lutetium Lu 177 satoreotide tetraxetan

Lutetium Lu 177 satoreotide tetraxetan (also known as 177Lu-DOTA-JR11 or 177Lu-OPS201) is a clinical-stage, targeted therapeutic radiopharmaceutical (radioligand therapy) developed by Ariceum Therapeutics. It consists of the somatostatin receptor type 2 (SSTR2) antagonist peptide satoreotide tetraxetan (JR11) conjugated via the chelator DOTA to the beta-emitting radioisotope lutetium-177 (Lu-177). Unlike conventional SSTR agonists (such as Lu-177 DOTATATE) which internalize into cells, satoreotide tetraxetan is an antagonist that binds to both active and inactive SSTR2 conformations on the cell membrane, occupying more binding sites and delivering a higher cumulative radiation dose to tumor cells. Upon binding, the Lu-177 payload delivers localized, cytotoxic beta radiation that induces DNA double-strand breaks and cell death. Originally developed by OctreoPharm Sciences and subsequently acquired by Ipsen, the global development rights were licensed to Ariceum Therapeutics in 2021. The drug is currently in Phase I/II clinical trials for the treatment of SSTR2-positive neuroendocrine tumors (NETs), extensive-stage small cell lung cancer (ES-SCLC), and progressive meningiomas.

Other names

177Lu-satoreotide tetraxetanLu-177 DOTA-JR11Lu177 DOTA-JR11Lu 177 DOTA-JR11Lu-177 satoreotide tetraxetanLu177 satoreotide tetraxetanLu 177 satoreotide tetraxetanlutetium (177Lu) satoreotide tetraxetanlutetium Lu 177 satoreotide tetraxetansatoreotide tetraxetan lutetium Lu-177satoreotide tetraxetan lutetium-177