177Lu-DOTATATE for the treatment of gastroenteropancreatic neuroendocrine tumors

Introduction: ¹⁷⁷Lutetium-[DOTA°,Tyr³]octreotate (¹⁷⁷Lu-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 ¹⁷⁷Lu.Areas Covered: Herein we describe the pharmacology, clinical efficacy and adverse event data from prospective and retrospective studies with ¹⁷⁷Lu-DOTATATE. We discuss the role of ¹⁷⁷Lu-DOTATATE within the current treatment landscape for GEP NET patients.Expert Opinion: ¹⁷⁷Lu-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 ¹⁷⁷Lu-DOTATATE fits into the treatment sequence for GEP NET patients remains an area of active investigation.