Radiohalogenated Prostate-Specific Membrane Antigen (PSMA)-Based Ureas as Imaging Agents for Prostate Cancer
作者： Ying Chen , Catherine A. Foss , Youngjoo Byun , Sridhar Nimmagadda , Mrudula Pullambhatla
DOI: 10.1021/JM801055H
关键词:
摘要: To extend our development of new imaging agents targeting the prostate-specific membrane antigen (PSMA), we have used versatile intermediate 2-[3-(5-amino-1-carboxy-pentyl)-ureido]-pentanedioic acid (Lys-C(O)-Glu), which allows ready incorporation radiohalogens for single photon emission computed tomography (SPECT) and positron (PET). We prepared 2-[3-[1-carboxy-5-(4-[(125)I]iodo-benzoylamino)-pentyl]-ureido]-pentanedioic ([(125)I]3), 2-[3-[1-carboxy-5-(4-[(18)F]fluoro-benzoylamino)-pentyl]-ureido]-pentanedioic ([(18)F]6), 2-(3-[1-carboxy-5-[(5-[(125)I]iodo-pyridine-3-carbonyl)-amino]-pentyl]-ureido)-pentanedioic ([(125)I]8) in 65-80% (nondecay-corrected), 30-35% (decay corrected), 59-75% (nondecay-corrected) radiochemical yields. Compound [(125)I]3 demonstrated 8.8 +/- 4.7% injected dose per gram (%ID/g) within PSMA(+) PC-3 PIP tumor at 30 min postinjection, persisted, with clear delineation by SPECT. Similar uptake values early time points were [(18)F]6 (using PET) [(125)I]8. Because many radiohalogenated moieties that can be attached via epsilon amino group, Lys-C(O)-Glu is an attractive template upon to develop prostate cancer.
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