Lutetium Lu 177 dotatate (Lutathera)

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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

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