Antagonist Archives

Tag: Antagonist

e.g. in the context of conventional beta PRRT (e.g. Lutathera, Lu177 Dotatate) which is based on a somatostatin receptor ‘agonist’ approach, whereas (e.g.) 177Lu Satoreotide is a receptor ‘antagonist’. The differences are quite technical but in the most layman terms, the antagonist has the capability of attaching (binding) to more receptors, including those in a ‘resting’ or ‘inactive’ state, spends more time on the tumor than agonist-based therapies. The result is a higher number of receptor binding sites and greater tumor uptake.

02 Oct 2023

By Ronny Allan

5 Comments

Neuroendocrine Cancer Clinical Trial – Lutetium-177Lu (Satoreotide)

Clinical Trials and ResearchAntagonist, Ga68 PET/CT, JR11, Neuroendocrine cancer, PRRT, Satoreotide (Lutetium-177), Small cell lung cancer (SCLC), Somatostatin receptors (SSTR)

What is Satoreotide? It's an agonist treatment. i.e. a 'next generation' radioligand for Peptide receptor radionuclide therapy (PRRT) or more specifically the radiopharmaceutical that binds to both activated and inactivated somatostatin receptors which are upregulated on these tumours. There is far higher binding via this mechanism than standard octreotate. The technical name of the radiopharmaceutical is Satoreotide tetraxetan lutetium-177 (author's note, I'm guessing but it could be a variant of Lanreotide). Somatostatin type 2 (SST2) receptor is overexpressed in many around 80% of NETs, some NEC and in certain hard-to-treat cancers such as small cell lung cancer (SCLC) and neuroblastoma,…