Lutathera ®: The First FDA- and EMA-Approved Radiopharmaceutical for Peptide Receptor Radionuclide Therapy

Pharmaceuticals (Basel). 2019 Jul 29;12(3):114. doi: 10.3390/ph12030114.

Abstract

As the first radiopharmaceutical for Peptide Receptor Radionuclide Therapy (PRRT), Lutathera® was approved by the EMA in 2017 and the FDA in 2018 for the treatment of somatostatin receptor (SSTR) positive gastroenteropancreatic neuroendocrine tumors. Using the concept of PRRT, Lutathera® combines the radionuclide 177Lu with the somatostatin analogue DOTA-TATE, thus delivering ionizing radiation specifically to tumor cells expressing somatostatin receptors. As a result, DNA single- and double-strand breaks are provoked, in case of double-strand breaks leading to cell death of the tumor and its SSTR-positive lesions.

Keywords: Lutathera®, [177Lu]Lu-DOTA-TATE; neuroendocrine tumors (NET); peptide receptor radionuclide therapy (PRRT); somatostatin receptor (SSTR); thera(g)nostics.

Publication types

  • Review