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Article Abstract
Objective: In the recent time, endoradionuclide therapy for metastatic castration-resistant prostate carcinoma employing Lu-PSMA-617 has yielded encouraging results and several clinical trials with the agent are currently ongoing. Routine preparation of Lu-PSMA-617 patient doses can be made simpler and convenient, if the ingredients essential for radiolabeling are made available in a ready-to-use lyophilized form.
Methods: PSMA-617 freeze-dried kit was formulated and used for the preparation of Lu-PSMA-617 clinical dose with high radiochemical purity using low/medium specific activity Lu. Detailed radiochemical studies were performed to determine the maximum activity and volume of LuCl, which can be added in the kit for the formulation of Lu-PSMA-617. Studies were also performed to determine the shelf life of the kit to ensure its long-term usage. Studies were performed in buffer as well as human serum medium to determine the stability of the Lu-PSMA-617 complex after storing in respective media up to 7 days postpreparation. About ten patient doses of Lu-PSMA-617 were administered, and posttherapy scans were acquired.
Results: The formulated freeze-dried kit of PSMA-617 could be radiolabeled with an average percentage radiochemical purity > 98.53 ± 0.38. The freeze-dried kit was found suitable for tolerating up to 0.5 mL of LuCl (in 0.01 N HCl) and specific activity of 555 MBq/g (15 mCi/g) for the preparation of the patient dose of Lu-PSMA-617. The Lu-PSMA-617 complex prepared using the freeze-dried kit of PSMA-617 was observed to maintain % radiochemical purity (RCP) of 96.74 ± 0.87 and 94.81 ± 2.66, respectively, even after storing up to 7 days in buffer and human serum, respectively. Lu-PSMA-617 prepared using the in-house formulated freeze-dried kit of PSMA-617 exhibited accumulation in metastatic lesions picked up in a pretherapy PET scan. Reduction in number as well as size of lesions was observed in posttherapy scans acquired after two months of administering the first therapeutic dose of Lu-PSMA-617.
Conclusions: The freeze-dried kit of PSMA-617 could be used for the preparation of Lu-PSMA-617 with high radiochemical purity (>98%) in a reproducible manner. Lu-PSMA-617 prepared using the developed kit was successfully evaluated in patients suffering from metastatic prostate cancer.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC8627353 | PMC |
| http://dx.doi.org/10.1155/2021/1555712 | DOI Listing |
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