2-(3-{1-Carboxy-5-[(6-[F-18]Fluoro-Pyridine-3-Carbonyl)-Amino]-Pentyl}-Ureido)-Pentanedioic Acid, [F-18]DCFPyL, a PSMA-Based PET Imaging Agent for Prostate Cancer
DC Field | Value | Language |
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dc.contributor.author | Chen, Ying | - |
dc.contributor.author | Pullambhatla, Mrudula | - |
dc.contributor.author | Foss, Catherine A. | - |
dc.contributor.author | Byun, Youngjoo | - |
dc.contributor.author | Nimmagadda, Sridhar | - |
dc.contributor.author | Senthamizhchelvan, Srinivasan | - |
dc.contributor.author | Sgouros, George | - |
dc.contributor.author | Mease, Ronnie C. | - |
dc.contributor.author | Pomper, Martin G. | - |
dc.date.accessioned | 2021-09-07T05:02:32Z | - |
dc.date.available | 2021-09-07T05:02:32Z | - |
dc.date.created | 2021-06-19 | - |
dc.date.issued | 2011-12-15 | - |
dc.identifier.issn | 1078-0432 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/110901 | - |
dc.description.abstract | Purpose: We have synthesized and evaluated in vivo 2-(3-{1-carboxy-5-[(6-[F-18]fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-pentanedioicacid, [F-18]DCFPyL, as a potential imaging agent for the prostate-specific membrane antigen (PSMA). PSMA is upregulated in prostate cancer epithelia and in the neovasculature of most solid tumors. Experimental Design: [F-18] DCFPyL was synthesized in two steps from the p-methoxybenzyl (PMB) protected lys-C(O)-glu urea precursor using 6-[F-18]fluoronicotinic acid tetrafluorophenyl ester ([F-18]F-PyTFP) for introduction of F-18. Radiochemical synthesis was followed by biodistribution and imaging with PET in immunocompromised mice using isogenic PSMA PC3 PIP and PSMA-PC3 flu xenograft models. Human radiation dosimetry estimates were calculated using OLINDA/EXM 1.0. Results: DCFPyL displays a K-i value of 1.1 +/- 0.1 nmol/L for PSMA. [F-18] DCFPyL was produced in radiochemical yields of 36%-53% (decay corrected) and specific radioactivities of 340-480 Ci/mmol (12.6-17.8 GBq/mu mol, n = 3). In an immunocompromised mouse model [F-18] DCFPyL clearly delineated PSMA+ PC3 PIP prostate tumor xenografts on imaging with PET. At 2 hours postinjection, 39.4 +/- 5.4 percent injected dose per gramof tissue (%ID/g) was evident within the PSMA+ PC3 PIP tumor, with a ratio of 358:1 of uptake within PSMA+ PC3 PIP to PSMA- PC3 flu tumor placed in the opposite flank. At or after 1 hour postinjection, minimal nontarget tissue uptake of [F-18] DCFPyL was observed. The bladder wall is the dose-limiting organ. Conclusions: These data suggest [F-18] DCFPyL as a viable, new positron-emitting imaging agent for PSMA-expressing tissues. Clin Cancer Res; 17(24); 7645-53. (C)2011 AACR. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | AMER ASSOC CANCER RESEARCH | - |
dc.subject | GLUTAMATE-CARBOXYPEPTIDASE-II | - |
dc.subject | MEMBRANE ANTIGEN-EXPRESSION | - |
dc.subject | UREA-BASED INHIBITORS | - |
dc.subject | PRECLINICAL EVALUATION | - |
dc.subject | MONOCLONAL-ANTIBODIES | - |
dc.subject | TARGET | - |
dc.subject | C-11-ACETATE | - |
dc.subject | THERAPY | - |
dc.subject | RADIOSYNTHESIS | - |
dc.subject | XENOGRAFTS | - |
dc.title | 2-(3-{1-Carboxy-5-[(6-[F-18]Fluoro-Pyridine-3-Carbonyl)-Amino]-Pentyl}-Ureido)-Pentanedioic Acid, [F-18]DCFPyL, a PSMA-Based PET Imaging Agent for Prostate Cancer | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Byun, Youngjoo | - |
dc.identifier.doi | 10.1158/1078-0432.CCR-11-1357 | - |
dc.identifier.scopusid | 2-s2.0-84055217846 | - |
dc.identifier.wosid | 000298410300016 | - |
dc.identifier.bibliographicCitation | CLINICAL CANCER RESEARCH, v.17, no.24, pp.7645 - 7653 | - |
dc.relation.isPartOf | CLINICAL CANCER RESEARCH | - |
dc.citation.title | CLINICAL CANCER RESEARCH | - |
dc.citation.volume | 17 | - |
dc.citation.number | 24 | - |
dc.citation.startPage | 7645 | - |
dc.citation.endPage | 7653 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Oncology | - |
dc.relation.journalWebOfScienceCategory | Oncology | - |
dc.subject.keywordPlus | GLUTAMATE-CARBOXYPEPTIDASE-II | - |
dc.subject.keywordPlus | MEMBRANE ANTIGEN-EXPRESSION | - |
dc.subject.keywordPlus | UREA-BASED INHIBITORS | - |
dc.subject.keywordPlus | PRECLINICAL EVALUATION | - |
dc.subject.keywordPlus | MONOCLONAL-ANTIBODIES | - |
dc.subject.keywordPlus | TARGET | - |
dc.subject.keywordPlus | C-11-ACETATE | - |
dc.subject.keywordPlus | THERAPY | - |
dc.subject.keywordPlus | RADIOSYNTHESIS | - |
dc.subject.keywordPlus | XENOGRAFTS | - |
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