Preparation and clinical translation of 99mTc-PSMA-11 for SPECT imaging of prostate cancer.
Kusum VatsKanhaiyalal AgrawalRohit SharmaHaladhar Dev SarmaDrishty SatpatiAshutosh DashPublished in: MedChemComm (2019)
This study explores the feasibility of radiolabeling the HBED-CC-PSMA (PSMA-11) ligand with Tc-99m for SPECT imaging of prostate cancer patients. 68Ga-HBED-CC-PSMA (PSMA-11) is used clinically for PET/CT imaging of prostate cancer (PCa) patients. However, a PET/CT facility may not be affordable and/or accessible to remotely located health centers. Thus, economic considerations require development of a SPECT-based tracer to provide low cost effective health care to the entire global population. Hence, radiochemical parameters were varied and optimized to obtain the maximum radiochemical yield of 99mTc-PSMA-11. 99mTc-PSMA-11 could be prepared in 60 ± 5% radiochemical yield and >98% radiochemical purity with a specific activity of 15 ± 5 GBq μmol-1. The radiotracer exhibited high stability in vitro in human serum after 24 h. A cell uptake of 15.2 ± 1.2% was observed for 99mTc-PSMA-11 in PSMA-positive prostate carcinoma LNCaP cells. Rapid clearance from blood, liver, intestine, lungs and other major organs was observed during normal biodistribution studies. The radiotracer, 99mTc-PSMA-11, exhibited physiological distribution in salivary and lacrimal glands similar to that of 68Ga-PSMA-11 in mice and successfully identified primary tumors as well as metastatic lesions in human patients. This study thus highlights successful radiolabeling of HBED-CC-PSMA with Tc-99m and the potential of 99mTc-PSMA-11 as a SPECT imaging agent for PCa.
Keyphrases
- pet ct
- prostate cancer
- positron emission tomography
- healthcare
- high resolution
- end stage renal disease
- newly diagnosed
- ejection fraction
- chronic kidney disease
- computed tomography
- endothelial cells
- stem cells
- squamous cell carcinoma
- oxidative stress
- health insurance
- climate change
- social media
- benign prostatic hyperplasia
- high fat diet induced
- patient reported