Vapreotide

Summary

Vapreotide (CHEMBL3349523) is a phase-3 clinical-stage protein (ATC H01CB04) targeting SSTR2, SSTR3, and SSTR5; indicated across 1 condition.

At a glance

• Status: Max clinical phase 3 (not approved)
• Modality: Protein
• ATC class: H01CB04
• Targets: 3 (SSTR2, SSTR3, SSTR5)
• Indications: 1 condition
• Clinical trials: 1
• Chemistry: 1131.4 Da · C57H70N12O9S2

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3349523
Name	Vapreotide
Type	Protein
Max phase	3
FDA approved	no
PubChem CID	6918026
ATC	H01CB04
Molecular formula	C57H70N12O9S2
Molecular weight	1131.4
InChIKey	SWXOGPJRIDTIRL-DOUNNPEJSA-N

SMILES: CC(C)[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=C(C=C4)O)NC(=O)[C@@H](CC5=CC=CC=C5)N)C(=O)N[C@@H](CC6=CNC7=CC=CC=C76)C(=O)N

IUPAC name: (4R,7S,10S,13R,16S,19R)-10-(4-aminobutyl)-N-[(2S)-1-amino-3-(1H-indol-3-yl)-1-oxopropan-2-yl]-19-[[(2R)-2-amino-3-phenylpropanoyl]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: BMY-41606, RC-160, Vapreotida, Vapreotide, VAPREOTIDE

Parent form; salt/anhydrous children: CHEMBL6067976

Patent coverage: 3,363 distinct patent families (14,736 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 14,735 (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
SSTR2	SST2 receptor	Full agonist	10.1	0.7%	P30874
SSTR3	SST3 receptor	Full agonist	7.9	0.2%	P32745
SSTR5	SST5 receptor	Full agonist	9.2	0%	P35346

Broader ChEMBL bioactivity targets: 5 (assay-derived). Sample: Somatostatin receptor type 5, Somatostatin receptor type 2, Somatostatin receptor type 4, Somatostatin receptor type 1, Somatostatin receptor type 3.

Bioactivity

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

Target	pChembl	Type	Value	Unit	Activity ID
SSTR2	10.1	Ki	0.08	nM	CHEMBL_ACT_514151
SSTR5	8.3	Ki	5.01	nM	CHEMBL_ACT_514154
SSTR3	7.7	Ki	19.95	nM	CHEMBL_ACT_514152
SSTR1	6.8	Ki	158.5	nM	CHEMBL_ACT_514150
SSTR4	6.8	Ki	158.5	nM	CHEMBL_ACT_514153

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

1 indication record carries no mapped disease name (EFO/MeSH-only); none shown.

Clinical trials

Total trials: 1.

Phase distribution

Phase	Trials
PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT00014651	PHASE3	TERMINATED	Vapreotide in Treating Patients Undergoing Elective Pancreatic Resection

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
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