Presented at the 18th EBF Open Symposium
Dany Spaggiari, Francesca Tessaro, Frederic Massière, Emilie Da Costa Branquinho, Severin Mamet
Introduction
Targeted radioligand agents are a rapidly emerging class of drug modalities in oncology. They are comprised of a tumor-targeting moiety linked to a chelator (e.g., DOTA) which can bind a radionuclide such as Ga-68 or Lu-177 for theranostic applications. Typically, the administered agent is a mixture of radiolabeled and unlabeled ligands. The clinical trials of such compounds pose unique challenges regarding bioanalysis and biosample management. Radioactive biological samples (whole blood, plasma, urine) have to be collected, stored, and dispatched to various laboratories. Some “hot” analyses require to be conducted within minimal radioactivity decay at clinical sites in a harmonized way. Some “cold” analyses require prior radioactivity decay. Here, we describe a strategy with integrated bioanalytical and biosample workflows to streamline sample management and data collection. This strategy was successfully employed in a dose-escalating clinical trial of a radioligand labeled with Ga-68 and non-carrier-added (n.c.a) Lu-177 where the targeting moiety, a cyclic peptidomimetic, posed an additional technical challenge with the mass spectrometry analysis.