177Lu-Satoreotide tetratexan (177Lu-OPS201, 177Lu-DOTA-JR11) is the lutetium-177 analogue of 90Y-OPS201, a proprietary drug that specifically binds to somatostatin receptors (antagonist, ssr2) and can be used for treating neuroendocrine neoplasms. The drug is being developed in parallel with the Imaging agent 68Ga-OPS202 (SOMScan®). OPS201 is based on the JR11 peptide molecule coupled to the strong DOTA Chelating agent.

JR11 is a third-generation somatostatin analogue with improved receptor binding to sst2 compared to other currently used peptides. The radiolabeled compound 177Lu-Satoreotide tetratexan has the potential to deliver up to five times more dose to NET tumor cells than other radiolabeled somatostatin analogues. On the contrary to all other analogues under development, JR11 is a receptor antagonistic, which provides a different profile to the molecule with some advantages that can be potentially translated into a higher efficacy.

First data have been collected on the basis of the 90Y-analogue and the first clinical trial has been launched in 2016. The drug is presently in Phase I/II.

Target/Mechanism: somatostatin receptors

Carrier/Ligand: Satoreotide

Radiation Type: beta electrons (β)