Advancing fibroblast activation protein inhibitors for targeted radioligand therapy: Strategies and innovations to increase tumor residence time

Ac), as the FAPi ligand's rapid clearance limits effective radiation delivery. To enable effective clinical translation of targeted radiotherapy, optimizing pharmacokinetics is critical, prolonging tumor residence time while accelerating clearance from non-target tissues to minimize off-target radiation exposure. This review summarizes current progress in FAP-targeted radiopharmaceuticals and outlines strategies to enhance their therapeutic applicability through different strategies that lead to prolonged tumor retention.