A review of advances in the last decade on targeted cancer therapy using Lu: focusing on Lu produced by the direct neutron activation route.

Lutetium-177 [T½ = 6.76 d; E (max) = 0.497 MeV; maximum tissue range ~2.5 mm; 208 keV γ-ray] is one of the most important theranostic radioisotope used for the management of various oncological and non-oncological disorders. The present review chronicles the advancement in the last decade in Lu-radiopharmacy with a focus on Lu produced via direct Lu (n, γ) Lu nuclear reaction in medium flux research reactors. The specific nuances of Lu production by various routes are described and their pros and cons are discussed. Lutetium, is the last element in the lanthanide series. Its chemistry plays a vital role in the preparation of a wide variety of radiopharmaceuticals which demonstrate appreciable stability. Traditional bifunctional chelators (BFCs) that are used for Lu-labeling are discussed and the upcoming ones are highlighted. Research efforts that resulted in the growth of various Lu-based radiopharmaceuticals in preclinical and clinical settings are provided. This review also summarizes the results of clinical studies with potent Lu-based radiopharmaceuticals that have been prepared using medium specific activity Lu produced by direct neutron activation route in research reactors. Overall, the review amply demonstrates the practicality of the medium specific activity Lu towards formulation of various clinically useful radiopharmaceuticals, especially for the benefit of millions of cancer patients in developing countries with limited reactor facilities.