Development of Potential 177Lu Radiopharmaceuticals: Design, Radiolabelling and Nonclinical Evaluation

Open for proposals

Project Type

Coordinated Research Project

Project Code




Approved Date

22 March 2023


2 - New - Collecting or Evaluating proposals


Lutetium-177 (177Lu) is currently the most important therapeutic radionuclide and it will continue to be the key role player in the nuclear medicine field in the developed and developing world. Radionuclide decay characteristics of 177Lu have specific advantages for this purpose. Eβ(max) = 497 keV offers LET with 1-2 mm effective radiation radius supporting targeted therapy at cellular level and gamma radiation component of Eg = 113 keV (6.4%) and 208 keV(11%), allows organ dosimetry. 177Lu decays to stable hafnium making waste management and patient safety easy. Its half-life of 6.65 days permits logistic of production and supply of radioisotope and finished product. The convenient half-life and lutetium chemistry supports using varying types of pharmacological carrier molecules and design radiopharmaceutical with desired pharmacokinetics to achieve high target to non-target organ ratios. Currently there are over 70 radiopharmaceuticals for therapy in clinical trials and about 40% of them are based on 177Lu alone. The mainstream includes radiopharmaceuticals for neuroendocrine tumors and prostate cancer, and this list is expected to grow fast for other indications, thanks to the identification of new biological targets and targeting vectors such as peptides, peptidomimetics, monoclonal antibodies and their engineered fragments, aptamers, targeting nanoparticles etc. This Coordinated Research Project (CRP) will identify potential carrier molecules that target some of the major cancers for labelling with 177Lu using bifunctional agents and carry out preclinical evaluation towards the development of radiopharmaceuticals for targeted therapy. 


The objective of this CRP is to develop and carry out preclinical evaluation of Lu-177 radiopharmaceuticals using bifunctional ligands to label peptides, monoclonal antibodies, enzyme inhibitors and other small molecules that target some of the major cancers and to enhance availability of Lu-177 radiopharmaceuticals in Member States (MS)

Specific objectives

To improve the design of Lu-177 radiopharmaceuticals through the introduction of novel chelating groups for the radiometal with higher stability and kinetic inertness

To design novel alternative pharmacophores for the selective targeting of receptors overexpressed by common cancers and evaluate radiopharmaceutical formulations facilitating further therapeutic development.

To guide MSs on the correct understanding and application of the principles of Good Radiopharmacy Practice (GRP) for the preparation of Lu-177 radiopharmaceuticals.

To produce protocols on quality control procedures and non-clinical studies

To evaluate the therapeutic efficacies of Lu-177 radiopharmaceuticals in comparison or in combination with other therapeutics in nonclinical studies

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