Somatostatin

Summary

Somatostatin (CHEMBL1823872) is a phase-3 clinical-stage protein (ATC H01CB01) targeting MRGPRX2, SSTR1, and SSTR2; indicated across 13 conditions including hepatocellular carcinoma and portal hypertension.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Protein
• ATC class: H01CB01
• Targets: 6 (MRGPRX2, SSTR1, SSTR2…)
• Indications: 13 conditions
• Clinical trials: 46
• Chemistry: 1637.9 Da · C76H104N18O19S2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1823872
Name	Somatostatin
Type	Protein
Max phase	3
FDA approved	no
PubChem CID	16129706
ChEBI	CHEBI:64628
ATC	H01CB01
Molecular formula	C76H104N18O19S2
Molecular weight	1637.9
InChIKey	NHXLMOGPVYXJNR-ATOGVRKGSA-N

SMILES: C[C@H]([C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)CC(=O)N)CCCCN)NC(=O)CNC(=O)[C@H](C)N)C(=O)O)CO)[C@@H](C)O)CC6=CC=CC=C6)O

IUPAC name: (4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-37-[[2-[[(2S)-2-aminopropanoyl]amino]acetyl]amino]-13,25,28-tribenzyl-10,16-bis[(1R)-1-hydroxyethyl]-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic acid

ChEBI definition: A fourteen-membered heterodetic cyclic peptide comprising the sequence Ala-Gly-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys cyclised by a disulfide bridge between the two Cys residues at positions 3 and 14.

Also known as: Somatostatin, Somatostatin-14, Somatostatina, Somatostatine, SRIF-14, somatostatin (SRIF), Somatostatin receptor ligand, SRIF, Peptide analogue, somatostatin, Somatostain, SOMATOSTATIN

Patent coverage: 1,126 distinct patent families (2,276 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 2,274 (100%) of the total. Mentions count patents naming the compound (not distinct inventions), so promiscuous / reference molecules inflate the mention figure — families are the dedup metric.

Targets

Targets

Primary targets (GtoPdb curated mechanism): the Cancer dependency column is the DepMap CRISPR fitness signal (% of screened cell lines dependent on the target).

Gene	Target	Action	pAffinity	Cancer dependency	UniProt
MRGPRX2	MRGPRX2	Agonist	5.38	0%	Q96LB1
SSTR1	SST1 receptor	Full agonist	9.4	0%	P30872
SSTR2	SST2 receptor	Full agonist	10.2	0.7%	P30874
SSTR3	SST3 receptor	Full agonist	9.9	0.2%	P32745
SSTR4	SST4 receptor	Full agonist	9.2	0.7%	P31391
SSTR5	SST5 receptor	Full agonist	10.3	0%	P35346

Broader ChEMBL bioactivity targets: 17 (assay-derived). Sample: Somatostatin receptor type 5, Somatostatin receptor type 2, Somatostatin receptor type 4, Somatostatin receptor type 1, Histamine H2 receptor, Somatostatin receptor type 3, Somatostatin receptor, Somatostatin receptor, Somatostatin receptor, Sodium-dependent noradrenaline transporter.

Bioactivity

ChEMBL activities: 76 potent at pChembl ≥ 5 of 77 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SSTR2	10.46	Ki	0.04	nM	CHEMBL_ACT_1220038
SSTR2	10.4	Ki	0.04	nM	CHEMBL_ACT_943571
SSTR2	10.31	Ki	0.05	nM	CHEMBL_ACT_1273261
SSTR5	10.19	EC50	0.07	nM	CHEMBL_ACT_1004579
O08858	10.13	IC50	0.07	nM	CHEMBL_ACT_16501787
P30935	10.1	IC50	0.08	nM	CHEMBL_ACT_370688
SSTR4	10.1	IC50	0.08	nM	CHEMBL_ACT_370689
SSTR2	10.08	Ki	0.08	nM	CHEMBL_ACT_1476988
SSTR3	10	Ki	0.1	nM	CHEMBL_ACT_1220041
SSTR2	10	EC50	0.1	nM	CHEMBL_ACT_1476992
SSTR5	9.92	Ki	0.12	nM	CHEMBL_ACT_1220040
SSTR3	9.85	Ki	0.14	nM	CHEMBL_ACT_1273263
SSTR5	9.85	Ki	0.14	nM	CHEMBL_ACT_1273265
SSTR1	9.85	IC50	0.14	nM	CHEMBL_ACT_13336161
SSTR5	9.82	Ki	0.15	nM	CHEMBL_ACT_1476991
SSTR5	9.72	EC50	0.19	nM	CHEMBL_ACT_1476993
SSTR5	9.7	IC50	0.2	nM	CHEMBL_ACT_1602003
P28646	9.7	IC50	0.2	nM	CHEMBL_ACT_173954
SSTR2	9.7	Ki	0.2	nM	CHEMBL_ACT_519231
SSTR2	9.7	Ki	0.2	nM	CHEMBL_ACT_823675
SSTR5	9.64	Ki	0.23	nM	CHEMBL_ACT_13867664
SSTR2	9.64	Ki	0.23	nM	CHEMBL_ACT_1602009
SSTR3	9.6	Ki	0.25	nM	CHEMBL_ACT_519232
SSTR5	9.59	Ki	0.26	nM	CHEMBL_ACT_1476989
P30875	9.55	IC50	0.28	nM	CHEMBL_ACT_370687
SSTR1	9.54	Ki	0.29	nM	CHEMBL_ACT_1220037
SSTR1	9.44	Ki	0.36	nM	CHEMBL_ACT_1273262
SSTR1	9.42	Ki	0.38	nM	CHEMBL_ACT_943570
SSTR2	9.4	IC50	0.4	nM	CHEMBL_ACT_1601998
SSTR3	9.4	IC50	0.4	nM	CHEMBL_ACT_1602002

Target pathways

Aggregated over 6 target gene(s): MRGPRX2, SSTR1, SSTR2, SSTR3, SSTR4, SSTR5.

Top Reactome pathways

11 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	5	SSTR1, SSTR2, SSTR3, SSTR4, SSTR5
Signaling by GPCR	5	SSTR1, SSTR2, SSTR3, SSTR4, SSTR5
Class A/1 (Rhodopsin-like receptors)	5	SSTR1, SSTR2, SSTR3, SSTR4, SSTR5
Peptide ligand-binding receptors	5	SSTR1, SSTR2, SSTR3, SSTR4, SSTR5
GPCR downstream signalling	5	SSTR1, SSTR2, SSTR3, SSTR4, SSTR5
G alpha (i) signalling events	5	SSTR1, SSTR2, SSTR3, SSTR4, SSTR5
GPCR ligand binding	5	SSTR1, SSTR2, SSTR3, SSTR4, SSTR5
Organelle biogenesis and maintenance	1	SSTR3
Cilium Assembly	1	SSTR3
Cargo trafficking to the periciliary membrane	1	SSTR3
BBSome-mediated cargo-targeting to cilium	1	SSTR3

Dominant GO biological processes

GO term	Targets
G protein-coupled receptor signaling pathway	6
signal transduction	6
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger	5
neuropeptide signaling pathway	5
negative regulation of cell population proliferation	5
somatostatin signaling pathway	5
cellular response to glucocorticoid stimulus	3
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	2
positive regulation of cytokinesis	2
cellular response to estradiol stimulus	2
positive regulation of cytokine production	1
phospholipase C-activating G protein-coupled receptor signaling pathway	1
sensory perception of pain	1
sleep	1
positive regulation of chemokine production	1

Indications & clinical

Indications

13 indications (0 at ChEMBL trial phase 4). Phase below is the highest clinical-trial phase recorded for this drug against each disease — not the molecule’s overall approval status (that is in the Summary).

Indication	Trial phase	MONDO	EFO
hepatocellular carcinoma	3	MONDO:0007256	EFO:0000182
portal hypertension	3	MONDO:0005080	EFO:0000666
gallbladder neoplasm	3	MONDO:0021253	EFO:0004606
pancreatic neuroendocrine tumor	3	MONDO:0019954	EFO:1000045
autosomal dominant polycystic kidney disease	3	MONDO:0004691	EFO:1001496
acute pancreatitis	3	MONDO:0006515	EFO:1000652
liver failure	3	MONDO:0100192	MONDO:0100192
carcinoid tumor	2	MONDO:0005369	EFO:0004243
peptic ulcer disease	2	MONDO:0004247	HP:0004398
type 1 diabetes mellitus	2	MONDO:0005147	MONDO:0005147
prostate adenocarcinoma	1	MONDO:0005082	EFO:0000673
hypoglycemia	1	MONDO:0004946	HP:0001943

1 further indication record had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.

Clinical trials

Total trials: 46.

Phase distribution

Phase	Trials
Not specified	16
PHASE4	11
PHASE3	8
PHASE1	6
PHASE2/PHASE3	2
PHASE2	2
EARLY_PHASE1	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT05701241	PHASE4	RECRUITING	Continuing Somatostatin Analogues Upon Progression in Neuroendocrine Tumour pAtients
NCT00966355	PHASE4	COMPLETED	Comparison of Terlipressin, Somatostatin, and Octreotide for Control of Variceal Bleeding
NCT01082627	PHASE4	COMPLETED	Identifying the Effect of Somatostatin Treatment in Early Postoperative Simple Small Bowel Obstruction
NCT01914692	PHASE4	COMPLETED	Application of Somatostatin for Advanced Gastric Cancer After D2 Lymph Node Dissection
NCT01992198	PHASE4	UNKNOWN	Multi-center Clinical Study of Early Antibios of Severe Acute Pancreatitis
NCT02757703	PHASE4	COMPLETED	Vasoactive Drugs in Real World Practice
NCT03349424	PHASE4	COMPLETED	Somatostatin Prevent Post-operation Pancreatic Fistula in Intermediate Risk Patients After Pancreaticoduodenectomy
NCT03998293	PHASE4	WITHDRAWN	Direct Measurement of Proinsulin Clearance in Humans
NCT03998709	PHASE4	WITHDRAWN	Effect of Fasting Free Fatty Acids and Fasting Glucose on 1st and 2nd Phase Insulin Secretion
NCT04107428	PHASE4	UNKNOWN	Somatostatin in Living Donor Liver Transplantation
NCT04358016	PHASE4	COMPLETED	Terlipression Prevent Developing of Acute Kidney Injury During Upper-gastroentestinal Bleeding
NCT06855095	PHASE2/PHASE3	RECRUITING	Absorbed Tumor Dose in Peptide Receptor Radionuclide Therapy with Long-acting Somatostatin Analogues - ATSA Trial
NCT00309283	PHASE3	COMPLETED	Somatostatin in Polycystic Kidney: a Long-term Three Year Follow up Study
NCT00386984	PHASE3	COMPLETED	Hector-Study to Evaluate the Efficacy of Octreotide in Patients With Inoperable Hepatocellular Carcinoma
NCT01053390	PHASE3	COMPLETED	New Chemotherapy Regimen in the Treatment of Advanced Gallbladder Carcinoma
NCT01060826	PHASE3	UNKNOWN	Efficacy of Administration of Somatostatin in the Prevention of Post-endoscopic Retrograde Cholangiopancreatography (ERCP) Pancreatitis
NCT02799212	PHASE3	COMPLETED	Evaluation of Postoperative Ascites After Somatostatin Infusion Following Hepatectomy for Hepatocellular Carcinoma
NCT02882347	PHASE3	UNKNOWN	The Effect of Somatostatin for Treatment of Post Hepatectomy Liver Failure (PHLF)
NCT03000946	PHASE3	COMPLETED	Prevention of Postoperative Pancreatic Fistula by Somatostatin
NCT04010669	PHASE3	UNKNOWN	The Role of Somatostatin in the Hemodynamics of the Hepatic Circulation in Patients Undergoing Liver Resection
NCT04329039	PHASE2/PHASE3	SUSPENDED	Somatostatin Analogues With Perioperative Antibiotics Versus Prolonged Antibiotics
NCT00786825	PHASE2	COMPLETED	Measurement of Glucose/Glycogen Metabolism in Humans Using Magnetic Resonance at 4 or 7 Tesla
NCT02795858	PHASE2	COMPLETED	A Phase II Study of Ramucirumab With Somatostatin Analog Therapy in Patients With Advanced, Progressive Carcinoid Tumors
NCT03241706	PHASE1	ACTIVE_NOT_RECRUITING	Liver Glycogen and Hypoglycemia in Humans
NCT01290172	PHASE1	COMPLETED	Evaluation of Efficacy and Safety of Somatostatin Used as Inflow Modulator in Liver Transplantation.
NCT01665638	PHASE1	COMPLETED	Effects of Canagliflozin on C-peptide Clearance in Healthy Volunteers
NCT02026973	PHASE1	COMPLETED	Impact of Endogenous E2 on SSI and GH Rebound
NCT02631616	PHASE1	UNKNOWN	Treatment With Sandostatin in Patients With Castrate Resistance Prostate Cancer Showing Uptake of 68Ga-DOTATET
NCT02748369	PHASE1	COMPLETED	In Vivo Assessment of Cellular Metabolism in Humans
NCT06416969	EARLY_PHASE1	RECRUITING	Regional Lipolysis and Adipocyte Lipolysis Protein Stimulation
NCT07252401	Not specified	NOT_YET_RECRUITING	Terlipressin vs. Somatostatin in Cirrhotic Patients With Acute Gastrointestinal Bleeding and Acute Kidney Injury
NCT07304466	Not specified	RECRUITING	Effects of Terlipressin and Somatostatin on Portal Pressure in Patients Undergoing Living Donor Liver Transplantation
NCT07366710	Not specified	ACTIVE_NOT_RECRUITING	Measuring Amino Acid and Glucose Metabolism in Healthy Volunteers and NAFLD Patients Using Total-body PET
NCT07534371	Not specified	ACTIVE_NOT_RECRUITING	Analysis of Optimal Treatment Sequencing of Surufatinib and Somatostatin Analogs in Neuroendocrine Tumors: A Retrospective Cohort Study
NCT07605611	Not specified	RECRUITING	Somatostatin Plus Clear Liquid Diet Versus Diverting Stoma in Patients With Rectal Cancer Undergoing Ultra-Low Anterior Resection
NCT00431665	Not specified	COMPLETED	Effect of Elevated Plasma-Free-Fatty-Acids on Renal Hemodynamic Parameters
NCT00793741	Not specified	COMPLETED	Measurement of Glucose Metabolism in Humans Using Magnetic Resonance at 4 Tesla. Substudy: Hypoglycemia Unawareness
NCT01062529	Not specified	COMPLETED	Peripheral Metabolic Effects of Somatostatin
NCT01267669	Not specified	COMPLETED	A Trial of Somatostatin With Endoscopic Variceal Ligation (EVL) in Control of Acute Variceal Bleeding
NCT01426087	Not specified	UNKNOWN	Effects of Somatostatin on Post-endoscopic Portal Hemodynamic in Cirrhotic Patients With Esophageal Gastric Varices

Clinical evidence (CIViC)

No CIViC predictive evidence (expected for non-precision-medicine drugs).

Pharmacology

Pharmacogenomics

No PharmGKB pharmacogenomic data curated for this drug.

Related molecules

Related molecules

Molecules sharing ≥1 of this drug’s curated primary targets, merged from two biobtree sources and ranked by shared-target count, then clinical phase: ChEMBL clinical-stage candidates (development phase ≥2) and PubChem drug-class bioactivity (approved / known drugs acting on the target). Deduplicated by drug name; the drug’s own salt forms are excluded. Note: for a drug with few primary targets a shared-target match can reflect off-target / promiscuous binding rather than the same therapeutic mechanism — the phase ordering surfaces bona-fide therapeutics first.

40 molecules share ≥1 primary target. Top 40 by shared-target count:

Molecule	Source	Status	Shared targets
VAPREOTIDE	ChEMBL	Phase 3	SSTR1, SSTR2, SSTR3, SSTR4, SSTR5
oxodotreotide	PubChem	Approved	SSTR1, SSTR2, SSTR3, SSTR4, SSTR5
Octreotide	ChEMBL + PubChem	Phase 4 (approved)	MRGPRX2, SSTR2, SSTR4, SSTR5
LANREOTIDE	ChEMBL	Phase 4 (approved)	SSTR1, SSTR2, SSTR3, SSTR5
PASIREOTIDE	ChEMBL	Phase 4 (approved)	SSTR1, SSTR2, SSTR3, SSTR5
SEGLITIDE	ChEMBL	Phase 2	SSTR2, SSTR3, SSTR4, SSTR5
GALLIUM OXODOTREOTIDE	ChEMBL	Phase 4 (approved)	SSTR2, SSTR4, SSTR5
EDOTREOTIDE	ChEMBL	Phase 3	SSTR2, SSTR3, SSTR5
EDOTREOTIDE YTTRIUM	ChEMBL	Phase 2	SSTR2, SSTR3, SSTR5
PALTUSOTINE	ChEMBL	Phase 3	SSTR2, SSTR4
CETRORELIX	ChEMBL + PubChem	Phase 4 (approved)	MRGPRX2
CODEINE	ChEMBL + PubChem	Phase 4 (approved)	MRGPRX2
DEXTROMETHORPHAN	ChEMBL + PubChem	Phase 4 (approved)	MRGPRX2
HYDROCODONE	ChEMBL + PubChem	Phase 4 (approved)	MRGPRX2
ICATIBANT	ChEMBL + PubChem	Phase 4 (approved)	MRGPRX2
LEVORPHANOL	ChEMBL + PubChem	Phase 4 (approved)	MRGPRX2
LOPERAMIDE	ChEMBL + PubChem	Phase 4 (approved)	SSTR5
METHADONE	ChEMBL + PubChem	Phase 4 (approved)	MRGPRX2
MORPHINE	ChEMBL + PubChem	Phase 4 (approved)	MRGPRX2
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	SSTR5
LEVOPROPOXYPHENE	ChEMBL	Phase 4 (approved)	MRGPRX2
SINOMENINE	ChEMBL	Phase 3	MRGPRX2
ADL-5859	ChEMBL	Phase 2	MRGPRX2
DEXTRORPHAN	ChEMBL	Phase 2	MRGPRX2
MK-8189	ChEMBL	Phase 2	SSTR2
MORPHINE GLUCURONIDE	ChEMBL	Phase 2	MRGPRX2
NORCODEINE	ChEMBL	Phase 2	MRGPRX2
Atracurium	PubChem	Approved	MRGPRX2
Belzutifan	PubChem	Approved	SSTR4
Ciprofloxacin	PubChem	Approved	MRGPRX2
Fentanyl	PubChem	Approved	MRGPRX2
Leuprolide	PubChem	Approved	MRGPRX2
Levofloxacin	PubChem	Approved	MRGPRX2
Meperidine	PubChem	Approved	MRGPRX2
Moxifloxacin	PubChem	Approved	MRGPRX2
Naloxone	PubChem	Approved	MRGPRX2
Naltrexone	PubChem	Approved	MRGPRX2
Ofloxacin	PubChem	Approved	MRGPRX2
Propoxyphene	PubChem	Approved	MRGPRX2
Rocuronium	PubChem	Approved	MRGPRX2