Delving into the Latest Updates on [18F]DCFBC with Synapse

Overview

Basic Info

Drug Type

Small molecule drug, Diagnostic radiopharmaceuticals

Synonyms

18F DCFBC

Target

PSMA

Action

inhibitors

Mechanism

PSMA inhibitors(Prostate-specific membrane antigen inhibitors)

Therapeutic Areas

NeoplasmsUrogenital Diseases

Active Indication-

Inactive Indication

Advanced Prostate CarcinomaMetastatic Prostate Carcinoma

Originator Organization

Washington University in St. Louis

Active Organization-

Inactive Organization

The Sidney Kimmel Comprehensive Cancer Center

License Organization-

Drug Highest PhasePendingPhase 1/2

First Approval Date-

Regulation-

Login to view timeline

Structure/Sequence

Molecular FormulaC16H19FN2O7S

InChIKeyIDTMSHGCAZPVLC-STUNTBJNSA-N

CAS Registry1169942-33-9

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.

Start Date12 Jul 2014

Sponsor / Collaborator

National Cancer Institute

NCT01815515

/ CompletedPhase 1/2IIT

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.

Start Date01 Mar 2013

Sponsor / Collaborator

The Sidney Kimmel Comprehensive Cancer Center

NCT01496157

/ CompletedPhase 1/2IIT

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).

Start Date11 Sep 2012

Sponsor / Collaborator

The Sidney Kimmel Comprehensive Cancer Center

100 Clinical Results associated with [18F]DCFBC

Login to view more data

100 Translational Medicine associated with [18F]DCFBC

Login to view more data

100 Patents (Medical) associated with [18F]DCFBC

Login to view more data

5

Literatures (Medical) associated with [18F]DCFBC

01 Oct 2017·Clinical nuclear medicineQ3 · MEDICINE

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

Q3 · MEDICINE

Article

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

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.

01 Dec 2012·Journal of nuclear medicine : official publication, Society of Nuclear MedicineQ1 · MEDICINE

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

Q1 · MEDICINE

Article

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

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.

26 Nov 2012·Journal of medicinal chemistryQ1 · MEDICINE

Radiofluorinated Derivatives of 2-(Phosphonomethyl)pentanedioic Acid as Inhibitors of Prostate Specific Membrane Antigen (PSMA) for the Imaging of Prostate Cancer

Q1 · MEDICINE

Article

Author: Graham, Keith ; Dinkelborg, Ludger ; Schäfer, Martina ; Gromov, Alexey V. ; Kettschau, Georg ; Hassfeld, Jorma ; Lesche, Ralf ; Böhnke, Niels

For prostate cancer, prostate specific membrane antigen (PSMA) has been identified as a diagnostic and therapeutic target. Fluorinated derivatives of 2-(phosphonomethyl)pentanedioic acid were designed and synthesized to explore whether this fluorine-substituent is tolerated in the pentanedioic acid moiety that is common to almost all PSMA targeting small molecule inhibitors. The binding affinities of the racemic and individual stereoisomers of 2-fluoro-4-(phosphonomethyl)pentanedioic acid were determined and showed that the introduction of fluorine was well tolerated. The radiosynthesis of the analogous 2-[(18)F]fluoro-4-(phosphonomethyl)pentanedioic acid was developed and evaluated in vivo with the PSMA positive LNCaP human prostate cancer cell. The biological results demonstrated specific binding of the tracer to PSMA positive tumors in mice. These results warrant the further evaluation of this class of compounds as radiolabeled tracers for the detection and staging of prostate cancer.

100 Deals associated with [18F]DCFBC

Login to view more data

External Link

KEGG	Wiki	ATC	Drug Bank
-	-	-	DB14772

R&D Status

10 top R&D records.

Login

to view more data

Indication	Highest Phase	Country/Location	Organization	Date
Metastatic Prostate Carcinoma	Phase 2	United States	The Sidney Kimmel Comprehensive Cancer Center	01 Mar 2013
Advanced Prostate Carcinoma	Phase 1	United States	The Sidney Kimmel Comprehensive Cancer Center	01 Sep 2010

Login to view more data

Clinical Result

Indication

Phase

Evaluation

View All Results

Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02190279 (CTgov)	Early Phase 1	Prostatic Cancer	116	18F DCFBC (Suspected Localized Prostate Cancer)	powthjrayo = vjxayummpr abbkosbvvl (azdskbxbwz, jkbcnnwwae - wmndwkngnz) View more	-	23 Apr 2019
NCT02190279 (CTgov)	Early Phase 1	Prostatic Cancer	116	18F DCFBC (Biochemical Recurrence)	powthjrayo = bvblhaxolw abbkosbvvl (azdskbxbwz, eqhzehqscj - dsoyvoftmc) View more	-	23 Apr 2019
NCT01496157 (CTgov)	Phase 1/2	Prostatic Cancer	15	18F-DCFBC	njfpiiwcrl = thpyenrxxo jbrvsydwyh (nlphknioik, kxtkegebds - zjvxzpkfal) View more	-	28 Aug 2018
NCT01815515 (CTgov)	Phase 1/2	Metastatic Prostate Carcinoma	22	18F-DCFBC	hpvpugrgqn = iqoqnsjvzo pkjpcrbagv (nkifcxjctr, vncolddfrx - zurgcrgafc) View more	-	20 Aug 2018
Pubmed \| Clin Nucl Med	Early Phase 1	Localized Prostate Carcinoma	13	18F-DCFBC (F-DCFBC PET/CT)	fyepqrnsxt(oocxfmfetv) = duvkkhfgjs mwyfmhwbnv (ejubhwzfur ) View more	-	01 Oct 2017
Pubmed \| Clin Nucl Med	Early Phase 1	Localized Prostate Carcinoma	13	18F-DCFBC (mpMRI)	fyepqrnsxt(oocxfmfetv) = grvfxssimo mwyfmhwbnv (ejubhwzfur ) View more	-	01 Oct 2017