Skip to main content
Key Specialties
Cardiology Diabetology Endocrinology Gastroenterology Geriatrics and Gerontology Gynecology and Obstetrics Hematology Infectious Disease Internal Medicine Nephrology Neurology Oncology Pediatrics Respiratory Medicine Rheumatology Surgery
Congress Coverage
2024 ACC Congress 2023 ESMO Congress 2023 EASD Congress 2023 ERS Congress 2023 ESC Congress
Clinical Collections
Advances in Alzheimer’s

At a glance: The STEP trials

A round-up of the STEP phase 3 clinical trials evaluating semaglutide for weight loss in people with overweight or obesity.
ADVANCED SEARCH
Log in
Top
Molecular Imaging and Biology
Published in: Molecular Imaging and Biology 4/2015

01-08-2015 | Research Article

Initial Evaluation of [18F]DCFPyL for Prostate-Specific Membrane Antigen (PSMA)-Targeted PET Imaging of Prostate Cancer

Authors: Zsolt Szabo, Esther Mena, Steven P. Rowe, Donika Plyku, Rosa Nidal, Mario A. Eisenberger, Emmanuel S. Antonarakis, Hong Fan, Robert F. Dannals, Ying Chen, Ronnie C. Mease, Melin Vranesic, Akrita Bhatnagar, George Sgouros, Steve Y. Cho, Martin G. Pomper

Published in: Molecular Imaging and Biology | Issue 4/2015

Login to get access

Abstract

Purpose

Prostate-specific membrane antigen (PSMA) is a recognized target for imaging prostate cancer. Here we present initial safety, biodistribution, and radiation dosimetry results with [18F]DCFPyL, a second-generation fluorine-18-labeled small-molecule PSMA inhibitor, in patients with prostate cancer.

Procedures

Biodistribution was evaluated using sequential positron-emission tomography (PET) scans in nine patients with prostate cancer. Time-activity curves from the most avid tumor foci were determined. The radiation dose to selected organs was estimated using OLINDA/EXM.

Results

No major radiotracer-specific adverse events were observed. Physiologic accumulation was observed in known sites of PSMA expression. Accumulation in putative sites of prostate cancer was observed (SUVmax up to >100, and tumor-to-blood ratios up to >50). The effective radiation dose from [18F]DCFPyL was 0.0139 mGy/MBq or 5 mGy (0.5 rem) from an injected dose of 370 MBq (10 mCi).

Conclusions

[18F]DCFPyL is safe with biodistribution as expected, and its accumulation is high in presumed primary and metastatic foci. The radiation dose from [18F]DCFPyL is similar to that from other PET radiotracers.
Literature
1.
2.
Shinohara K, Wheeler TM, Scardino PT (1989) The appearance of prostate cancer on transrectal ultrasonography: correlation of imaging and pathological examinations. J Urol 142:76–82PubMed
3.
Hricak H, Dooms GC, Jeffrey RB et al (1987) Prostatic carcinoma: staging by clinical assessment, CT, and MR imaging. Radiology 162:331–336PubMedCrossRef
4.
Scheidler J, Hricak H, Vigneron DB et al (1999) Prostate cancer: localization with three-dimensional proton MR spectroscopic imaging—clinicopathologic study. Radiology 213:473–480PubMedCrossRef
5.
Blomqvist L, Carlsson S, Gjertsson P et al (2014) Limited evidence for the use of imaging to detect prostate cancer: a systematic review. Eur J Radiol 83:1601–1606PubMedCrossRef
6.
Turlakow A, Yeung HW, Pui J et al (2001) Fludeoxyglucose positron emission tomography in the diagnosis of giant cell arteritis. Arch Intern Med 161:1003–1007PubMedCrossRef
7.
Hofer C, Laubenbacher C, Block T (1999) Fluorine-18-fluorodeoxyglucose positron emission tomography is useless for the detection of local recurrence after radical prostatectomy. Eur Urol 36:31–35PubMedCrossRef
8.
Nunez R, Macapinlac HA, Yeung HW et al (2002) Combined 18F-FDG and 11C-methionine PET scans in patients with newly progressive metastatic prostate cancer. J Nucl Med 43:46–55PubMed
9.
Shreve PD, Grossman HB, Gross MD, Wahl RL (1996) Metastatic prostate cancer: initial findings of PET with 2-deoxy-2-[F-18]fluoro-D-glucose. Radiology 199:751–756PubMedCrossRef
10.
Hricak H, Choyke PL, Eberhardt SC et al (2007) Imaging prostate cancer: a multidisciplinary perspective. Radiology 243:28–53PubMedCrossRef
11.
Lawrentschuk N, Davis ID, Bolton DM, Scott AM (2006) Positron emission tomography and molecular imaging of the prostate: an update. BJU Int 97:923–931PubMedCrossRef
12.
de Jong IJ, Pruim J, Elsinga PH et al (2003) 11C-choline positron emission tomography for the evaluation after treatment of localized prostate cancer. Eur Urol 44:32–38, Discussion 8–9 PubMedCrossRef
13.
Picchio M, Messa C, Landoni C et al (2003) Value of [11C]choline-positron emission tomography for re-staging prostate cancer: a comparison with [18F]fluorodeoxyglucose-positron emission tomography. J Urol 169:1337–1340PubMedCrossRef
14.
Scattoni V, Picchio M, Suardi N et al (2007) Detection of lymph-node metastases with integrated [11C]choline PET/CT in patients with PSA failure after radical retropubic prostatectomy: results confirmed by open pelvic-retroperitoneal lymphadenectomy. Eur Urol 52:423–429PubMedCrossRef
15.
Greco C, Cascini GL, Tamburrini O (2008) Is there a role for positron emission tomography imaging in the early evaluation of prostate cancer relapse? Prostate Cancer Prostatic Dis 11:121–128PubMedCrossRef
16.
17.
Wright GL Jr, Grob BM, Haley C et al (1996) Upregulation of prostate-specific membrane antigen after androgen-deprivation therapy. Urology 48:326–334PubMedCrossRef
18.
Silver DA, Pellicer I, Fair WR et al (1997) Prostate-specific membrane antigen expression in normal and malignant human tissues. Clin Cancer Res 3:81–85PubMed
19.
Mease RC, Dusich CL, Foss CA et al (2008) N-[N-[(S)-1,3-Dicarboxypropyl]carbamoyl]-4-[18F]fluorobenzyl-L-cysteine, [18F]DCFBC: a new imaging probe for prostate cancer. Clin Cancer Res 14:3036–3043PubMedCentralPubMedCrossRef
20.
Cho SY, Gage KL, Mease RC et al (2012) 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. J Nucl Med 53:1883–1891PubMedCentralPubMedCrossRef
21.
Banerjee SR, Pullambhatla M, Byun Y et al (2010) 68Ga-labeled inhibitors of prostate-specific membrane antigen (PSMA) for imaging prostate cancer. J Med Chem 53:5333–5341PubMedCentralPubMedCrossRef
22.
Eder M, Schafer M, Bauder-Wust U et al (2012) 68Ga-complex lipophilicity and the targeting property of a urea-based PSMA inhibitor for PET imaging. Bioconjug Chem 23:688–697PubMedCrossRef
23.
Baur B, Solbach C, Andreolli E et al (2014) Synthesis, radiolabelling and in vitro characterization of the gallium-68-, yttrium-90- and lutetium-177-labelled PSMA ligand, CHX-A″-DTPA-DUPA-Pep. Pharmaceuticals 7:517–529PubMedCentralPubMedCrossRef
24.
Chen Y, Pullambhatla M, Byun Y et al (2011) 2-(3-{1-Carboxy-5-[(6-[18F]fluoro-pyridine-3-carbonyl)-amino]-pentyl}-urei do)-pentanedioic acid, [18F]DCFPyL, a PSMA-based PET imaging agent for prostate cancer. Clin Cancer Res 17:7645PubMedCentralPubMedCrossRef
25.
Olberg DE, Arukwe JM, Grace D et al (2010) One step radiosynthesis of 6-[(18)F]fluoronicotinic acid 2,3,5,6-tetrafluorophenyl ester ([(18)F]F-Py-TFP): a new prosthetic group for efficient labeling of biomolecules with fluorine-18. J Med Chem 53:1732–1740PubMedCrossRef
26.
Maresca KP, Hillier SM, Femia FJ et al (2009) A series of halogenated heterodimeric inhibitors of prostate specific membrane antigen (PSMA) as radiolabeled probes for targeting prostate cancer. J Med Chem 52:347–357PubMedCrossRef
27.
Bachner M, Loriot Y, Gross-Goupil M et al (2012) 2-(1)(8)fluoro-deoxy-D-glucose positron emission tomography (FDG-PET) for postchemotherapy seminoma residual lesions: a retrospective validation of the SEMPET trial. Ann Oncol 23:59–64PubMedCrossRef
28.
Bolch WE, Eckerman KF, Sgouros G, Thomas SR (2009) MIRD pamphlet No. 21: a generalized schema for radiopharmaceutical dosimetry—standardization of nomenclature. J Nucl Med 50:477–484PubMedCrossRef
29.
Stabin MG, Sparks RB, Crowe E (2005) OLINDA/EXM: the second-generation personal computer software for internal dose assessment in nuclear medicine. J Nucl Med 46:1023–1027PubMed
30.
Valentin J (2002) Basic anatomical and physiological data for use in radiological protection: reference values. A report of age- and gender-related differences in the anatomical and physiological characteristics of reference individuals. ICRP Publication 89. Ann ICRP 32:5–265CrossRef
31.
Thomas SR, Stabin MG, Chen CT, Samaratunga RC (1992) MIRD Pamphlet No. 14: a dynamic urinary bladder model for radiation dose calculations. J Nucl Med 33:783–802PubMed
32.
Mhawech-Fauceglia P, Zhang S, Terracciano L et al (2007) Prostate-specific membrane antigen (PSMA) protein expression in normal and neoplastic tissues and its sensitivity and specificity in prostate adenocarcinoma: an immunohistochemical study using multiple tumour tissue microarray technique. Histopathology 50:472–483PubMedCrossRef
33.
Afshar-Oromieh A, Zechmann CM, Malcher A et al (2014) Comparison of PET imaging with a (68)Ga-labelled PSMA ligand and (18)F-choline-based PET/CT for the diagnosis of recurrent prostate cancer. Eur J Nucl Med Mol Imaging 41:11–20PubMedCentralPubMedCrossRef
34.
Demirci E, Ocak M, Kabasakal L et al (2014) (68)Ga-PSMA PET/CT imaging of metastatic clear cell renal cell carcinoma. Eur J Nucl Med Mol Imaging 41:1461–1462PubMedCrossRef
35.
Afshar-Oromieh A, Malcher A, Eder M et al (2013) PET imaging with a [68Ga]gallium-labelled PSMA ligand for the diagnosis of prostate cancer: biodistribution in humans and first evaluation of tumour lesions. Eur J Nucl Med Mol Imaging 40:486–495PubMedCrossRef
36.
37.
U.S. Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research Center for Biologics Evaluation and Res. The radioactive drug research committee: human research without an investigational new drug application. 2010
38.
Deloar HM, Fujiwara T, Shidahara M et al (1999) Internal absorbed dose estimation by a TLD method for 18F-FDG and comparison with the dose estimates from whole body PET. Phys Med Biol 44:595–606PubMedCrossRef
39.
Hartmann H, Freudenberg R, Oehme L et al (2014) Dosimetric measurements of (68)Ga-high affinity DOTATATE: twins in spirit - part III. Nuklearmedizin. J Nucl Med 53:211–216
40.
Zechmann CM, Afshar-Oromieh A, Armor T et al (2014) Radiation dosimetry and first therapy results with a (124)I/ (131)I-labeled small molecule (MIP-1095) targeting PSMA for prostate cancer therapy. Eur J Nucl Med Mol Imaging 41:1280–1292PubMedCentralPubMedCrossRef
41.
Afshar-Oromieh A, Avtzi E, Giesel FL et al (2015) The diagnostic value of PET/CT imaging with the (68)Ga-labelled PSMA ligand HBED-CC in the diagnosis of recurrent prostate cancer. Eur J Nucl Med Mol Imaging 42:197–209PubMedCentralPubMedCrossRef
42.
Kim JH, Lee JS, Kim JS et al (2010) Physical performance comparison of Ga-68 and F-18 in small animal PET systems [abstract]. J Nucl Med 51(Supplement 2):1423
Metadata
Title
Initial Evaluation of [18F]DCFPyL for Prostate-Specific Membrane Antigen (PSMA)-Targeted PET Imaging of Prostate Cancer
Authors
Zsolt Szabo
Esther Mena
Steven P. Rowe
Donika Plyku
Rosa Nidal
Mario A. Eisenberger
Emmanuel S. Antonarakis
Hong Fan
Robert F. Dannals
Ying Chen
Ronnie C. Mease
Melin Vranesic
Akrita Bhatnagar
George Sgouros
Steve Y. Cho
Martin G. Pomper
Publication date
01-08-2015
Publisher
Springer US
Published in
Molecular Imaging and Biology / Issue 4/2015
Print ISSN: 1536-1632
Electronic ISSN: 1860-2002
DOI
https://doi.org/10.1007/s11307-015-0850-8

Other articles of this Issue 4/2015

Molecular Imaging and Biology 4/2015 Go to the issue

Original Article

Perturbed Development of Striatal Dopamine Transporters in Fatty Versus Lean Zucker Rats: a Follow-up Small Animal PET Study

Research Article

Evaluations of Tumor Acidosis Within In Vivo Tumor Models Using Parametric Maps Generated with AcidoCEST MRI

Research Article

Correlation between Choline Peak at MR Spectroscopy and Calcium-Sensing Receptor Expression Level in Breast Cancer: A Preliminary Clinical Study

Editorial

Precision Medicine…Visualized—a Message from the President of the WMIC

Research Article

Inhibition of Lipid Oxidation Increases Glucose Metabolism and Enhances 2-Deoxy-2-[18F]Fluoro-d-Glucose Uptake in Prostate Cancer Mouse Xenografts

Research Article

A Hyaluronic Acid-Conjugated Gadolinium Hepatocyte-Specific T1 Contrast Agent for Liver Magnetic Resonance Imaging