Ready-to-use ¹⁷⁷Lu-Rituximab injection for Non-Hodgkin's Lymphoma: Formulation and preliminary clinical study

This study was aimed at the preparation of ¹⁷⁷Lu-CHX-A″-DTPA-Rituximab injection at the hospital pharmacy for non-Hodgkin lymphoma. Rituximab was conjugated with CHX-A″-DTPA-NCS and the CHX-A″-DTPA-Rituximab conjugate was radiolabeled with ¹⁷⁷Lu in > 95% purity. The product exhibited excellent in vitro stability up to 5 days at 37 °C. In vitro cell binding studies in Raji cells confirmed the specificity of ¹⁷⁷Lu-CHX-A″-DTPA-Rituximab to CD20 antigen. The radioimmunoconjugate exhibited predominantly hepatobiliary clearance and low bone uptake in Swiss mice. Preliminary clinical studies corroborated the usefulness of ¹⁷⁷Lu-CHX-A″-DTPA-Rituximab for therapy of non-Hodgkin lymphoma. (author)