[18F]DCFBC([18F]DCFBC) - 药物靶点：PSMA_专利_临床

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 DCFBC

靶点

PSMA

作用方式

抑制剂

作用机制

PSMA抑制剂(前列腺癌特异性膜抗原抑制剂)

治疗领域

肿瘤泌尿生殖系统疾病

在研适应症-

非在研适应症

晚期前列腺癌转移性前列腺癌

原研机构

Washington University in St. Louis

在研机构-

非在研机构

The Sidney Kimmel Comprehensive Cancer Center

权益机构-

最高研发阶段无进展临床1/2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C16H19FN2O7S

InChIKeyIDTMSHGCAZPVLC-STUNTBJNSA-N

CAS号1169942-33-9

关联

4

项与 [18F]DCFBC 相关的临床试验

NCT02190279

/ Completed早期临床1期IIT

A Pilot Study of 18F-DCFBC PET/CT in Prostate Cancer

Background:
- Prostate cancer is the second leading cause of cancer deaths in American men. A chemical called a radiotracer helps doctors get images of this type of cancer. Researchers want to test a radiotracer called N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-4-(18)F-fluorobenzyl-L-cysteine ((18)F-DCFBC) (18F-DCFBC).
Objective:
- To see if the radiotracer 18F-DCFBC can identify sites of prostate cancer in the body.
Eligibility:
- Men ages 18 and over with prostate cancer. The cancer must be newly diagnosed, have relapsed, or has spread outside the prostate.
Design:
* Participants will be screened with physical exam and medical history. They will give a blood sample.
* Participants will be divided into three groups.
Group 1: people with cancer only in the prostate scheduled for surgical prostate removal or biopsy at National Institutes of Health (NIH).
Group 2: people who had their prostate removed or had radiation therapy and now have a rising prostate-specific antigen (PSA) without other signs of disease.
Group 3: people whose cancer has spread to other areas of the body.
* Participants will have 18F-DCFBC injected into a vein then imaged in a positron emission tomography (PET)/computed tomography (CT) camera. During the scans, they will lie on their back on the scanner table.
* Group 1 will have a magnetic resonance imaging (MRI) scan. A tube will be placed in the rectum. Coils may be wrapped around the outside of the pelvis. Participants will have a contrast agent injected through an intravenous line.
* Group 3 will have another PET/CT scan with a different radiotracer, 18F NaF, within 21 days of the 18F-DCFBC scan to look for prostate cancer in the bone.
* Group 3 will repeat the two PET/CT scans 4-6 months after the initial scans.
* A few days after each scan, participants will be contacted for follow-up.

开始日期2014-07-12

申办/合作机构

National Cancer Institute

NCT01815515

/ Completed临床1/2期IIT

Evaluation of 18F-DCFBC PSMA-based PET Imaging for Detection of Metastatic Prostate Cancer.

This research is being done to see if an investigational radioactive drug called 18F-DCFBC can help us find cancer that has spread (metastatic disease) from its original site in people who have cancer in their prostate to other parts of their body.

开始日期2013-03-01

申办/合作机构

The Sidney Kimmel Comprehensive Cancer Center

NCT01496157

/ Completed临床1/2期IIT

Evaluation of PSMA-based PET as an Imaging Biomarker of Primary Prostate Cancer

The objective of this study is to evaluate a radiolabeled urea-based small molecule inhibitor of prostate-specific membrane antigen (PSMA), [18F]DCFBC (DCFBC), as a PET imaging biomarker of prostate cancer detection and aggressiveness at initial diagnosis. PSMA is a well characterized histological marker of prostate cancer tumor aggressiveness but a quantitative non-invasive method for PSMA detection and monitoring is not currently available. Development of such an imaging biomarker would be useful to differentiate indolent from aggressive prostate cancer phenotypes and allow for selection of appropriate risk adaptive therapies. The investigators preliminary first-in-human studies demonstrate high specific DCFBC uptake in metastatic prostate cancer and feasibility for prostate cancer imaging. The investigators propose to study patients initially diagnosed with biopsy-positive prostate cancer to determine if DCFBC uptake and location by PET imaging will be positively correlated with prostate cancer by prostatectomy tissue step-section analysis. DCFBC uptake at sites of suspected metastatic disease will be compared to conventional imaging modalities (CT, bone scan) and biopsy results when available. In addition, DCFBC-PET uptake quantification will be compared with expression levels of PSMA and other prostate cancer relevant markers (PSA, Ki-67, TMPRSS2-ERG) by prostate tissue immunohistochemistry analysis and compared with clinical prognostic markers (PSA, Gleason score, clinical stage, Partin tables derived prediction of pathologic stage).

开始日期2012-09-11

申办/合作机构

The Sidney Kimmel Comprehensive Cancer Center

100 项与 [18F]DCFBC 相关的临床结果

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100 项与 [18F]DCFBC 相关的转化医学

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100 项与 [18F]DCFBC 相关的专利（医药）

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6

项与 [18F]DCFBC 相关的文献（医药）

2019-09-06·ACS Catalysis

Electrostatic Effects Accelerate Decatungstate-Catalyzed C–H Fluorination Using [¹⁸F]- and [¹⁹F]NFSI in Small Molecules and Peptide Mimics

作者: Martin, Rainer E. ; Warren, Jeffrey J. ; Yuan, Zheliang ; Yang, Hua ; Britton, Robert ; Weber, David S. ; Schaffer, Paul ; Malik, Noeen ; Čolović, Milena ; Wilson, Darryl ; Bénard, François

The site-selective fluorination of unactivated C(sp³)-H bonds provides unique opportunities to rapidly alter drug properties or generate radiotracers for positron emission tomog. (PET) imaging.Toward this goal, photoactivated decatungstate (DT) is capable of generating carbon radicals through hydrogen atom transfer that subsequently undergo fluorination by reaction with N-fluorobenzenesulfonimide (NFSI) or [¹⁸F]NFSI.This process enables C(sp³)-H fluorination of a wide range of aliphatic compounds, though reaction rates can be highly variable and limit applications in radiotracer synthesis.Here, we demonstrate that cationic ammonium functions in aliphatic mols. promote formation of a precursor complex with DT that significantly increases the rate of C-H abstraction.The general utility of this rate-accelerating electrostatic effect is demonstrated on more than 30 ammonium-containing mols., including amino acids, heterocycles, and pseudopeptides.Moreover, this effect is highlighted in the rapid production of [¹⁸F]Glu-U-FHLeu, a ¹⁸F-labeled prostate specific membrane antigen (PSMA)-binding ligand.

2017-10-01·Clinical nuclear medicine3区 · 医学

18F-DCFBC Prostate-Specific Membrane Antigen–Targeted PET/CT Imaging in Localized Prostate Cancer

3区 · 医学

Article

作者: McKinney, Yolanda ; Bhattacharyya, Sibaprasad ; Choyke, Peter L ; Eclarinal, Philip ; Berman, Rose ; Bednarova, Sandra ; Mease, Ronnie C ; Ton, Anita T ; Pinto, Peter A ; Hill, Craig ; Pomper, Martin G ; Jacobs, Paula M ; Wood, Bradford J ; Adler, Stephen ; Mena, Esther ; Merino, Maria J ; Turkbey, Baris ; Lindenberg, Liza ; Afari, George

PURPOSE:

To assess the ability of (N-[N-[(S)-1,3-dicarboxypropyl]carbamoyl]-4-F-fluorobenzyl-L-cysteine) (F-DCFBC), a prostate-specific membrane antigen-targeted PET agent, to detect localized prostate cancer lesions in correlation with multiparametric MRI (mpMRI) and histopathology.

METHODS:

This Health Insurance Portability and Accountability Act of 1996-compliant, prospective, institutional review board-approved study included 13 evaluable patients with localized prostate cancer (median age, 62.8 years [range, 51-74 years]; median prostate-specific antigen, 37.5 ng/dL [range, 3.26-216 ng/dL]). Patients underwent mpMRI and F-DCFBC PET/CT within a 3 months' window. Lesions seen on mpMRI were biopsied under transrectal ultrasound/MRI fusion-guided biopsy, or a radical prostatectomy was performed. F-DCFBC PET/CT and mpMRI were evaluated blinded and separately for tumor detection on a lesion basis. For PET image analysis, MRI and F-DCFBC PET images were fused by using software registration; imaging findings were correlated with histology, and uptake of F-DCFBC in tumors was compared with uptake in benign prostatic hyperplasia nodules and normal peripheral zone tissue using the 80% threshold SUVmax.

RESULTS:

A total of 25 tumor foci (mean size, 1.8 cm; median size, 1.5 cm; range, 0.6-4.7 cm) were histopathologically identified in 13 patients. Sensitivity rates of F-DCFBC PET/CT and mpMRI were 36% and 96%, respectively, for all tumors. For index lesions, the largest tumor with highest Gleason score, sensitivity rates of F-DCFBC PET/CT and mpMRI were 61.5% and 92%, respectively. The average SUVmax for primary prostate cancer was higher (5.8 ± 4.4) than that of benign prostatic hyperplasia nodules (2.1 ± 0.3) or that of normal prostate tissue (2.1 ± 0.4) at 1 hour postinjection (P = 0.0033).

CONCLUSIONS:

The majority of index prostate cancers are detected with F-DCFBC PET/CT, and this may be a prognostic indicator based on uptake and staging. However, for detecting prostate cancer with high sensitivity, it is important to combine prostate-specific membrane antigen PET/CT with mpMRI.

2012-12-01·Journal of nuclear medicine : official publication, Society of Nuclear Medicine1区 · 医学

Biodistribution, Tumor Detection, and Radiation Dosimetry of ¹⁸F-DCFBC, a Low-Molecular-Weight Inhibitor of Prostate-Specific Membrane Antigen, in Patients with Metastatic Prostate Cancer

1区 · 医学

Article

作者: Senthamizhchelvan, Srinivasan ; Rojas, Camilo ; Cho, Steve Y. ; Jeffrey-Kwanisai, Akimosa ; Dannals, Robert F. ; Holt, Daniel P. ; Endres, Christopher J. ; Rodiguez, Ronald ; Eisenberger, Mario A. ; Gage, Kenneth L. ; Pomper, Martin G. ; Mease, Ronnie C. ; Sgouros, George ; Slusher, Barbara S. ; Lodge, Martin ; Carducci, Michael A. ; Kozikowski, Alan P.

METHODS:

Five patients with radiologic evidence of metastatic PCa were studied after the intravenous administration of 370 MBq (10 mCi) of (18)F-DCFBC. Serial PET was performed until 2 h after administration. Time-activity curves were generated for selected normal tissues and metastatic foci. Radiation dose estimates were calculated using OLINDA/EXM 1.1.

RESULTS:

Most vascular organs demonstrated a slow decrease in radioactivity concentration over time consistent with clearance from the blood pool, with primarily urinary radiotracer excretion. Thirty-two PET-positive suspected metastatic sites were identified, with 21 concordant on both PET and conventional imaging for abnormal findings compatible with metastatic disease. Of the 11 PET-positive sites not identified on conventional imaging, most were within the bone and could be considered suggestive for the detection of early bone metastases, although further validation is needed. The highest mean absorbed dose per unit administered radioactivity (μGy/MBq) was in the bladder wall (32.4), and the resultant effective dose was 19.9 ± 1.34 μSv/MBq (mean ± SD).

CONCLUSION:

Although further studies are needed for validation, our findings demonstrate the potential of (18)F-DCFBC as a new positron-emitting imaging agent for the detection of metastatic PCa. This study also provides dose estimates for (18)F-DCFBC that are comparable to those of other PET radiopharmaceuticals such as (18)F-FDG.

100 项与 [18F]DCFBC 相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB14772

研发状态

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
转移性前列腺癌	临床2期	美国	The Sidney Kimmel Comprehensive Cancer Center	2013-03-01
晚期前列腺癌	临床1期	美国	The Sidney Kimmel Comprehensive Cancer Center	2010-09-01

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临床结果

适应症

分期

评价

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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


NCT02190279 (CTgov)	早期临床1期	前列腺癌	116	18F DCFBC (Suspected Localized Prostate Cancer)	蓋願艱製壓糧選糧憲選 = 窪鏇鹹鑰鏇齋壓觸顧艱窪廠廠觸獵觸餘齋膚鹽 (衊構淵衊壓夢鏇鏇齋製, 衊壓壓鏇壓鏇範選齋築 ~ 選壓夢鹽憲願鏇鬱願構) 更多	-	2019-04-23
NCT02190279 (CTgov)	早期临床1期	前列腺癌	116	18F DCFBC (Biochemical Recurrence)	蓋願艱製壓糧選糧憲選 = 艱構廠餘構蓋鹽築襯壓窪廠廠觸獵觸餘齋膚鹽 (衊構淵衊壓夢鏇鏇齋製, 蓋膚壓鹽齋構繭糧範膚 ~ 艱艱範製廠廠醖簾衊顧) 更多	-	2019-04-23
NCT01496157 (CTgov)	临床1/2期	前列腺癌	15	18F-DCFBC	衊衊鹽襯鬱憲窪蓋廠壓 = 積鏇廠觸憲壓艱獵糧壓觸範衊構廠鏇鏇選艱願 (壓繭襯繭構夢範廠艱艱, 築網構餘窪壓鏇繭築獵 ~ 鬱願憲糧淵餘糧憲遞淵) 更多	-	2018-08-28
NCT01815515 (CTgov)	临床1/2期	转移性前列腺癌	22	18F-DCFBC	廠餘願製築積鹽鹹簾廠 = 糧鑰範廠醖醖鑰獵網艱願憲製鹽淵顧製選糧鑰 (鏇鹹鑰艱壓願鹽壓蓋鏇, 遞簾鹹鬱夢繭繭夢構鏇 ~ 鑰膚糧鏇築遞鹹網範醖) 更多	-	2018-08-20
NCT02190279 (Pubmed \| Clin Nucl Med)	早期临床1期	局限性前列腺癌	13	18F-DCFBC (F-DCFBC PET/CT)	網獵襯壓淵淵蓋選構顧(製簾淵鏇艱艱蓋繭鏇鬱) = 顧鹽淵網糧遞蓋鬱廠衊簾窪壓廠淵觸範鹹製糧 (鹽網鏇網艱壓廠積衊餘 ) 更多	-	2017-10-01
NCT02190279 (Pubmed \| Clin Nucl Med)	早期临床1期	局限性前列腺癌	13	18F-DCFBC (mpMRI)	網獵襯壓淵淵蓋選構顧(製簾淵鏇艱艱蓋繭鏇鬱) = 製簾淵窪鬱積鑰襯鏇鏇簾窪壓廠淵觸範鹹製糧 (鹽網鏇網艱壓廠積衊餘 ) 更多	-	2017-10-01
SNMMI2017	N/A	复发性前列腺癌 PSMA	68	18F-DCFBC PET/CT	選顧夢壓顧鏇鑰壓廠齋(獵衊網醖襯獵獵簾醖鏇) = 醖夢餘窪範憲糧壓糧廠窪夢蓋糧糧憲醖糧願製 (鹹鏇鹹窪範顧製鬱襯醖 )	积极	2017-05-24
SNMMI2016	N/A	复发性前列腺癌 PSA	34	18F-DCFBC (Prostatectomy)	選廠觸製積窪壓願獵鹽(築鹽鏇鬱製積鑰築製鏇) = 鏇獵顧範膚夢鹽淵獵襯遞願齋餘壓構齋壓積餘 (網鹽鹹鬱鑰積齋簾壓鹹, 7.5)	积极	2016-05-24
SNMMI2016	N/A	复发性前列腺癌 PSA	34	Salvage radiation therapy	選廠觸製積窪壓願獵鹽(築鹽鏇鬱製積鑰築製鏇) = 憲繭醖鑰夢襯齋壓鹹膚遞願齋餘壓構齋壓積餘 (網鹽鹹鬱鑰積齋簾壓鹹, 7.5)	积极	2016-05-24