OnCo
ideasIdea

SSTR antagonist radioligands to increase tumour dose

Radioligands that block the receptor instead of activating it bind many more sites on each cell, delivering more radiation per dose.

177Lu-satoreotide tetraxetan (antagonist) showed higher tumour uptake and dose than agonists in first-in-human studies; phase 1/2 trials report responses in PRRT-refractory patients.

Hypothesis
Antagonist PRRT achieves higher response rates than agonist PRRT at equivalent renal dose, including in low-SSTR-expressing tumours.
Rationale
Antagonists bind receptors in all conformational states and are not internalised, increasing binding sites several-fold.
What would test it
Randomised phase 2 antagonist vs agonist 177Lu-PRRT in grade 1-2 GEP-NETs.
Maturity
early clinical

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cancers

1
Neuroendocrine tumours

technologies

1
Peptide receptor radionuclide therapy (PRRT)

targets

1
Somatostatin receptor 2