177Lu-Oxodotreotide (177Lu-Lutathera®, 177Lu-DOTATATE, 177Lu-DOTA0-Tyr3-octreotate, 177Lu-Octreotate, 177Lu-Lutate, 177Lu-Edotreotate) is a radiolabeled somatostatin analogue developed for the treatment of neuroendocrine tumors (NET). Advanced Accelerator Applications (AAA) now within Novartis owns exclusive rights to DOTATATE for therapeutic use. In terms of development of radiolabeled peptides for therapy, 177Lu-DOTATATE/Oxodotreotide is the most advanced molecule under the name Lutathera®. The drug was launched in January 2018. AAA has also been granted Orphan Drug designation status for the drug both in the US and Europe.
This radiolabeled drug has been under clinical evaluation for the past 15 years at the Erasmus MC (Rotterdam, The Netherland). Other clinical investigations have been carried out at Uppsala Sweden, Milano (Italy) and Fremantle Australia, and more recently at Bad Berka, Germany, and Basel, Switzerland. In the US, the Excel Diagnostics Nuclear Oncology Center in Houston TX was the first research facility in North America to obtain authorization to treat patients with 177Lu-DOTATATE.
177Lu-DOTATATE has been developed for treatment of patients with gastro-entero-pancreatic neuroendocrine tumors (GEP-NET). Phase II results (Erasmus MC, Rotterdam) in progressive midgut carcinoid showed progression-free survival of more than 45.1 months compared to the reported 14.6 months of Novartis’ Sandostatin® LAR®. Considering all the centers who have investigated the drug in patients, more than 3,000 patients have been treated with this drug prior to the start of the Phase III trial.