Lanreotide
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Also known as AngiopeptinLanreotidaSomatuline autogelSomatuline la
Summary
Lanreotide (CHEMBL1201185) is an approved protein (ATC H01CB03) targeting SSTR2, SSTR3, and SSTR5; indicated across 23 conditions including neoplasm and acromegaly.
At a glance
- Status: Approved (max clinical phase 4)
- Modality: Protein
- ATC class: H01CB03
- Targets: 3 (SSTR2, SSTR3, SSTR5)
- Indications: 23 conditions
- Clinical trials: 33
- Chemistry: 1096.3 Da · C54H69N11O10S2
Identifiers
Drug identity and classification
| Field | Value |
|---|---|
| ChEMBL ID | CHEMBL1201185 |
| Name | Lanreotide |
| Type | Protein |
| Max phase | 4 |
| FDA approved | yes |
| PubChem CID | 6918011 |
| ATC | H01CB03 |
| Molecular formula | C54H69N11O10S2 |
| Molecular weight | 1096.3 |
| InChIKey | PUDHBTGHUJUUFI-SCTWWAJVSA-N |
SMILES: C[C@H]([C@@H](C(=O)N)NC(=O)[C@@H]1CSSC[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)C(C)C)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=C(C=C4)O)NC(=O)[C@@H](CC5=CC6=CC=CC=C6C=C5)N)O
IUPAC name: (4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-N-[(2S,3R)-1-amino-3-hydroxy-1-oxobutan-2-yl]-19-[[(2R)-2-amino-3-naphthalen-2-ylpropanoyl]amino]-16-[(4-hydroxyphenyl)methyl]-13-(1H-indol-3-ylmethyl)-6,9,12,15,18-pentaoxo-7-propan-2-yl-1,2-dithia-5,8,11,14,17-pentazacycloicosane-4-carboxamide
Also known as: Angiopeptin, Lanreotida, Lanreotide, Somatuline autogel, Somatuline la, lanreotide, LANREOTIDE
Parent form; salt/anhydrous children: CHEMBL1201184
Patent coverage: 102 distinct patent families (177 SureChEMBL compound mentions), from 3 matched compound structure(s). One matched structure accounts for 119 (67%) 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 | 9.6 | 0.7% | P30874 |
| SSTR3 | SST3 receptor | Full agonist | 8 | 0.2% | P32745 |
| SSTR5 | SST5 receptor | Full agonist | 9.3 | 0% | P35346 |
Broader ChEMBL bioactivity targets: 4 (assay-derived). Sample: Somatostatin receptor type 5, Somatostatin receptor type 2, Somatostatin receptor type 1, Somatostatin receptor type 3.
Bioactivity
ChEMBL activities: 4 potent at pChembl ≥ 5 of 4 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):
| Target | pChembl | Type | Value | Unit | Activity ID |
|---|---|---|---|---|---|
| SSTR2 | 9.3 | Ki | 0.5 | nM | CHEMBL_ACT_515409 |
| SSTR5 | 8.4 | Ki | 3.98 | nM | CHEMBL_ACT_515412 |
| SSTR3 | 7.2 | Ki | 63.1 | nM | CHEMBL_ACT_515410 |
| SSTR1 | 6.3 | Ki | 501.2 | nM | CHEMBL_ACT_515408 |
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
23 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 |
|---|---|---|---|
| neoplasm | 3 | MONDO:0005070 | EFO:0000616 |
| acromegaly | 3 | MONDO:0019933 | EFO:1001485 |
| carcinoid syndrome | 3 | MONDO:0100347 | EFO:1000852 |
| carcinoid tumor | 3 | MONDO:0005369 | EFO:0004243 |
| endocrine gland neoplasm | 3 | MONDO:0002082 | EFO:0003769 |
| autosomal dominant polycystic kidney disease | 3 | MONDO:0004691 | EFO:1001496 |
| carcinoid heart disease | 3 | MONDO:0043529 | EFO:1001769 |
| rectal neoplasm | 3 | MONDO:0002165 | MONDO:0044937 |
| pituitary gland adenoma | 3 | MONDO:0006373 | EFO:1000478 |
| peptic esophagitis | 2 | MONDO:0006896 | EFO:1001095 |
| diarrheal disease | 2 | MONDO:0001673 | HP:0002014 |
| cutaneous neuroendocrine carcinoma | 2 | MONDO:0019210 | EFO:1001471 |
| hepatocellular carcinoma | 2 | MONDO:0007256 | EFO:0000182 |
| dumping syndrome | 2 | MONDO:0001979 | EFO:1001307 |
| hyperglycemia | 2 | MONDO:0002909 | HP:0003074 |
| intestinal disorder | 2 | MONDO:0005020 | EFO:0009431 |
| neuroendocrine neoplasm | 2 | MONDO:0019496 | EFO:1001901 |
| intestinal obstruction | 2 | MONDO:0004565 | MONDO:0004565 |
| adrenal gland pheochromocytoma | 2 | MONDO:0004974 | EFO:0000239 |
| paraganglioma | 2 | MONDO:0000448 | EFO:1000453 |
3 further indication records had no mapped disease name (EFO/MeSH-only) or were duplicates, and are omitted.
Clinical trials
Total trials: 33.
Phase distribution
| Phase | Trials |
|---|---|
| PHASE3 | 10 |
| PHASE2 | 9 |
| Not specified | 5 |
| PHASE4 | 3 |
| PHASE2/PHASE3 | 3 |
| PHASE1/PHASE2 | 2 |
| EARLY_PHASE1 | 1 |
Top trials by phase / activity
| NCT | Phase | Status | Title |
|---|---|---|---|
| NCT01070758 | PHASE4 | COMPLETED | Lanreotide Autogel Treatment of Patients With Congenital Hyperinsulinism of Infancy |
| NCT01861717 | PHASE4 | TERMINATED | A Pilot Study of Pre- and Post-operative Use of Somatuline Depot. |
| NCT03083210 | PHASE4 | UNKNOWN | Study of Lanreotide in Metastatic or Recurrent Grade I-II Hindgut NET |
| 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 |
| NCT06807437 | PHASE3 | RECRUITING | Lanreotide Versus Placebo Before Surgery to Prevent a Surgical Complication Called a Pancreatic Fistula |
| NCT00565097 | PHASE2/PHASE3 | COMPLETED | Lanreotide as Treatment of Polycystic Livers |
| NCT00630695 | PHASE3 | COMPLETED | Prevention of Lymphorrhea by Lanreotide in Axillary Dissection for Breast Cancer |
| NCT00729313 | PHASE3 | COMPLETED | Efficacy and Safety of Lanreotide Versus Placebo for Treatment of Patients With Digestive Fistulae |
| NCT00771888 | PHASE2/PHASE3 | UNKNOWN | Open-Label Extension of LOCKCYST Trial |
| NCT00774930 | PHASE3 | COMPLETED | An Efficacy and Safety Study of Somatuline Depot (Lanreotide) Injection to Treat Carcinoid Syndrome |
| NCT01616927 | PHASE3 | UNKNOWN | Study of Lanreotide to Treat Polycystic Kidney Disease |
| NCT02127437 | PHASE3 | COMPLETED | Lanreotide In Polycystic Kidney Disease Study |
| NCT02288377 | PHASE2/PHASE3 | TERMINATED | A Study Evaluating Lanreotide as Maintenance Therapy in Patients With Non-Resectable Duodeno-Pancreatic Neuroendocrine Tumors (REMINET) |
| NCT02493517 | PHASE3 | COMPLETED | Efficacy and Safety of Lanreotide Autogel® 60, 90 or 120 mg With Lanreotide 40 mg Prolonged Release (PR) in Acromegaly |
| NCT04065165 | PHASE3 | WITHDRAWN | Lanreotide Combined With Telotristat Ethyl or Placebo for the First-line Treatment in Patients With Advanced Well Differentiated Small Intestinal Neuroendocrine Tumours (siNET) With Highly-functioning Carcinoid Syndrome |
| NCT04852679 | PHASE3 | COMPLETED | Study to Assess the Efficacy and Safety of Lanreotide Autogel® in Chinese Participants With GEP-NETs |
| NCT03946527 | PHASE2 | ACTIVE_NOT_RECRUITING | LAnreotide in Metastatic Pheochromocytoma / PARAganglioma (LAMPARA) |
| NCT05048901 | PHASE1/PHASE2 | RECRUITING | Cabozantinib and Lanreotide as Treatment for Gastroenteropancreatic Neuroendocrine Tumors |
| NCT01076803 | PHASE2 | COMPLETED | Efficacy and Safety of Lanreotide 120 Milligram (mg) as a Palliative Treatment of Clinical Symptoms Associated With Malignant Intestinal Obstruction in Inoperable Patients |
| NCT01731925 | PHASE2 | UNKNOWN | A Study of Sunitinib Versus Placebo in Combination With Lanreotide in Patients With Progressive Advanced/Metastatic Midgut Carcinoid Tumors |
| NCT02054637 | PHASE2 | UNKNOWN | Resolving Bile Reflux by Lanreotide in Patients With Roux-en-Y Gastrojejunostomy |
| NCT02275338 | PHASE2 | COMPLETED | Study to Assess Efficacy and Safety of Lanreotide Autogel 120 MG in Treatment of Clinical Symptoms Associated With Inoperable Malignant Intestinal Obstruction |
| NCT02351128 | PHASE2 | COMPLETED | Treatment of Unresecable and/or Metastatic Merkel Cell Carcinoma by Somatostatine Analogues |
| NCT02859064 | PHASE2 | TERMINATED | Study of Lanreotide in Patients With Metastatic Gastrointestinal Neuroendocrine Tumors Who Are Undergoing Liver-directed Radioembolization With Yttrium-90 Microspheres |
| NCT03012594 | PHASE2 | COMPLETED | Lanreotide in the Treatment of Small Bowel Motility Disorders |
| NCT03043664 | PHASE1/PHASE2 | COMPLETED | Study of Pembrolizumab With Lanreotide Depot for Gastroenteropancreatic Neuroendocrine Tumors |
| NCT04427787 | PHASE2 | UNKNOWN | A Trial Aiming to Assess the Safety and Activity of the Combination of Cabozantinib Plus Lanreotide in GEP and NET |
| NCT02823691 | EARLY_PHASE1 | UNKNOWN | The MetNET-2 Trial |
| NCT01354405 | Not specified | COMPLETED | Somatostatin Analogues as a Volume Reducing Treatment of Polycystic Livers (RESOLVE) |
| NCT01538966 | Not specified | TERMINATED | Acromegaly Combination Treatment Study |
| NCT02973204 | Not specified | COMPLETED | Circulating Tumor Cells and Tumor DNA in HCC and NET |
| NCT04696042 | Not specified | COMPLETED | Asian Investigation of Lanreotide Autogel® in the Management of GEP-NETs |
| NCT06607666 | Not specified | COMPLETED | Acromegaly Resistant to Conventional Dose of First Generation Somatostatin Ligands |
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 |
|---|---|---|---|
| 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 |
| OCTREOTIDE | 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 |
Related Atlas pages
- Genes: SSTR2, SSTR3, SSTR5
- Diseases: neoplasm, acromegaly, carcinoid syndrome, carcinoid tumor, endocrine gland neoplasm, autosomal dominant polycystic kidney disease, carcinoid heart disease, rectal neoplasm, pituitary gland adenoma
- Drugs: Pasireotide, Edotreotide, Somatostatin, Vapreotide, Gallium Oxodotreotide, Octreotide, Loperamide, Astemizole, Paltusotine