Comparative study on application of177Lu-labeled rituximab, tetulomab, cetuximab and huA33 monoclonal antibodies to targeted radionuclide therapy

Abstract

PurposeDose coefficients from rituximab, tetulomab, cetuximab, and huA33 monoclonal antibodies labelled with the radionuclide¹⁷⁷Lu were estimated for human organs and tumours via a theoretical simulation based on experimental results.MethodsThe real experimental results were obtained from radiopharmaceutical distribution in hairless mice. Using the Sparks and Aydogan method, the cumulated activity for humans was recalculated. The simulation was used to assess the behaviour of MAbs labelled with¹⁷⁷Lu after injection into the human body. The average absorbed doses were calculated for the most exposed organs and tissues.ResultsThe huA33 monoclonal antibodies (MAbs) labelled with 177Lu (Lu-rituximab, Lu-tetulomab, Lu-cetuximab, and Lu-huA33), presented the maximum nuclear transformation per Bq intake for the main organs (blood, kidneys, liver, lung, and spleen, as well as for a tumour) The absorbed dose in the liver is three times lower for Lu-huA33 compared to the other drugs. In the case of cetuximab, the spleen received the lowest dose compared to the other drugs. The dependencies on absorbed dose for the alveolar, bronchioles, bone surface, heart wall, kidneys, liver, lung, lymphatic nodes, and spleen, are presented. For tumours, the absorbed dose for each drug is calculated separately for a sphere of unit volume by using the information on the injected dose.Conclusion, The ratios of the dose coefficient for the tumour to each organ, indicate that lutetium-177 can be recommended for targeted radionuclide therapy since the dose per tumour is much greater than the dose per organ.

Keywords: cetuximab; huA33; lutetium-177; monoclonal antibody; rituximab; targeted radionuclide therapy.; tetulomab.