177Lu-DOTATATE for the treatment of gastroenteropancreatic neuroendocrine tumors

Introduction: (177)Lutetium-[DOTA degrees,Tyr(3)]octreotate (Lu-177-DOTATATE) is a type of peptide receptor radionuclide therapy that garnered FDA approval in January 2018 for the treatment of somatostatin receptor-positive gastroenteropancreatic (GEP) neuroendocrine tumor (NET) patients. The therapy approval was based on findings from the randomized international phase III NETTER-1 trial as well as outcome data from a large European registry. The mechanism of the drug stems directly from its structure: a somatostatin analog (octreotate) selectively binding to somatostatin receptor expressing cells and being internalized, along with a chelated beta-emitting isotope Lu-177. Areas Covered: Herein we describe the pharmacology, clinical efficacy and adverse event data from prospective and retrospective studies with Lu-177-DOTATATE. We discuss the role of Lu-177-DOTATATE within the current treatment landscape for GEP NET patients. Expert Opinion: Lu-177-DOTATATE represents a unique addition to the treatment armamentarium for GEP NETs because of its potential to elicit tumor cytoreduction, which is rare among other existing treatment options, and prolonged disease control. Where Lu-177-DOTATATE fits into the treatment sequence for GEP NET patients remains an area of active investigation.