lutetium Lu 177-edotreotide

Lutetium Lu 177-edotreotide is a radiopharmaceutical composed of the somatostatin analogue edotreotide, labeled with the beta-emitting radioisotope lutetium Lu 177. It binds with high affinity to somatostatin receptors, particularly type 2 SSTR, which are overexpressed on many neuroendocrine tumor cells. Upon binding and internalization into these cells, it delivers a cytotoxic dose of beta radiation directly to SSTR-positive tumor tissue, causing DNA damage and cell death while sparing surrounding healthy tissue. This targeted radioligand therapy is primarily developed for the treatment of gastro-entero-pancreatic neuroendocrine tumors (GEP-NETs), especially in patients with refractory or progressive disease[1][2][5][7]. Edotreotide is derived from octreotide by substituting tyrosine for phenylalanine at position three and chelated via DOTA[2]. The drug has received orphan drug designations from both EMA and FDA and has been evaluated in Phase III clinical trials for GEP-NETs[5].

Brand names

solucin

Other names

177lu–octreotide