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.
Overview
Somatostatin receptor 2 is a G-protein-coupled receptor overexpressed on well-differentiated neuroendocrine tumours, which internalise bound somatostatin analogues and so can be both imaged and treated with the same peptide. 68Ga-DOTATATE PET (Netspot) and 177Lu-DOTATATE (Lutathera, NETTER-1 and NETTER-2) established the theranostic paradigm, in which a diagnostic scan selects patients for a matched radioligand. SSTR PET is positive in 80-90% of well-differentiated neuroendocrine tumours but lower in grade 3, and the receptor is also expressed in meningioma, 30-50% of small-cell lung cancer, and some breast cancers. Alpha-emitting 225Ac-DOTATATE (RYZ101) and 212Pb-DOTAMTATE are in phase 3, testing whether alpha particles outperform beta. The simple version is a hormone receptor that lets doctors see and treat neuroendocrine tumours with the same molecule.
- 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.
Backbone ribbon from PDB 7T10. RCSB PDB 7T10. The ribbon widens where the chain is folded into a regular pattern and narrows where it is a loose loop.
The natural peptide in the receptor the dotatate and dotatoc analogues bind.
- 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
12 products aim at Somatostatin receptor 2: radioligands, imaging agents and other 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.
External identifiers
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 often this target appears
| 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.
An injectable tracer that sticks to a marker (somatostatin receptor) many neuroendocrine tumours carry. A PET scan afterwards shows where those tumours are, including small deposits that other scans can miss.
The PET scan for neuroendocrine tumours that finds far more disease than older scans and confirms eligibility for lutetium radioligand therapy (the theranostic pair).
A cousin of the Ga-68 DOTATATE and Cu-64 DOTATATE scans: it sticks to the same receptor on neuroendocrine tumours and lets PET find them. It is FDA-approved but, unusually, has no brand name and no pharmaceutical-company sponsor.
The original nuclear medicine scan for finding neuroendocrine tumours, used before PET scans like Ga-68 DOTATATE became available. It is still FDA-approved but has largely been superseded because PET gives sharper pictures with less radiation.
A drug that targets a marker on neuroendocrine tumour cells is being tested with two versions of a radioactive metal: one lets doctors see where the tumour is on a scan, and the other delivers a strong, short-range dose of radiation to kill the tumour cells.
Lutetium-177 dotatate was the first modern radioligand therapy (2018), for neuroendocrine tumours, and is now used in first line.
A second, cheaper version of an already-approved radioactive drug for neuroendocrine tumours has been approved, using the same active radioactive ingredient as the original but made by a different company.
Pasireotide is a second-generation somatostatin analogue that hits more receptor types than octreotide. It is approved for Cushing's disease and acromegaly caused by pituitary tumours when surgery has not cured them, at the cost of frequent high blood sugar.
The original targeted radiotherapy: thyroid cells soak up iodine, so radioactive iodine destroys leftover thyroid tissue and metastases while sparing everything else.
Latest papers
topQuery for this target: (TITLE:"Somatostatin receptor 2" OR ABSTRACT:"Somatostatin receptor 2" OR TITLE:"SSTR2" OR ABSTRACT:"SSTR2") AND (radiopharmaceutical OR radioligand OR radionuclide OR theranostic OR "nuclear medicine" OR "molecular imaging" OR radiotracer OR scintigraphy OR 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.
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