PT  - JOURNAL ARTICLE
AU  - Ying Chen
AU  - Mrudula Pullambhatla
AU  - Catherine Foss
AU  - Sridhar Nimmagadda
AU  - Youngjoo Byun
AU  - James Fox
AU  - Ronnie Mease
AU  - Martin Pomper
TI  - Synthesis and biological evaluation of [<sup>18</sup>F]DCFPyL for PSMA-targeted imaging of prostate cancer
DP  - 2011 May 01
TA  - Journal of Nuclear Medicine
PG  - 294--294
VI  - 52
IP  - supplement 1
4099  - http://jnm.snmjournals.org/content/52/supplement_1/294.short
4100  - http://jnm.snmjournals.org/content/52/supplement_1/294.full
SO  - J Nucl Med2011 May 01; 52
AB  - 294 Objectives Previously we demonstrated successful imaging of prostate tumor xenografts that express the prostate specific membrane antigen (PSMA) using the 18F-labeled cystine-glutamate urea [18F]DCFBC and the lysine-glutamate urea [18F]DCFBzL. Here we extend that work by testing 2-(3-{1-carboxy-5-[(6-[18F]fluoro-pyridine-3-carbonyl)-amino]-pentyl}-ureido)-pentanedioic acid ([18F]DCFPyL). Methods [18F]DCFPyL was prepared by the reaction of [18F]F-Py-TFP with Lys-NHC(O)NH-glu-tri-p-methoxybenzyl ester followed by ester cleavage. SCID mice bearing PSMA+ PC-3 PIP tumor and a PSMA- PC-3 flu tumor in opposite flanks were injected intravenously prior to PET imaging and biodistribution. Results The radiochemical yield (n.d.c) for [18F]DCFPyL was 39-42% from [18F]F-Py-TFP and the specific radioactivity was 340-480 mCi/μmol (12.6-17.8 GBq/μmol). Imaging showed PSMA selective uptake with very low non-target uptake. Biodistribution of [18F]DCFPyL showed significant uptake in the PIP tumors which remained high over 4 h. Uptake in PSMA+ PC-3 PIP tumor was 46.7 ± 5.8 % ID/g at 30 min p.i. and 36.6 ± 4.3 % ID/g at 4 h. Uptake in flu tumor ranged from 1.2 ± 0.4 % ID/g at 30 min p.i. to 0.03 ± 0.01 % ID/g at 4 h. PIP to flu ratio was 123:1 at 1 h p.i.. Radioactivity cleared from normal organs. The PIP tumors (T)/blood, T/liver, T/spleen, T/kidney, and T/muscle ratios were: 30, 12, 6, 0.6, 120 at 30 min; 184, 15, 16, 1, 72 at 1 h; 92, 18, 57, 3, 986 at 2 h; and 1219, 20, 159, 5, 731 at 4 h. Conclusions [18F]DCFPyL shows high and prolonged uptake in PSMA expressing tumors in mice and rapid clearance from normal organs. It is an attractive candidate for further studies of PET imaging of prostate cancer