SSTR antagonist radioligands to increase tumour dose
Radioligand therapy for neuroendocrine tumours built on somatostatin receptor antagonists rather than the agonists used today: antagonists bind the receptor in every state and are not internalised, so they occupy several times more sites per cell and deliver more radiation per dose. The test is a randomised phase 2 against agonist lutetium therapy.
Overview
The idea is to build peptide receptor radionuclide therapy for neuroendocrine tumours on somatostatin receptor 2 antagonists rather than the agonists used today. Antagonists bind receptors in every conformational state and are not internalised, so they occupy several times more binding sites on each cell and deliver more radiation per dose. First-in-human studies of the antagonist 177Lu-satoreotide tetraxetan showed higher tumour uptake and dose than agonists, and early trials report responses in patients refractory to agonist PRRT. The hypothesis is higher response rates at an equivalent renal dose, including in tumours with low SSTR2 expression; the test is a randomised phase 2 of antagonist versus agonist 177Lu-PRRT in grade 1 to 2 gastroenteropancreatic NETs.
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