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. 2010 Jul 22;53(14):5333-41.
doi: 10.1021/jm100623e.

68Ga-labeled inhibitors of prostate-specific membrane antigen (PSMA) for imaging prostate cancer

Sangeeta Ray Banerjee  1 , Mrudula Pullambhatla, Youngjoo Byun, Sridhar Nimmagadda, Gilbert Green, James J Fox, Andrew Horti, Ronnie C Mease, Martin G Pomper
Affiliations

68Ga-labeled inhibitors of prostate-specific membrane antigen (PSMA) for imaging prostate cancer

Sangeeta Ray Banerjee et al. J Med Chem. .

Abstract

Gallium-68 is a generator-produced radionuclide for positron emission tomography (PET) that is being increasingly used for radiolabeling of tumor-targeting peptides. Compounds [(68)Ga]3 and [(68)Ga]6 are high-affinity urea-based inhibitors of the prostate-specific membrane antigen (PSMA) that were synthesized in decay-uncorrected yields ranging from 60% to 70% and radiochemical purities of more than 99%. Compound [(68)Ga]3 demonstrated 3.78 +/- 0.90% injected dose per gram of tissue (%ID/g) within PSMA+ PIP tumor at 30 min postinjection, while [(68)Ga]6 showed a 2 h PSMA+ PIP tumor uptake value of 3.29 +/- 0.77 %ID/g. Target (PSMA+ PIP) to nontarget (PSMA- flu) ratios were 4.6 and 18.3, respectively, at those time points. Both compounds delineated tumor clearly by small animal PET. The urea series of imaging agents for PSMA can be radiolabeled with (68)Ga, a cyclotron-free isotope useful for clinical PET studies, with maintenance of target specificity.

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Figures

Figure 1
Figure 1
Urea-based PSMA radioligands 99mTcL1, [68Ga]3 and [68Ga]6.
Figure 2
Figure 2
GE eXplore VISTA pseudodynamic PET image (co-registered with the corresponding CT image) of a PSMA+ LNCaP tumor-bearing mouse injected intravenously with 0.2 mCi (7.4 MBq) of [68Ga]3.
Figure 3
Figure 3
GE eXplore VISTA PET image (co-registered with the corresponding CT image) of a PSMA+ PIP and PSMA− flu tumor-bearing mouse injected intravenously with 0.2 mCi (7.4 MBq) of [68Ga]6.
Scheme 1
Scheme 1
Scheme 2
Scheme 2
See this image and copyright information in PMC

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