Somatostatin Analogues
17 compounds in this family, each with its recorded mechanism, routes of administration, safety notes and references to published literature.
- 99mTc-HYNIC (Tyr3)-octreotide99mTc-HYNIC‑(Tyr3)-octreotide is an investigational radiopharmaceutical that combines a somatostatin‑analogue peptide with technetium‑99m. After intravenous injection it binds somatostatin receptors on neuroendocrine tumour cells, allowing gamma‑camera imaging of receptor‑positive lesions. It is used primarily for diagnostic localisation, staging and follow‑up of neuroendocrine tumours, offering an alternative to the older 111In‑octreotide scans.
- Copper oxodotreotide Cu-64Cu‑64‑labeled oxodotreotide is a radiopharmaceutical used experimentally for PET imaging of SSTR2‑expressing neuroendocrine tumors. The peptide chelates Cu‑64 via a DOTA moiety, providing high‑resolution PET signal.
- DepreotideDepreotide is a technetium‑99m‑labeled synthetic analogue of somatostatin used as a radiopharmaceutical for single‑photon emission computed tomography (SPECT). It is employed primarily to image tumours that express somatostatin receptors, especially indeterminate pulmonary nodules and, in limited studies, bone metastases from breast cancer.
- DopastatinDopastatin is a research‑stage chimeric peptide that combines a somatostatin analogue with a dopamine‑D2 receptor agonist. It is being investigated for disorders in which excess pituitary hormone secretion or neuroendocrine tumour growth is driven by somatostatin and dopamine receptor pathways, such as acromegaly, prolactin‑secreting adenomas, Cushing’s disease and gastro‑entero‑pancreatic neuroendocrine tumours. The compound remains experimental, with no regulatory approval for any indication.
- Dotatate gallium Ga-68Gallium Ga-68 dotatate (Netspot) is an FDA-approved PET imaging agent used for the localization of somatostatin receptor-positive neuroendocrine tumors (NETs) in adults and pediatric patients (≥2 years). It consists of the somatostatin analogue DOTA-Tyr3-octreotate chelated to the radiometal gallium-68 and provides superior sensitivity and resolution compared to conventional somatostatin receptor scintigraphy (octreotide scan).
- EdotreotideEdotreotide is a radiolabeled somatostatin analogue used in peptide receptor radionuclide therapy (PRRT) for advanced, somatostatin‑receptor‑positive neuroendocrine tumours (NETs), especially gastro‑enteropancreatic (GEP) NETs. The drug is administered intravenously as a Lu‑177‑edotreotide complex and delivers targeted beta‑radiation to tumour cells, aiming to halt disease progression and improve survival.
- Edotreotide yttrium Y-90Edotreotide yttrium (90Y‑DOTATOC) is a radiolabeled somatostatin analogue used in peptide‑receptor radionuclide therapy (PRRT) for somatostatin‑receptor‑positive tumours, especially neuroendocrine tumours (NETs), gastro‑enteropancreatic NETs, pheochromocytomas and paragangliomas. The compound is administered intravenously and delivers high‑energy beta radiation from yttrium‑90 to tumour cells that express the sst2 receptor, aiming to halt tumour growth and induce tumour regression.
- Indium In-111 pentetreotideIndium‑111 pentetreotide (OctreoScan) is a radiolabelled somatostatin analogue used as a diagnostic imaging tracer. After intravenous injection, it binds to somatostatin receptor subtype 2 on neuroendocrine and certain paraganglioma cells, allowing gamma‑camera scintigraphy to locate primary tumors and metastases. It is employed in both human and veterinary medicine for conditions such as insulinomas, carcinoid tumors, carotid body tumors, and orbital metastases from neuroendocrine cancers.
- LanreotideLanreotide is a long‑acting synthetic analogue of somatostatin approved for prescription use. It is administered by subcutaneous injection and is employed to suppress excess hormone secretion in conditions such as thyrotropin‑secreting pituitary adenomas and acromegaly, and to slow disease progression in well‑differentiated, somatostatin‑receptor positive enteropancreatic neuroendocrine tumours.
- Lutetium Lu 177 dotatateLutetium Lu 177 dotatate (Lutathera) is an FDA‑approved radiopharmaceutical that combines the somatostatin analogue DOTATATE with the beta‑emitting radionuclide lutetium‑177. It is indicated for patients with somatostatin receptor‑positive gastroenteropancreatic neuroendocrine tumors (GEP‑NETs). By delivering targeted radiation to receptor‑expressing cells, it aims to control tumor growth while sparing most normal tissues.
- Lutetium Lu177 EdotreotideLutetium‑177 edotreotide (177Lu‑DOTATOC) is a radiolabeled somatostatin analogue used in peptide‑receptor radionuclide therapy (PRRT). The molecule binds somatostatin receptors, especially SSTR2, on neuroendocrine and other SSTR‑expressing tumours and delivers beta‑particle radiation to destroy cancer cells. It is administered intravenously under prescription and is approved for clinical use in SSTR‑positive neuroendocrine neoplasms, with exploratory applications in breast neuroendocrine carcinoma, adrenocortical carcinoma, and meningioma.
- OctreotideOctreotide is a synthetic analogue of the hormone somatostatin that binds somatostatin receptors to suppress hormone secretion and reduce splanchnic blood flow. It is used clinically to manage symptoms of neuroendocrine tumours, control acute variceal bleeding, and treat other hormone‑related conditions.
- PasireotidePasireotide is a synthetic analogue of somatostatin that binds multiple somatostatin receptor subtypes. It is approved as a prescription medication for the treatment of Cushing's disease when surgery is not curative or feasible, and is being investigated for refractory dumping syndrome. The drug is administered by injection and works by suppressing hormone secretion from pituitary and gastrointestinal sources.
- PentetreotidePentetreotide, marketed as OctreoScan, is an indium‑111‑labeled somatostatin analogue used in nuclear medicine to image tumours that express somatostatin receptors, especially neuroendocrine tumours (NETs) and certain paragangliomas. After intravenous injection, the radiopharmaceutical circulates and binds to receptor‑positive cells, allowing whole‑body scintigraphy to locate primary lesions, assess disease spread, and guide therapeutic decisions.
- TT-232TT-232 is a synthetic cyclic heptapeptide derived from somatostatin. It is being investigated as a research compound for analgesic, anti‑inflammatory and anticancer applications. The peptide shows high affinity for somatostatin receptor subtype 4 (SST4) and also interacts with SST1, providing a non‑endocrine mode of action that distinguishes it from native somatostatin.
- VapreotideVapreotide is an investigational somatostatin analogue administered intravenously or subcutaneously. It has been studied as an adjunct in pancreatic surgery and as a vasoactive agent for acute esophageal variceal bleeding in patients with portal hypertension. Research suggests it may lower postoperative complications after distal pancreatectomy and improve bleeding control in variceal hemorrhage, though it remains unapproved for routine clinical use.
- VeldoreotideVeldoreotide is an investigational cyclic octapeptide somatostatin analogue that binds to somatostatin receptor subtypes 2, 4 and 5, with particularly high efficacy as an SSTR4 agonist. It is being studied for its ability to suppress hormone secretion and inhibit proliferation of neuroendocrine tumor cells. The peptide is administered subcutaneously in experimental settings and is being evaluated for conditions such as neuroendocrine tumors and disorders characterized by excess secretory activity.