Pre-clinical Physiologically Based Pharmacokinetic Modelling of PSMA Radioligands: Analysis of Unspecific Uptakes and Unspecific Uptake Reference Tissues (EANM 2026) - Sep 29, 2026 - Abstract #EP-0211; "Materials and Pre-clinical mouse biodistribution data were obtained for two conventional PSMA radioligands, [177Lu]Lu-PSMA-617 and [177Lu]Lu-PSMA-I&T, and for three albumin-binding PSMA radioligands, [177Lu]Lu-SibuDAB, [177Lu]Lu-PSMA-ALB-53 and [177Lu]Lu-PSMA-ALB-56... This study demonstrates that neglecting unspecific uptakes leads to activity underestimations in PSMA-negative tissues, which is particularly relevant for the radiosensitive PSMA-negative red marrow. Implementing unspecific uptake in the PBPK model reduced underestimations and improved overall model performance. Using muscle as a predictor of unspecific uptake parameters outperformed other tissues as predictors and the baseline model, illustrating that a simplified PBPK model with unspecific uptake could potentially outperform a conventional model regarding PSMA-negative tissues."
PK/PD data • Preclinical • Castration-Resistant Prostate Cancer • Genito-urinary Cancer • Prostate Cancer • Solid Tumor
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A. Alvers 1; A. K. Mapanao 2; C. Müller 2, 3; P. Bernhardt 1, 4
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