Present and future of target therapies and theranostics: refining traditions and exploring new frontiers—highlights from annals of Nuclear Medicine 2021

Pini, Cristiano; Gelardi, Fabrizia; Sollini, Martina

doi:10.1007/s00259-022-05921-7

Cited by 7 publications

(1 citation statement)

References 55 publications

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“…The use of radiopharmaceuticals for targeted radionuclide therapy (RNT), the effectiveness of which has been established during clinical trials, is currently recognized as a safe, economically, and logistically competitive method for the treatment of primary cancer, as well as distant metastases [ 1 , 2 , 3 ]. Currently, the segment of therapeutic radiopharmaceuticals comprises approximately one-third of the total number of radiopharmaceuticals in the global pharmacy market.…”

Section: Introductionmentioning

confidence: 99%

Radiolysis-Associated Decrease in Radiochemical Purity of 177Lu-Radiopharmaceuticals and Comparison of the Effectiveness of Selected Quenchers against This Process

et al. 2023

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The radiolytic degradation of vector molecules is a major factor affecting the shelf life of therapeutic radiopharmaceuticals. The development of time-stable dosage forms of radiopharmaceuticals is the key to their successful implementation in clinical practice. Using [177Lu]Lu-PSMA-617 molecule as an example, the time dependence of the change in radiochemical purity (RCP, %) under radiolysis conditions was studied. The dependence of [177Lu]Lu-PSMA-617 radiolysis on parameters such as time, radionuclide activity, buffer agent concentration, precursor amount, and preparation volume was evaluated. It was shown that the absorbed dose was the dominant factor influencing the RCP. The RCP value is inversely proportional to the absorbed dose in the [177Lu]Lu-PSMA-617 preparation and has an exponential dependence. The lutetium-177 dose factor ψ (Gy·mL·MBq−1) and PSMA-617 concentration-dependent dose constant κ (Gy−1) were evaluated for absorbed dose estimation via computer modeling, chemical dosimetry, and radiochemical purity monitoring under various conditions. The further refinement and application of the dependencies found can be useful for predicting the RCP value at the stage of optimizing the composition of the finished dosage form of therapeutic radiopharmaceuticals. The influence of the buffer agent (sodium acetate) concentration on [177Lu]Lu-PSMA-617 radiolytic degradation was shown and should be considered both when developing a dosage form, and when comparing the results of independent studies. The effectiveness of the addition of various stabilizing agents, such as DMSA, cysteine, gentisic acid, vanillin, methionine, adenine, dobesilic acid, thymine, uracil, nicotinamide, meglumine, and mannitol, in suppressing the effects of radiolysis was evaluated.

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Section: Introductionmentioning

confidence: 99%