PSMA I&T_01.png PSMA I&T_02.png PSMA I&T_03.png PSMA I&T_04.png


Corresponding ligands

Chelator With Radiometal
Bifunctional Linker

Improved Pharmacokinetics

Although the continuously increasing therapeutic use and a current phase III clinical trial impressively demonstrates the relevance of 177Lu- PSMA I&T, further rational design and SAR analyses have also resulted in a better understanding on how to improve the pharmacokinetics and renal handling of structurally similar successor compounds. 

As demonstrated in preclinical studies, modification of the arene binding inhibitor moieties resulted in radiopharmaceuticals with even higher tumor uptake, superior biodistribution, i.e. faster renal excretion and lower activity retention in the kidneys.