Lutetium Lu 177 dotatate (Lutathera)
Mechanism of action
From the NCI Drug Dictionary: A radioconjugate consisting of the tyrosine-containing somatostatin analog Tyr3-octreotate (TATE) conjugated with the bifunctional, macrocyclic chelating agent tetra-azacyclododecanetetra-acetic acid (DOTA) and radiolabeled with the beta-emitting radioisotope lutetium Lu 177 with potential antineoplastic activities. Lutetium Lu 177-DOTA-TATE binds to somatostatin receptors (SSTRs), with high affinity to type 2 SSTR, present on the cell membranes of many types of neuroendocrine tumor (NET) cells. Upon binding and internalization, this radioconjugate specifically delivers a cytotoxic dose of beta radiation to SSTR-positive cells. Tyr3-octreotate (TATE) is an octreotide derivative in which phenylalanine at position 3 is substituted by tyrosine and position 8 threoninol is replaced with threonine.
Diseases for which it is established
History of changes in FDA indication
- 2018-01-26: Granted FDA approval for the treatment of somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs), including foregut, midgut, and hindgut neuroendocrine tumors in adults. (Based on NETTER-1 and ERASMUS)
History of changes in EMA indication
- 2017-09-26: Initial authorization
History of changes in Health Canada indication
- 2019-01-09: Initial notice of compliance (unclear details)
History of changes in PMDA indication
- 2021-06-23: Newly indicated for the treatment of somatostatin receptor-positive neuroendocrine tumor.
Patient Drug Information
Also known as
- Generic name: lutetium (177Lu) oxodotreotide
- Brand name: Lutathera