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. 2021 Nov 20:2021:1555712.
doi: 10.1155/2021/1555712. eCollection 2021.

Preparation of 177Lu-PSMA-617 in Hospital Radiopharmacy: Convenient Formulation of a Clinical Dose Using a Single-Vial Freeze-Dried PSMA-617 Kit Developed In-House

Mohini Guleria  1 , Jeyachitra Amirdhanayagam  1 , Haladhar D Sarma  2 , Ramya Priya Rallapeta  3 , V S Krishnamohan  3 , Ajit Nimmagadda  3 , Parthasarathy Ravi  3 , Sailaja Patri  3 , Tekchand Kalawat  3 , Tapas Das  1   4
Affiliations

Preparation of 177Lu-PSMA-617 in Hospital Radiopharmacy: Convenient Formulation of a Clinical Dose Using a Single-Vial Freeze-Dried PSMA-617 Kit Developed In-House

Mohini Guleria et al. Biomed Res Int. .

Abstract

Objective: In the recent time, endoradionuclide therapy for metastatic castration-resistant prostate carcinoma employing 177Lu-PSMA-617 has yielded encouraging results and several clinical trials with the agent are currently ongoing. Routine preparation of 177Lu-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 177Lu-PSMA-617 clinical dose with high radiochemical purity using low/medium specific activity 177Lu. Detailed radiochemical studies were performed to determine the maximum activity and volume of 177LuCl3, which can be added in the kit for the formulation of 177Lu-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 177Lu-PSMA-617 complex after storing in respective media up to 7 days postpreparation. About ten patient doses of 177Lu-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 177LuCl3 (in 0.01 N HCl) and specific activity of 555 MBq/μg (15 mCi/μg) for the preparation of the patient dose of 177Lu-PSMA-617. The 177Lu-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. 177Lu-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 177Lu-PSMA-617.

Conclusions: The freeze-dried kit of PSMA-617 could be used for the preparation of 177Lu-PSMA-617 with high radiochemical purity (>98%) in a reproducible manner. 177Lu-PSMA-617 prepared using the developed kit was successfully evaluated in patients suffering from metastatic prostate cancer.

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Conflict of interest statement

The authors declare that they have no conflict of interests.

Figures

Figure 1
Figure 1
Paper chromatography patterns of (a) free 177LuCl3 and (b) 177Lu-PSMA-617 obtained using acetonitrile : water (1 : 1, v/v) as the eluting solvent.
Figure 2
Figure 2
Typical HPLC profiles of (a) free 177LuCl3 and (b) 177Lu-PSMA-617.
Figure 3
Figure 3
HPLC profiles depicting stability of 177Lu-PSMA-617, prepared using the freeze-dried PSMA-617 kit, at two different postpreparation time points viz. 1 d and 7 d.
Figure 4
Figure 4
Stability of 177Lu-PSMA-617, prepared using the freeze-dried PSMA-617 kit, in human blood serum at different postpreparation time points viz. 1 d, 2 d, 5 d, and 7 d.
Figure 5
Figure 5
HPLC profile of 177Lu-PSMA-617, prepared using the freeze-dried PSMA-617 kit stored for one year at 2-8°C.
Figure 6
Figure 6
18F-PSMA-1007 (PET-CT) scans: (a) maximum intensity projection (MIP) PET image, (b) noncontrast CT (sagittal) image, and (c) PET-CT fused sagittal image showing multiple PSMA-avid lesions in bone (skull, spine, and right femur) and right-side cervical nodes.
Figure 7
Figure 7
SPECT scans (anterior and posterior) of the same patient (a and b), obtained at 24 h postadministration of the first and second therapeutic doses of 177Lu-PSMA-617, prepared using the freeze-dried PSMA-617 kit, respectively.
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