Loading
Somatostatin receptor 2 is a hormone receptor densely present on neuroendocrine tumours, and was the first theranostic target to reach routine care.
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.
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.
Somatostatin receptor 2 is a hormone receptor densely present on neuroendocrine tumours, and was the first theranostic target to reach routine care.
G-protein-coupled receptor; also expressed in meningioma, small-cell lung cancer, and some breast cancers.
9 products aim at Somatostatin receptor 2: radioligands, small molecules, hormonal therapies, 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.
Tumour-associated overexpression or amplification: 1 of 1 label readouts filed under it score protein level or gene copies (Somatostatin receptor expression by PET (SSTR-positive)), so the medicines rely on the tumour carrying more of it than normal tissue. HPA SSTR2: RNA tissue enhanced (brain 18 nTPM); blood lineage lineage enriched (granulocytes 1 nTPM); no normal tissue stained high; highest cancer staining skin cancer (1 of 12 high). Distribution: 2 cancer families in the corpus carry a prevalence row, label threshold or catalogue link for it (Neuroendocrine tumours, Lung cancer (all types)); approvals of single-target medicines aimed at it also list Pheochromocytoma and paraganglioma (PPGL), Nasal cavity and paranasal sinus cancers (including esthesioneuroblastoma), Thymoma and thymic carcinoma, Brain and spinal cord tumours (all types), not counted; Open Targets associates it with 1 specific cancer type at or above 0.5 (carcinoid tumor). (Rule 3 of scripts/fetch-target-specificity.ts.)
Sources: Somatostatin receptor expression by PET (SSTR-positive) label threshold; Human Protein Atlas SSTR2 tissue; Human Protein Atlas SSTR2 pathology; Open Targets ENSG00000180616 associations
First described 1992. Earliest sequence paper UniProt cites for the protein: Yamada et al, Proc. Natl. Acad. Sci. U.S.A, 1992, "Cloning and functional characterization of a family of human and mouse somatostatin receptors expressed in brain, gastrointestinal tract, and kidney". Source.
What a pathology or genomic report can say about this target, each with the thresholds approvals use.
G-protein-coupled receptor; also expressed in meningioma, small-cell lung cancer, and some breast cancers.
RNA: tissue enhanced (brain 18 nTPM), detected in many normal tissues. Blood: lineage enriched (granulocytes 1 nTPM).
No normal tissue stained high.
Medium only: carcinoid, cervical cancer, colorectal cancer, endometrial cancer.
HPA SSTR2 tissue · HPA SSTR2 pathology · HPA protein class: FDA approved drug targets
Human Protein Atlas version 25.1, antibody staining at reliability approved, enhanced or supported; used under CC BY-SA 3.0. Staining counts are patients per level in the atlas cohort, not population prevalence.
| 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.
CAM2029 is Camurus's monthly octreotide depot that patients can inject themselves, positive in the phase 3 SORENTO trial for gastroenteropancreatic neuroendocrine tumours against the standard depot formulations.
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.
Paltusotine is the first somatostatin-type drug that works as a once-daily pill instead of a monthly injection. It was approved in 2025 for acromegaly and is being tested for the flushing and diarrhoea of carcinoid syndrome from small-bowel neuroendocrine tumours.
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.
Monthly injections of a synthetic hormone that both quiets tumour hormone symptoms and slows tumour growth, the first treatment for most neuroendocrine tumours.
Query 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.
Shares Radioligand therapy (beta emitters) and the tag theranostic.
Shares POINT Biopharma, Auger-electron therapy, Perspective Therapeutics, Radioligand plus DNA-repair inhibitor combinations and the tag theranostic.
Shares Targeted alpha therapy, Radioligand therapy (beta emitters) and the tag theranostic.
Shares SSTR PET → PRRT, Somatostatin receptor expression by PET (SSTR-positive), PRRT (peptide receptor radionuclide therapy), IRCCS Istituto Romagnolo per lo Studio dei Tumori 'Dino Amadori' (IRST).
Shares SSTR antagonist radioligands to increase tumour dose, 177Lu-edotreotide, ITM Isotope Technologies Munich, Grade 3 well-differentiated neuroendocrine tumour.
Shares NETTER-1, 177Lu-edotreotide, COMPETE, Grade 3 well-differentiated neuroendocrine tumour.
Shares SSTR antagonist radioligands to increase tumour dose, RadioMedix, 212Pb-DOTAMTATE, Orano Med.
Shares Auger-electron therapy, PRRT (peptide receptor radionuclide therapy), IRCCS Istituto Romagnolo per lo Studio dei Tumori 'Dino Amadori' (IRST), Inselspital, Bern University Hospital / University Cancer Center Inselspital.