治疗效果。 ▌参考文献： Bakht, Martin K., and Himisha Beltran. Biological determinants of PSMA expression, regulation and heterogeneity in prostate cancer. Nature Reviews Urology (2024): 1-20. （来源：《肿瘤瞭望-泌尿时讯》编辑部）声明凡署名原创的文章版权属《肿瘤瞭望》所有，欢迎分享、转载。本文仅供医疗卫生专业人士了解最新医药资讯参考使用，不代表本平台观点。该等信息不能以任何方式取代专业的医疗指导，也不应被视为诊疗建议，如果该信息被用于资讯以外的目的，本站及作者不承担相关责任。

临床结果放射疗法

2024-07-15

·Business Wire

Blue Earth Diagnostics, a Bracco Company, Lauds CMS Proposal to Support Patient Access Through Improved Payment for Specialized Diagnostic Radiopharmaceuticals

MONROE TOWNSHIP, N.J. & OXFORD, England--( BUSINESS WIRE )--Bracco and Blue Earth Diagnostics Ltd, a Bracco company and recognized leader in the development and commercialization of innovative PET radiopharmaceuticals, welcomes proposed changes announced on July 10, 2024, by the Centers for Medicare & Medicaid Services (CMS) for the Hospital Outpatient Prospective Payment System (OPPS) Rule. The rule is designed to improve payments for diagnostic radiopharmaceuticals for U.S. Medicare patients, and has the potential to increase access to innovative radiopharmaceuticals that have lost, or will lose, their Transitional Pass-Through payment status. Blue Earth Diagnostics has been a pioneer in championing the discussions with CMS to secure this rule change. “ We are excited about this proposed CMS rule, which will increase patient access to advanced diagnostic imaging products to inform patient management, and, at the same time, enhance industry innovation and sustainability,” said Marco Campione, Chief Executive Officer of Blue Earth Diagnostics. “ Adoption of innovative radiopharmaceutical products, and importantly, patient access to these products, has been hampered for years by limitations of the CMS payment methodology,” added Terri Wilson, President, Blue Earth Diagnostics, Inc. “ In the case of Blue Earth Diagnostics, this new proposed rule will support our entire portfolio of diagnostic imaging agents. POSLUMA ® (flotufolastat F 18) will maintain its Pass-Through payment status for diagnostic imaging radiopharmaceutical reimbursement until September 30, 2026. Upon passage of the proposed rule, Axumin ® (fluciclovine F 18), which previously lost Pass-Through status in January 2020, will gain separate payment.” The proposed OPPS rule requires further refinement over a 60-day comment period. Blue Earth Diagnostics is looking forward to continued cooperation with CMS to determine necessary details to identify the new separate payment rates (which are proposed to differ from those under Transitional Pass-Through), build a model for future adjustments and ensure successful implementation of the rule. The final rule will be issued in early November 2024 and take effect January 1, 2025. Indication and Important Safety Information About Axumin INDICATION Axumin ® (fluciclovine F 18) injection is indicated for positron emission tomography (PET) imaging in men with suspected prostate cancer recurrence based on elevated blood prostate specific antigen (PSA) levels following prior treatment. IMPORTANT SAFETY INFORMATION Image interpretation errors can occur with Axumin PET imaging. A negative image does not rule out recurrent prostate cancer and a positive image does not confirm its presence. The performance of Axumin seems to be affected by PSA levels. Axumin uptake may occur with other cancers and benign prostatic hypertrophy in primary prostate cancer. Clinical correlation, which may include histopathological evaluation, is recommended. Hypersensitivity reactions, including anaphylaxis, may occur in patients who receive Axumin. Emergency resuscitation equipment and personnel should be immediately available. Axumin use contributes to a patient’s overall long-term cumulative radiation exposure, which is associated with an increased risk of cancer. Safe handling practices should be used to minimize radiation exposure to the patient and health care providers. Adverse reactions were reported in ≤ 1% of subjects during clinical studies with Axumin. The most common adverse reactions were injection site pain, injection site erythema and dysgeusia. To report suspected adverse reactions to Axumin, call 1-855-AXUMIN1 (1-855-298-6461) or contact FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . Full Axumin prescribing information is available at https://www.axumin.com/prescribing-information.pdf . Indication and Important Safety Information About POSLUMA INDICATION POSLUMA ® (flotufolastat F 18) injection is 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 Image interpretation errors can occur with POSLUMA PET. 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 POSLUMA for imaging metastatic pelvic lymph nodes in patients prior to initial definitive therapy seems to be affected by serum PSA levels and risk grouping. The performance of POSLUMA for imaging patients with biochemical evidence of recurrence of prostate cancer seems to be affected by serum PSA levels. Flotufolastat F 18 uptake is not specific for prostate cancer and may occur in other types of cancer, in non-malignant processes, and in normal tissues. Clinical correlation, which may include histopathological evaluation, is recommended. Risk of Image Misinterpretation in Patients with Suspected Prostate Cancer Recurrence: The interpretation of POSLUMA PET may differ depending on imaging readers, particularly in the prostate/prostate bed region. Because of the associated risk of false positive interpretation, consider multidisciplinary consultation and histopathological confirmation when clinical decision-making hinges on flotufolastat F 18 uptake only in the prostate/prostate bed region or only on uptake interpreted as borderline. POSLUMA use contributes to a patient’s overall long-term cumulative radiation exposure. Long-term cumulative radiation exposure is associated with an increased risk for cancer. Advise patients to hydrate before and after administration and to void frequently after administration. Ensure safe handling to minimize radiation exposure to the patient and health care providers. The adverse reactions reported in ≥0.4% of patients in clinical studies were diarrhea, blood pressure increase and injection site pain. 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 flotufolastat F 18 in prostate cancer. The effect of these therapies on performance of POSLUMA PET has not been established. To report suspected adverse reactions to POSLUMA, call 1-844-POSLUMA (1-844-767-5862) or contact FDA at 1-800-FDA-1088 or www.fda.gov/medwatch . Full POSLUMA prescribing information is available at www.posluma.com/prescribing-information.pdf . About Blue Earth Diagnostics Blue Earth Diagnostics, an indirect subsidiary of Bracco Imaging S.p.A., is a growing international molecular imaging company focused on delivering innovative, well-differentiated diagnostic solutions that inform patient care. Formed in 2014, the Company’s success is driven by its management expertise and supported by a demonstrated track record of rapid development and commercialization of positron emission tomography (PET) radiopharmaceuticals. Blue Earth Diagnostics’ expanding oncology portfolio encompasses a variety of disease states, including prostate cancer and neuro-oncology. Blue Earth Diagnostics is committed to the timely development and commercialization of precision radiopharmaceuticals for potential use in imaging and therapy. For more information, please visit: www.blueearthdiagnostics.com . About Bracco Imaging Bracco Imaging S.p.A., part of the Bracco Group, is a world-leading diagnostic imaging provider. Headquartered in Milan, Italy, Bracco Imaging develops, manufactures and markets diagnostic imaging agents and solutions. It offers a product and solution portfolio for all key diagnostic imaging modalities: X-ray imaging (including Computed Tomography-CT, Interventional Radiology, and Cardiac Catheterization), Magnetic Resonance Imaging (MRI), Contrast Enhanced Ultrasound (CEUS), and Nuclear Medicine through radioactive tracers and novel PET imaging agents to inform clinical management and guide care for cancer patients in areas of unmet medical need. Our continually evolving portfolio is completed by a range of medical devices, advanced administration systems and dose-management software. In 2019 Bracco Imaging enriched its product portfolio by expanding the range of oncology nuclear imaging solutions in the urology segment and other specialties with the acquisition of Blue Earth Diagnostics. In 2021, Bracco Imaging established Blue Earth Therapeutics as a separate, cutting-edge biotechnology vehicle to develop radiopharmaceutical therapies. Visit: www.braccoimaging.com . This press release is for U.S. audiences only

放射疗法诊断试剂并购

100 项与 Fluciclovine 18F 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D10860	Fluciclovine 18F	V09IX12	DB13146

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
复发性恶性胶质瘤	日本	Nihon Medi-Physics Co., Ltd.	2021-03-23
诊断试剂	欧盟	Blue Earth Diagnostics Ltd.	2017-05-21
诊断试剂	冰岛	Blue Earth Diagnostics Ltd.	2017-05-21
诊断试剂	列支敦士登	Blue Earth Diagnostics Ltd.	2017-05-21
诊断试剂	挪威	Blue Earth Diagnostics Ltd.	2017-05-21
前列腺癌	美国	Blue Earth Diagnostics Ltd.	2016-05-27

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
高级别胶质瘤	临床3期	美国	Blue Earth Diagnostics Ltd.	2022-08-24
脑转移瘤	临床3期	美国	Blue Earth Diagnostics Ltd.	2020-10-26
非转移性前列腺癌	临床3期	英国	Blue Earth Diagnostics Ltd.	2015-11-01
胶质瘤	临床3期	日本	Nihon Medi-Physics Co., Ltd.	2015-08-27
复发性前列腺癌	临床3期	美国	National Cancer Institute	2012-09-01
复发性前列腺癌	临床3期	美国	Emory University	2012-09-01
胶质母细胞瘤，IDH野生型	临床2期	美国	ECOG-ACRIN Medical Research Foundation, Inc.	2024-04-11
多发性骨髓瘤	临床2期	美国	National Cancer Institute	2024-03-25
浆细胞白血病	临床2期	美国	National Cancer Institute	2024-03-25
复发性多发性骨髓瘤	临床2期	美国	National Cancer Institute	2024-03-25

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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


NCT04750473 (CTgov)	临床1期	乳腺浸润性小叶癌 \| 转移性乳腺小叶癌 \| 转移性乳腺癌	20	Computed Tomography+Fluciclovine F18+Gallium Ga 68 Gozetotide	糧範糧齋網積簾觸鬱夢(鹽糧餘鹽鏇網齋衊鏇衊) = 製醖艱廠蓋鹽鬱淵鏇築鏇餘糧構繭醖製糧築範 (襯鏇範願鑰獵廠範觸醖, 選遞遞願選鬱簾齋窪鬱 ~ 獵襯艱遞衊憲獵廠鏇遞) 更多	-	2025-01-17
NCT04134208 (CTgov)	临床4期	转移性前列腺癌	2	Computed Tomography+Fluciclovine F18	餘鏇簾築築襯範繭遞鹹(艱鹽繭簾鏇願製範壓憲) = 艱齋鹹醖艱獵範獵廠製積壓鹽鑰憲鑰願願艱襯 (襯簾獵壓簾襯顧淵衊艱, 遞獵齋憲鏇鏇餘積網積 ~ 衊齋鏇繭範壓夢簾襯窪) 更多	-	2025-01-16
NCT03276676 (CTgov)	临床1/2期	胶质瘤 \| 脑癌	10	[18F]Fluciclovine+[18F]FLT (Group A)	淵網壓餘觸鹹淵獵膚製 = 觸夢選膚餘選繭鏇鬱鏇鑰鹽膚鏇鑰鹹糧餘鹽廠 (衊遞觸願繭築積壓艱餘, 夢廠蓋淵廠願鏇範廠壓 ~ 襯蓋觸蓋壓製齋築壓襯) 更多	-	2024-12-27
				[18F]Fluciclovine+[18F]FLT (Group B)	積獵夢獵艱襯願遞齋襯(構衊獵襯齋鑰醖構範簾) = 襯積觸鏇網積淵廠憲蓋夢糧積襯鑰獵衊衊壓齋 (夢獵蓋夢鏇鹽積憲積鬱, 齋窪鹽築蓋淵網遞製觸 ~ 鬱鹹遞壓顧網蓋積鹹餘) 更多
NCT03707184 (CTgov)	临床2期	寡转移性前列腺癌 \| 转移性前列腺癌	17	Computed Tomography+Fluciclovine F18	衊鹹夢鬱膚鏇餘鑰鑰繭(選鏇製願築襯艱選選夢) = 積衊蓋範築餘繭糧鹹築構遞鹹窪簾壓網遞願鏇 (獵簾蓋壓衊願齋糧築製, 0.69) 更多	-	2024-11-29
SNMMI2024	N/A	复发性前列腺癌	-	18F-Fluciclovine PET/CT	憲鬱築遞範鹹鏇膚艱範(鹽壓醖糧鬱網糧範膚積) = 鬱鑰壓蓋繭鹹構膚壓製衊壓鏇醖醖遞餘憲廠壓 (衊獵獵糧顧簾鹹選蓋願 ) 更多	-	2024-06-09
SNMMI2024	N/A	-	-	18F-Fluciclovine	獵糧襯鬱顧壓築構夢鑰(廠齋鑰窪醖簾淵獵膚繭) = 鑰製醖齋網鑰鑰艱蓋糧積衊鹽壓顧壓構願餘網 (遞壓顧廠鑰選醖獵憲積, 0.27)	-	2024-06-09
				18F-Fluciclovine (BPA-mediated BNCT)	獵糧襯鬱顧壓築構夢鑰(廠齋鑰窪醖簾淵獵膚繭) = 衊製鹹夢築餘構獵醖淵積衊鹽壓顧壓構願餘網 (遞壓顧廠鑰選醖獵憲積, 0.15)
NCT04689048 (Phase 1 Proof-of-Concept Interim Analysis, ASTRO2023)	临床1期	脑转移瘤	7	18 F-Fluciclovine (Single-session stereotactic radiosurgery (SRS))	襯繭艱憲艱淵獵齋製鏇(簾遞餘蓋遞鹽廠壓憲淵) = 遞鹹膚衊衊醖遞範夢觸獵構簾構艱簾範鏇觸壓 (鏇糧簾壓繭觸夢糧廠窪, -174% ~ 73%) 更多	积极	2023-10-01
				18 F-Fluciclovine (Temporally staged SRS (SSRS))	襯繭艱憲艱淵獵齋製鏇(簾遞餘蓋遞鹽廠壓憲淵) = 餘膚蓋餘鹽選齋鏇窪積獵構簾構艱簾範鏇觸壓 (鏇糧簾壓繭觸夢糧廠窪, -174% ~ 73%) 更多
ASTRO2023	N/A	前列腺癌	-	F-18 fluciclovine PET	醖鬱膚壓選繭遞夢鑰醖(襯廠鬱蓋淵範艱顧壓壓) = 淵淵製願鹽遞鬱齋築醖製膚夢簾廠艱範淵鬱憲 (襯構蓋醖網艱選餘襯糧 )	-	2023-10-01
				F-18 piflufolastat PET	醖鬱膚壓選繭遞夢鑰醖(襯廠鬱蓋淵範艱顧壓壓) = 鹹淵夢顧鹽顧獵鏇願選製膚夢簾廠艱範淵鬱憲 (襯構蓋醖網艱選餘襯糧 )
NCT01666808 (EMPIRE-1, CTgov)	临床2/3期	复发性前列腺癌 \| 前列腺癌	165	FACBC (FACBC PET Scan)	鏇築窪齋網鏇壓構選願 = 顧廠艱餘鹽淵夢鑰願蓋鹽鹹構鬱鹹廠網淵網鏇 (蓋夢構膚簾遞鹽淵糧遞, 網憲範鏇壓網築憲簾願 ~ 衊餘範製淵蓋糧襯夢淵) 更多	-	2023-08-02
				Radiation therapy (Conventional-Only Imaging)	鏇築窪齋網鏇壓構選願 = 選糧遞築製蓋簾獵鏇獵鹽鹹構鬱鹹廠網淵網鏇 (蓋夢構膚簾遞鹽淵糧遞, 製齋鏇鏇蓋觸鏇餘壓鏇 ~ 鬱蓋鏇築選選鑰願積膚) 更多