Lutetium (177Lu) DOTA complex (177Lu-DOTA)

The Lutetium (177Lu) DOTA complex is a stable radiometal-chelate coordination compound consisting of the beta-emitting radioisotope Lutetium-177 (177Lu) sequestered within the macrocyclic chelator 1,4,7,10-tetraazacyclododecane-1,4,7,10-tetraacetic acid (DOTA) [11, 14]. It is not a biological target but rather a therapeutic payload used in targeted radionuclide therapy (TRT), where it is covalently linked to targeting vectors such as peptides or small molecules that recognize specific tumor-associated antigens [1, 9]. Upon binding to its biological target (e.g., somatostatin receptors or PSMA) and subsequent internalization, the 177Lu isotope undergoes beta decay, releasing high-energy electrons that induce lethal DNA damage in the vicinity of the tumor cell [2, 8]. Additionally, the accompanying gamma emissions facilitate real-time imaging and personalized dosimetry, making it a cornerstone of the theranostic approach in oncology [11, 15]. While highly effective at delivering localized radiation, its use requires careful management of potential toxicities to the bone marrow and kidneys [1, 13].

Other names

177Lu-DOTALutetium-177 DOTALutetium-177 tetraazacyclododecanetetraacetic acid177Lu-DOTA chelateLutetium-177 DOTA complex

The complex acts as a radioactive payload that delivers localized beta-particle radiation to induce DNA damage and apoptosis in target cells. It also emits gamma radiation for theranostic imaging and dosimetry.