177Lu-Oxodotreotide (177Lu-Lutathera®, 177Lu-DOTATATE) is a radiolabeled somatostatin analogue developed for the treatment of neuroendocrine tumors (NET). The drug was launched in January 2018.

177Lu-Oxodotreotide 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 Sandostatin®.

177Lu-Oxodotreotide could be efficient for most of the GEP-NET indications but further clinical exploration is needed and studies are presently under way.

Non-NET indications in which 177Lu-Oxodotreotide is explored include: medullary thyroid cancer (initiated 2013), carcinoid heart disease (2019), metastatic Merkel cell carcinoma (2020, in combination with avelumab), meningioma (2019), pheochromocytoma and ganglioma (2017), neuroblastoma (2019) and SCLC (2017).

Non-carrier-added 177Lu labeled oxodotreotide is under development under the name 177Lu-PNT2003. This is a full analogue of Lutathera, which is completing Phase III trial. This new form may reach the market by 2023. Indications for 177Lu-PNT2003 (non GEP-NET and new GEP indications) is not supposed to overlap indications for Lutathera (mid-gut GEP-NET).

Target/Mechanism: Somatostatin receptors

Carrier/Ligand: Oxodotreotide

Radiation Type: beta electrons (β)