[177Lu]Lu-IBA-DOTA-(PEG28)2-A20FMDV2

[177Lu]Lu-IBA-DOTA-(PEG28)2-A20FMDV2 is a targeted radiopharmaceutical conjugate designed for the treatment of cancers overexpressing the integrin αvβ6 receptor, such as pancreatic ductal adenocarcinoma. The drug consists of the A20FMDV2 peptide, derived from the foot-and-mouth disease virus, which serves as a high-affinity targeting ligand for αvβ6. To address the rapid renal clearance typical of small peptides, the construct is bi-terminally PEGylated with PEG28 linkers and incorporates a 4-(p-iodophenyl)butyric acid (IBA) moiety as a reversible albumin binder to significantly extend blood circulation half-life and enhance tumor uptake. The therapeutic component is the beta-emitting radionuclide Lutetium-177 (¹⁷⁷Lu), coordinated by a DOTA chelator. Preclinical studies in BxPC-3 tumor-bearing mice have demonstrated significant tumor growth inhibition, although dose-dependent renal toxicity remains a consideration for further optimization.