Somatostatin receptor 2
Somatostatin receptor 2 is a hormone receptor densely present on neuroendocrine tumours, and was the first theranostic target to reach routine care.
SSTR2 is overexpressed on well-differentiated neuroendocrine tumours. 68Ga-DOTATATE PET (Netspot) and 177Lu-DOTATATE (Lutathera, NETTER-1 and NETTER-2) established the theranostic paradigm. Alpha-emitting 225Ac-DOTATATE (RYZ101) and 212Pb-DOTAMTATE are in phase 3.
- Target · the protein and the cell it sits on
- Drug · antibody, small molecule, cell or radioligand
- Effect · signal, damage or kill
In plain words · Somatostatin receptor 2 is a hormone receptor densely present on neuroendocrine tumours, and was the first theranostic target to reach routine care.
- 1 · What it is
Somatostatin receptor 2 is a hormone receptor densely present on neuroendocrine tumours, and was the first theranostic target to reach routine care.
- 2 · What goes wrong in cancer
G-protein-coupled receptor; also expressed in meningioma, small-cell lung cancer, and some breast cancers.
- 3 · How drugs use it
7 products aim at Somatostatin receptor 2: radioligands, hormonal therapies and imaging agents. Because it sits on the outside of the cell, it can be reached from the bloodstream: antibodies flag the cell, ADCs deliver a toxin, radioligands deliver radiation, and CAR-T or bispecifics bring a T cell.
Biology
G-protein-coupled receptor; also expressed in meningioma, small-cell lung cancer, and some breast cancers.
- Neuroendocrine tumours
- Meningioma
- Small-cell lung cancer (subset)
How common it is, by cancer
| Cancer | Prevalence | Measure | Note | Source |
|---|---|---|---|---|
| Neuroendocrine tumours | 80-90% | SSTR PET positivity (well-differentiated) | Lower in grade 3 | Wikipedia |
| Small-cell lung cancer | 30-50% | IHC/imaging | Wikipedia |
Approximate, population-level figures; the measure column says what was counted. Ranges show the midpoint as a bar.
A second lutetium radioligand for neuroendocrine tumours that beat the standard pill everolimus in a head-to-head trial and is awaiting an FDA decision.
An alpha-particle version of neuroendocrine radioligand therapy that produced responses in over half of patients who had never had PRRT, with FDA Breakthrough designation.
An alpha-particle version of Lutathera for neuroendocrine tumours that have stopped responding to the beta version.
The PET scan for neuroendocrine tumours that finds far more disease than older scans and confirms eligibility for lutetium radioligand therapy (the theranostic pair).
Lutetium-177 dotatate was the first modern radioligand therapy (2018), for neuroendocrine tumours, and is now used in first line.
The original targeted radiotherapy: thyroid cells soak up iodine, so radioactive iodine destroys leftover thyroid tissue and metastases while sparing everything else.
Monthly injections of a synthetic hormone that both quiets tumour hormone symptoms and slows tumour growth, the first treatment for most neuroendocrine tumours.
Latest papers
topQuery for this target: (TITLE:"Somatostatin receptor 2" OR ABSTRACT:"Somatostatin receptor 2" OR TITLE:"SSTR2" OR ABSTRACT:"SSTR2") AND (cancer OR tumor OR tumour OR oncology OR carcinoma OR lymphoma OR leukemia OR leukaemia OR myeloma OR sarcoma OR melanoma OR glioma). Results are unfiltered search hits about Somatostatin receptor 2, not a curated reading list.