Prostate cancer imaging and late-stage management can be improved with prostate-specific membrane antigen (PSMA)-targeting radiotracers. We developed a PSMA positron emission tomography (PET) radiotracer, DOTHA
2-PSMA radiolabeled with
64Cu (T
1/2: 12.7 h), to leverage its large imaging time window.
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Prostate cancer imaging and late-stage management can be improved with prostate-specific membrane antigen (PSMA)-targeting radiotracers. We developed a PSMA positron emission tomography (PET) radiotracer, DOTHA
2-PSMA radiolabeled with
64Cu (T
1/2: 12.7 h), to leverage its large imaging time window. This preclinical study aimed to evaluate the biological and imaging properties of
64Cu-DOTHA
2-PSMA. Its stability was assessed in plasma ex vivo and in mice. Cellular behavior was studied for up to 48 h in LNCaP cells. Biodistribution studies were performed in balb/c mice for up to 48 h. Dynamic (1 h) and static (4 h and 24 h) PET imaging was completed in LNCaP tumor-bearing mice.
64Cu-DOTHA
2-PSMA was stable ex vivo in plasma and reached cellular internalization up to 34.1 ± 4.9% injected activity (IA)/10
6 cells at 48 h post-injection (p.i.). Biodistribution results showed significantly lower uptake in kidneys than
68Ga-PSMA-617, our reference PET tracer (
p < 0.001), but higher liver uptake at 2 h p.i. (
p < 0.001). PET images showed
64Cu-DOTHA
2-PSMA’s highest tumoral uptake at 4 h p.i., with a significant difference between blocked and non-blocked groups from the time of injection to 24 h p.i. The high stability and tumor uptake with a long tumor imaging time window of
64Cu-DOTHA
2-PSMA potentially contribute to the prostate cancer theranostic approach and its local recurrence detection.
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