Octreotide

Summary

Octreotide (CHEMBL1680) is an approved protein (ATC H01CB02) targeting SSTR2, SSTR3, and SSTR5; indicated across 26 conditions including carcinoid syndrome and carcinoid tumor.

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: H01CB02
• Targets: 3 (SSTR2, SSTR3, SSTR5)
• Indications: 26 conditions
• Clinical trials: 104
• Chemistry: 1019.2 Da · C49H66N10O10S2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL1680
Name	Octreotide
Type	Protein
Max phase	4
FDA approved	yes
PubChem CID	448601
ATC	H01CB02
Molecular formula	C49H66N10O10S2
Molecular weight	1019.2
InChIKey	DEQANNDTNATYII-OULOTJBUSA-N

SMILES: C[C@H]([C@H]1C(=O)N[C@@H](CSSC[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)NC(=O)[C@@H](CC5=CC=CC=C5)N)C(=O)N[C@H](CO)[C@@H](C)O)O

IUPAC name: (4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-19-[[(2R)-2-amino-3-phenylpropanoyl]amino]-16-benzyl-N-[(2R,3R)-1,3-dihydroxybutan-2-yl]-7-[(1R)-1-hydroxyethyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide

Also known as: Octreotida, Octreotide, SMS-995, SMS995, OCTREOTIDE

Parent form; salt/anhydrous children: CHEMBL1200480, CHEMBL2105834, CHEMBL3545066

Patent coverage: 738 distinct patent families (999 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 682 (68%) 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
SSTR2	SST2 receptor	Full agonist	9.9	0.7%	P30874
SSTR3	SST3 receptor	Full agonist	8.6	0.2%	P32745
SSTR5	SST5 receptor	Full agonist	9.5	0%	P35346

Broader ChEMBL bioactivity targets: 3 (assay-derived). Sample: Somatostatin receptor type 5, Somatostatin receptor type 2, Somatostatin receptor type 4.

Bioactivity

ChEMBL activities: 4 potent at pChembl ≥ 5 of 4 total. Top 100 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SSTR2	10.52	EC50	0.03	nM	CHEMBL_ACT_23298623
SSTR2	9.4	Ki	0.4	nM	CHEMBL_ACT_19104069
SSTR5	7.66	IC50	22	nM	CHEMBL_ACT_18948297
SSTR4	7.18	Ki	66	nM	CHEMBL_ACT_19104070

Target pathways

Aggregated over 3 target gene(s): SSTR2, SSTR3, SSTR5.

Top Reactome pathways

11 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	3	SSTR2, SSTR3, SSTR5
Signaling by GPCR	3	SSTR2, SSTR3, SSTR5
Class A/1 (Rhodopsin-like receptors)	3	SSTR2, SSTR3, SSTR5
Peptide ligand-binding receptors	3	SSTR2, SSTR3, SSTR5
GPCR downstream signalling	3	SSTR2, SSTR3, SSTR5
G alpha (i) signalling events	3	SSTR2, SSTR3, SSTR5
GPCR ligand binding	3	SSTR2, SSTR3, 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, coupled to cyclic nucleotide second messenger	3
neuropeptide signaling pathway	3
negative regulation of cell population proliferation	3
signal transduction	3
G protein-coupled receptor signaling pathway	3
somatostatin signaling pathway	3
cellular response to glucocorticoid stimulus	2
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	1
cellular response to estradiol stimulus	1
cell-cell signaling	1
hormone-mediated apoptotic signaling pathway	1
positive regulation of cytokinesis	1
glucose homeostasis	1
regulation of insulin secretion	1

Indications & clinical

Indications

21 diseases in clinical trials (phase 1–3, investigational — not approved indications). Highest ChEMBL trial phase per disease; a non-cancer approved use is occasionally logged at phase 3 here.

Disease (in trials)	Phase	MONDO	EFO
carcinoid syndrome	3	MONDO:0100347	EFO:1000852
carcinoid tumor	3	MONDO:0005369	EFO:0004243
diarrheal disease	3	MONDO:0001673	HP:0002014
hepatocellular carcinoma	3	MONDO:0007256	EFO:0000182
acromegaly	3	MONDO:0019933	EFO:1001485
exocrine pancreatic carcinoma	3	MONDO:0005192	EFO:0002618
autosomal dominant polycystic kidney disease	3	MONDO:0004691	EFO:1001496
neuroendocrine neoplasm	3	MONDO:0019496	EFO:1001901
pancreatic neuroendocrine tumor	3	MONDO:0019954	EFO:1000045
thymoma	2	MONDO:0006456	EFO:1000581
neoplasm	2	MONDO:0005070	EFO:0000616
pancreatic neuroendocrine neoplasm	2	MONDO:0005815	EFO:0007331
neuroendocrine carcinoma	2	MONDO:0002120	MONDO:0002120
intestinal obstruction	2	MONDO:0004565	MONDO:0004565
meningioma	2	MONDO:0016642	MONDO:0016642
hereditary hemorrhagic telangiectasia	2	MONDO:0019180	MONDO:0019180
idiopathic pulmonary fibrosis	1	MONDO:0800504	EFO:0000768
obesity disorder	1	MONDO:0011122	EFO:0001073
orthostatic hypotension	1	MONDO:0005469	EFO:0005252
irritable bowel syndrome	1	MONDO:0005052	EFO:0000555
migraine disorder	1	MONDO:0005277	MONDO:0005277

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

Clinical trials

Total trials: 104.

Phase distribution

Phase	Trials
PHASE2	22
Not specified	22
PHASE3	21
PHASE4	18
PHASE1	13
PHASE1/PHASE2	4
PHASE2/PHASE3	2
EARLY_PHASE1	2

Top trials by phase / activity

NCT	Phase	Status	Title
NCT06974344	PHASE4	NOT_YET_RECRUITING	Octreotide vs. Splenic Artery Ligation for Portal Flow Modulation in Living Donor Liver Transplants (SCALOP Trial)
NCT00171613	PHASE4	COMPLETED	A Study of Octreotide Depot vs Saline Control in Pediatric Hypothalamic Obesity Patients
NCT00171886	PHASE4	COMPLETED	Octreotide Efficacy and Safety in First-line Acromegalic Patients
NCT00376064	PHASE4	COMPLETED	Efficacy of Octreotide Acetate and Cabergoline in Patients With Acromegaly
NCT00521300	PHASE4	COMPLETED	Preoperative Octreotide Treatment of Acromegaly
NCT00534677	PHASE4	COMPLETED	The Safety & Efficacy of Terlipressin vs Octreotide for the Control of Variceal Bleed
NCT00966355	PHASE4	COMPLETED	Comparison of Terlipressin, Somatostatin, and Octreotide for Control of Variceal Bleeding
NCT01301222	PHASE4	COMPLETED	Role of Octreotide in Preventing Pancreatic Fistula After Pancreaticoduodenectomy (PD) in Patients With Soft Pancreas
NCT01917773	PHASE4	COMPLETED	Effect of Octreotide on the Colonic Motility in Pediatric Patients
NCT02032784	PHASE4	TERMINATED	Prophylactic Octreotide to Prevent Post Duodenal EMR and Ampullectomy Bleeding
NCT02119884	PHASE4	COMPLETED	Hemodynamic Effects of Terlipressin and High Dose Octreotide
NCT03289741	PHASE4	COMPLETED	A Study to Evaluate Patient Experience in the Therapy of Neuroendocrine Tumors Treated With Octreotide Long Acting Release Versus Lanreotide
NCT03455322	PHASE4	COMPLETED	Norepinephrine Infusion Versus Midodrine & Octreotide in Patients With Hepatorenal Syndrome Type 1.
NCT03624517	PHASE4	TERMINATED	Comparison of 24-hours Versus 72-hours of Octreotide Infusion in Preventing Early Rebleed From Esophageal Varices
NCT04028323	PHASE4	UNKNOWN	Functional MRI-based Assessment of Terlipressin vs. Octreotide on Renal Function in Cirrhotic Patients With Acute Variceal Bleeding (CHESS1903)
NCT04353193	PHASE4	UNKNOWN	Hemodynamic Profile of Terlipressin and Octreotide in Patients With Cirrhosis and Portal Hypertension. A Randomised, Single Blinded Clinical Trial.
NCT05199038	PHASE4	UNKNOWN	Comparison of 2 Days Versus 5 Days of Octreotide After Endoscopic Therapy in Preventing Early Esophageal Varices Rebleed : A Randomized Controlled Study
NCT05682209	PHASE4	COMPLETED	The Effect of Octreotide on Wound Drainage After Mastectomy
NCT05477576	PHASE3	RECRUITING	Study of RYZ101 Compared With SOC in Pts w Inoperable SSTR+ Well-differentiated GEP-NET That Has Progressed Following 177Lu-SSA Therapy
NCT05884255	PHASE3	RECRUITING	An Open-label Phase 3 Study of Lutetium (177Lu) Oxodotreotide Injection in Subjects With Advanced Gastrointestinal Pancreatic Neuroendocrine Tumors.
NCT07479784	PHASE3	NOT_YET_RECRUITING	Octreotide Microspheres for Preventing Pancreatic Fistula
NCT00130845	PHASE3	COMPLETED	Octreotide Acetate in Microspheres in Patients With Diabetic Retinopathy
NCT00131144	PHASE3	COMPLETED	Octreotide Acetate in Microspheres in Patients With Diabetic Retinopathy
NCT00240045	PHASE2/PHASE3	COMPLETED	The Use of Drugs to Improve Kidney Function in Patients With Liver and Kidney Dysfunction
NCT00241020	PHASE3	COMPLETED	Evaluation of the Efficacy of Long-acting Release Octreotide in Patients With Advanced Hepatocellular Carcinoma
NCT00248131	PHASE3	TERMINATED	Extension Study of Long-term Safety and Tolerability of Octreotide Acetate in Patients With Moderately Severe or Severe Non-proliferative Diabetic Retinopathy or Low Risk Proliferative Diabetic Retinopathy
NCT00248157	PHASE3	TERMINATED	Extension Study of the Long-term Safety and Tolerability of Octreotide Acetate in Patients With Moderately Severe or Severe Non-proliferative Diabetic Retinopathy or Low Risk Proliferative Diabetic Retinopathy
NCT00412061	PHASE3	COMPLETED	Everolimus and Octreotide in Patients With Advanced Carcinoid Tumor
NCT00426153	PHASE2/PHASE3	COMPLETED	Octreotide in Severe Polycystic Liver Disease
NCT00600886	PHASE3	COMPLETED	Safety and Efficacy of Pasireotide Long Acting Release (LAR) vs. Octreotide LAR in Patients With Active Acromegaly
NCT00616551	PHASE3	COMPLETED	Efficacy and Safety of C2L-OCT-01 PR in Acromegalic Patients
NCT00690430	PHASE3	COMPLETED	Efficacy and Safety of Pasireotide Long Acting Release vs. Octreotide Long Acting Release in Patients With Metastatic Carcinoid Disease
NCT00765323	PHASE3	TERMINATED	Efficacy and Safety Study of Octreotide Implant in Patients With Acromegaly
NCT00804297	PHASE3	COMPLETED	Octreotide for the Treatment of Sulfonylurea-Associated Hypoglycemia
NCT01295060	PHASE3	TERMINATED	Long-term Safety and Efficacy Study of Octreotide Implant in Patients With Acromegaly
NCT01412424	PHASE3	COMPLETED	Efficacy and Safety of Octreotide (MYCAPSSA™ [Formerly Octreolin™]) for Acromegaly
NCT02384122	PHASE3	COMPLETED	Efficacy of Octreotide on Blood and Iron Requirements in Patients With Anemia Due to Angiodysplasias
NCT02457156	PHASE3	COMPLETED	Cattell-Warren Versus Blumgart Techniques of Pancreatico-jejunostomy Following Pancreato-duodenectomy
NCT02685709	PHASE3	COMPLETED	Comparison of Oral Octreotide Capsules to Injectable Somatostatin Analogs in Acromegaly
NCT03000946	PHASE3	COMPLETED	Prevention of Postoperative Pancreatic Fistula by Somatostatin
NCT03252353	PHASE3	UNKNOWN	Efficacy and Safety of Octreotide Capsules (MYCAPSSA) in Acromegaly
NCT00262470	PHASE1/PHASE2	ACTIVE_NOT_RECRUITING	Treatment of Orthostatic Intolerance
NCT00004327	PHASE2	COMPLETED	Phase II Pilot Study of Octreotide, a Somatostatin Octapeptide Analog, for Gastrointestinal Hemorrhage in Hormone-Refractory Hereditary Hemorrhagic Telangiectasia and Senile Ectasia
NCT00005906	PHASE2	COMPLETED	Treatment With Octreotide in Patients With Lymphangioleiomyomatosis
NCT00113360	PHASE2	COMPLETED	RAD001 Plus Octreotide Depot in Metastatic or Unresectable Low Grade Neuroendocrine Carcinoma
NCT00250796	PHASE2	COMPLETED	Trial of Thalidomide, a- Interferon +/- Octreotide in Patients With Unresectable Hepatocellular Carcinoma
NCT00274170	PHASE1/PHASE2	UNKNOWN	Randomized Evaluation of Octreotide Versus Compazine for Emergency Department Treatment of Migraine Headache
NCT00332969	PHASE2	COMPLETED	Efficacy of Octreotide Treatment in Patients With Primary Inoperable Thymoma
NCT00363051	PHASE2	COMPLETED	Safety/Efficacy of Everolimus in Adults With Advanced Pancreatic Neuroendocrine Cancer Not Responsive to Chemotherapy
NCT00427349	PHASE2	COMPLETED	AMG 706 and Octreotide in Treating Patients With Low-Grade Neuroendocrine Tumors
NCT00463983	PHASE1/PHASE2	COMPLETED	Treatment of Idiopathic Pulmonary Fibrosis With Long Acting Octreotide
NCT00781911	PHASE2	COMPLETED	A Study of Cixutumumab (IMC-A12) in Islet Cell Cancer
NCT00884715	PHASE1/PHASE2	TERMINATED	Pharmacokinetics, Efficacy and Safety of an Octreotide Implant in Patients With Carcinoid Syndrome
NCT01587222	PHASE2	WITHDRAWN	Midodrine, Octreotide and Albumin: Impact on Renal Function of Patients With Liver Cirrhosis and Renal Failure
NCT02111044	PHASE2	COMPLETED	Phase II Study With ITF2984 in Acromegalic Patients
NCT02217800	PHASE2	COMPLETED	The Effect of Subcutaneous Infusions of 3 Doses of DG3173 on Growth Hormone Levels in Untreated Acromegalics
NCT02235987	PHASE2	COMPLETED	Single Dose Pharmacology Study of DG3173 and Octreotide in Acromegalic Patients.
NCT02294786	PHASE2	TERMINATED	Study of Prophylactic Octreotide to Prevent or Reduce the Frequency and Severity of Diarrhoea in Subjects Receiving Lapatinib With Capecitabine for the Treatment of Metastatic Breast Cancer
NCT02333565	PHASE2	COMPLETED	Combination of Everolimus and Octreotide LAR in Aggressive Recurrent Meningiomas
NCT02437825	PHASE2	UNKNOWN	Octreotide VS Placebo in Prevention of Salivary Fistulae After Post Radiation Salvage Surgery
NCT02916433	PHASE2	COMPLETED	Octreotide for Management of Bronchorrhea in Mechanically Ventilated Patients
NCT03179995	PHASE2	TERMINATED	Trial Using Octreotide to Enhance Liver Recovery After Hepatectomy
NCT04027348	PHASE2	TERMINATED	Palliative Management of Inoperable Malignant Bowel Obstruction
NCT04048707	PHASE2	WITHDRAWN	Angiotensin 2 for Hepatorenal Syndrome
NCT04871204	PHASE2	COMPLETED	Octreotide Treatment to Improve Nutritional Recovery After Surgery for Patients with Esophageal or Gastric Cancer
NCT06085976	PHASE2	UNKNOWN	Efficacy and Safety of Octreotide in Laparoscopic Hepatectomy Surgery: Effect on Blood Loss, Need for Vasoactive Drugs, Transfusion Requirements.
NCT06865677	PHASE2	TERMINATED	Sacituzumab Govitecan for Relapsed Ovarian, Endometrial, and Cervical Carcinomas
NCT06592261	PHASE1	RECRUITING	Graded Insulin Suppression Test P&F
NCT06881888	PHASE1	NOT_YET_RECRUITING	Intranasal Delivery of Octreotide for Treatment of Diabetic Macular Edema
NCT00223691	PHASE1	COMPLETED	Treatment of Orthostatic Hypotension in Autonomic Failure
NCT00584298	PHASE1	COMPLETED	Feasibility and Reproducibility of Barostat Assessments of Colorectal Sensation During Colorectal Distention and Its Pharmacological Modulation Using Octreotide
NCT01086982	PHASE1	SUSPENDED	Pharmacodynamics Of Product Octreotide Acetate Lar 30 Mg Compared To Product Sandostatin LAR ®
NCT01561066	PHASE1	COMPLETED	Autologous Fibrin Glues for Fistulas Closure
NCT01871844	PHASE1	COMPLETED	ITF2984 Repeated Doses Study in Healthy Volunteers
NCT02217826	PHASE1	COMPLETED	Single Dose Pharmacodynamic and Pharmacokinetic Study of DG3173
NCT02217839	PHASE1	COMPLETED	Multiple Ascending Dose Tolerability, Pharmacokinetic and Pharmacodynamic Study of DG3173
NCT02237053	PHASE1	COMPLETED	Effects of Glucagon Administration on Energy Expenditure
NCT03571594	PHASE1	TERMINATED	A Four-Part Study to Assess the Safety, Tolerability, PK and PD of ONO-5788 in Healthy Adult Volunteers
NCT05340192	PHASE1	COMPLETED	Effect of Octreotide on Saliva
NCT05761431	PHASE1	COMPLETED	A Single-dose Study of Octreotide Injection in Healthy Adult Subjects
NCT03520569	EARLY_PHASE1	COMPLETED	Effect of Hyperglycemia on Microvascular Perfusion in Healthy Adults
NCT05683444	EARLY_PHASE1	COMPLETED	Octreotide Improves Human Lymphatic Fluid Transport a Translational Trial
NCT06193616	Not specified	ACTIVE_NOT_RECRUITING	Outcome of ADPKD With Octreotide LAR
NCT06300216	Not specified	NOT_YET_RECRUITING	A Real-world Study of Octreotide Microspheres in Chinese Patients With Neuroendocrine Tumors
NCT07583563	Not specified	NOT_YET_RECRUITING	An Observational Study of Octreotide Subcutaneous Depot in Patients With Acromegaly
NCT00002252	Not specified	COMPLETED	A Multicenter Placebo-Controlled Dose Titration Study to Evaluate the Efficacy and Safety of Sandostatin (SMS 201-995) in the Treatment of Patients With Acquired Immunodeficiency Related Diarrhea
NCT00002253	Not specified	COMPLETED	A Multicenter Placebo-Controlled Double Blind Study to Evaluate the Efficacy and Safety of Sandostatin ( SMS 201-995 ) in Patients With Acquired Immunodeficiency Related Diarrhea Who Were Either Responders or Non-Responders in a Prior Placebo-Controlled Double-Blind Sandostatin Study.
NCT00399893	Not specified	TERMINATED	Octreotide Therapy in Children and Young Adults With Prader-Willi Syndrome (PWS)
NCT01613495	Not specified	UNKNOWN	Ghrelin Suppression by Octreotide in Prader-Willi
NCT01865760	Not specified	COMPLETED	Etiology, Assessment and Treatment of Post-gastric Bypass Severe Hypoglycemia
NCT02010385	Not specified	COMPLETED	Investigation of the Effects of Obesity Surgery on Appetitive Behaviour
NCT02305069	Not specified	COMPLETED	Effect of Obesity-derived Cytokines on Protein Turnover and Carbohydrate Metabolism in Human Skeletal Muscle
NCT02311608	Not specified	UNKNOWN	Effects of Terlipressin When Usual Somatostatin or Octreotide Dose Fails
NCT02381249	Not specified	COMPLETED	The Effect of Satiety Gut Hormone Modulation on Appetitive Drive After Upper Gastrointestinal Surgery
NCT02385617	Not specified	COMPLETED	Food Intake and Gut Hormones in Patients Who Have Undergone Upper Gastrointestinal Surgery for Cancer
NCT02474914	Not specified	COMPLETED	Octreotide in the Prevention of Postoperative Complications After Pancreaticoduodenectomy
NCT02920567	Not specified	UNKNOWN	Impact of Prophylactic Octreotide to Pancreatic Exocrine Secretion
NCT03061604	Not specified	COMPLETED	RCT to Determine the Efficacy of Combining Hemospray With Medical Treatment in Acute Variceal Bleeding
NCT03812939	Not specified	UNKNOWN	Recurrence Rates of Type I Gastric Neuroendocrine Tumors Treated With Long-acting Somatostatin Analogs
NCT03846180	Not specified	COMPLETED	Terlipressin on Effect of Renal Function in Cirrhotic Patients With Acute Gastrointestinal Hemorrhage

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.

13 molecules share ≥1 primary target. Top 13 by shared-target count:

Molecule	Source	Status	Shared targets
LANREOTIDE	ChEMBL	Phase 4 (approved)	SSTR2, SSTR3, SSTR5
PASIREOTIDE	ChEMBL	Phase 4 (approved)	SSTR2, SSTR3, SSTR5
EDOTREOTIDE	ChEMBL	Phase 3	SSTR2, SSTR3, SSTR5
SOMATOSTATIN	ChEMBL	Phase 3	SSTR2, SSTR3, SSTR5
VAPREOTIDE	ChEMBL	Phase 3	SSTR2, SSTR3, SSTR5
EDOTREOTIDE YTTRIUM	ChEMBL	Phase 2	SSTR2, SSTR3, SSTR5
SEGLITIDE	ChEMBL	Phase 2	SSTR2, SSTR3, SSTR5
oxodotreotide	PubChem	Approved	SSTR2, SSTR3, SSTR5
GALLIUM OXODOTREOTIDE	ChEMBL	Phase 4 (approved)	SSTR2, SSTR5
LOPERAMIDE	ChEMBL + PubChem	Phase 4 (approved)	SSTR5
ASTEMIZOLE	ChEMBL	Phase 4 (approved)	SSTR5
PALTUSOTINE	ChEMBL	Phase 3	SSTR2
MK-8189	ChEMBL	Phase 2	SSTR2