Pasireotide

Summary

Pasireotide (CHEMBL3349607) is an approved protein antineoplastic agent (ATC H01CB05) targeting SSTR1, SSTR2, and SSTR3; indicated across 33 conditions including carcinoid tumor and acromegaly; with CIViC clinical evidence for 1 variant-indication association (e.g. SSTR5 Overexpression in neuroendocrine tumor).

At a glance

• Status: Approved (max clinical phase 4)
• Modality: Protein
• ATC class: H01CB05
• Targets: 4 (SSTR1, SSTR2, SSTR3…)
• Indications: 33 conditions
• Clinical trials: 55
• Precision-oncology evidence (CIViC): 1 variant–indication association
• Chemistry: 1047.2 Da · C58H66N10O9

Identifiers

Drug identity and classification

Field	Value
ChEMBL ID	CHEMBL3349607
Name	Pasireotide
Type	Protein
Max phase	4
FDA approved	yes
PubChem CID	9941444
ChEBI	CHEBI:72312
ATC	H01CB05
Molecular formula	C58H66N10O9
Molecular weight	1047.2
InChIKey	VMZMNAABQBOLAK-DBILLSOUSA-N

SMILES: C1[C@H](CN2[C@@H]1C(=O)N[C@H](C(=O)N[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C2=O)CC3=CC=CC=C3)CC4=CC=C(C=C4)OCC5=CC=CC=C5)CCCCN)CC6=CNC7=CC=CC=C76)C8=CC=CC=C8)OC(=O)NCCN

IUPAC name: [(3S,6S,9S,12R,15S,18S,20R)-9-(4-aminobutyl)-3-benzyl-12-(1H-indol-3-ylmethyl)-2,5,8,11,14,17-hexaoxo-15-phenyl-6-[(4-phenylmethoxyphenyl)methyl]-1,4,7,10,13,16-hexazabicyclo[16.3.0]henicosan-20-yl] N-(2-aminoethyl)carbamate

ChEBI definition: A six-membered homodetic cyclic peptide composed from L-phenylglycyl, D-tryptophyl, L-lysyl, O-benzyl-L-tyrosyl, L-phenylalanyl and modified L-hydroxyproline residues joined in sequence. A somatostatin analogue with pharmacologic properties mimicking those of the natural hormone somatostatin; used (as its diaspartate salt) for treatment of Cushing’s disease.

Pharmacological roles (ChEBI): antineoplastic agent.

Also known as: Pasireotida, Pasireotide, Signifor, SOM 230, SOM-230, SOM230, PASIREOTIDE, pasireotide

Parent form; salt/anhydrous children: CHEMBL5314380, CHEMBL5314382, CHEMBL5316227

Patent coverage: 47 distinct patent families (109 SureChEMBL compound mentions), from 2 matched compound structure(s). One matched structure accounts for 103 (94%) 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
SSTR1	SST1 receptor	Full agonist	8	0%	P30872
SSTR2	SST2 receptor	Full agonist	9	0.7%	P30874
SSTR3	SST3 receptor	Full agonist	8.8	0.2%	P32745
SSTR5	SST5 receptor	Full agonist	9.8	0%	P35346

Broader ChEMBL bioactivity targets: 23 (assay-derived). Sample: Somatostatin receptor type 5, Somatostatin receptor type 2, Alpha-2A adrenergic receptor, Alpha-2C adrenergic receptor, Somatostatin receptor type 1, Histamine H2 receptor, Alpha-2B adrenergic receptor, Somatostatin receptor type 3, Muscarinic acetylcholine receptor M5, Muscarinic acetylcholine receptor M2.

Bioactivity

ChEMBL activities: 17 potent at pChembl ≥ 5 of 23 total. Top 30 by potency (10 = 0.1 nM, 6 = 1 µM):

Target	pChembl	Type	Value	Unit	Activity ID
SSTR5	9.9	Ki	0.13	nM	CHEMBL_ACT_544242
SSTR3	9.1	Ki	0.79	nM	CHEMBL_ACT_544240
SSTR2	9	Ki	1	nM	CHEMBL_ACT_544239
SSTR1	8.2	Ki	6.31	nM	CHEMBL_ACT_544238
OPRK1	7.28	AC50	52.4	nM	CHEMBL_ACT_25129614
GHSR	6.59	AC50	255.9	nM	CHEMBL_ACT_25172948
OPRM1	6.26	AC50	550	nM	CHEMBL_ACT_25157586
HTR1A	6.09	AC50	807.7	nM	CHEMBL_ACT_25164571
OPRD1	5.51	AC50	3100	nM	CHEMBL_ACT_25154269
ADRA1A	5.46	AC50	3479	nM	CHEMBL_ACT_25138466
SLC6A2	5.46	AC50	3500	nM	CHEMBL_ACT_25145198
DRD2	5.42	AC50	3800	nM	CHEMBL_ACT_25140535
HTR2A	5.33	AC50	4618	nM	CHEMBL_ACT_25173687
HRH2	5.32	AC50	4738	nM	CHEMBL_ACT_25114493
MC3R	5.29	AC50	5188	nM	CHEMBL_ACT_25183596
KCNH2	5.2	AC50	6294	nM	CHEMBL_ACT_25118150
ADRA2C	5.05	AC50	8900	nM	CHEMBL_ACT_25148079

Target pathways

Aggregated over 4 target gene(s): SSTR1, SSTR2, SSTR3, SSTR5.

Top Reactome pathways

11 total, by targets touching each:

Pathway	Targets	Genes
Signal Transduction	4	SSTR1, SSTR2, SSTR3, SSTR5
Signaling by GPCR	4	SSTR1, SSTR2, SSTR3, SSTR5
Class A/1 (Rhodopsin-like receptors)	4	SSTR1, SSTR2, SSTR3, SSTR5
Peptide ligand-binding receptors	4	SSTR1, SSTR2, SSTR3, SSTR5
GPCR downstream signalling	4	SSTR1, SSTR2, SSTR3, SSTR5
G alpha (i) signalling events	4	SSTR1, SSTR2, SSTR3, SSTR5
GPCR ligand binding	4	SSTR1, 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	4
neuropeptide signaling pathway	4
negative regulation of cell population proliferation	4
signal transduction	4
G protein-coupled receptor signaling pathway	4
somatostatin signaling pathway	4
cellular response to estradiol stimulus	2
cellular response to glucocorticoid stimulus	2
glutamate receptor signaling pathway	1
spermatogenesis	1
cerebellum development	1
forebrain development	1
response to starvation	1
cellular response to leukemia inhibitory factor	1
adenylate cyclase-inhibiting G protein-coupled receptor signaling pathway	1

Indications & clinical

Indications

33 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
carcinoid tumor	3	MONDO:0005369	EFO:0004243
acromegaly	3	MONDO:0019933	EFO:1001485
exocrine pancreatic carcinoma	3	MONDO:0005192	EFO:0002618
ACTH-dependent Cushing syndrome	3	MONDO:0020528	EFO:1001110
hyperglycemia	2	MONDO:0002909	HP:0003074
lung carcinoma	2	MONDO:0005138	EFO:0001071
adenoma	2	MONDO:0004972	EFO:0000232
hepatocellular carcinoma	2	MONDO:0007256	EFO:0000182
small cell lung carcinoma	2	MONDO:0008433	EFO:0000702
plasma cell myeloma	2	MONDO:0009693	EFO:0001378
lymphoid neoplasm	2	MONDO:0005157	EFO:0001642
Cushing syndrome	2	MONDO:0018912	EFO:0003099
pancreatic neuroendocrine neoplasm	2	MONDO:0005815	EFO:0007331
thymoma	2	MONDO:0006456	EFO:1000581
ectopic ACTH secretion syndrome	2	MONDO:0043472	EFO:1001256
dumping syndrome	2	MONDO:0001979	EFO:1001307
neuroendocrine neoplasm	2	MONDO:0019496	EFO:1001901
breast neoplasm	2	MONDO:0021100	MONDO:0007254
meningioma	2	MONDO:0016642	MONDO:0016642
neoplasm	2	MONDO:0005070	MONDO:0004992
uveal melanoma	2	MONDO:0006486	EFO:1000616
cutaneous neuroendocrine carcinoma	1	MONDO:0019210	EFO:1001471
ductal breast carcinoma in situ	1	MONDO:0005023	EFO:0000432
prostate adenocarcinoma	1	MONDO:0005082	EFO:0000673
digestive system neoplasm	1	MONDO:0021223	EFO:0008549
kidney disorder	1	MONDO:0005240	EFO:0003086

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

Clinical trials

Total trials: 55.

Phase distribution

Phase	Trials
PHASE2	26
PHASE1	10
PHASE4	7
PHASE3	6
Not specified	3
PHASE1/PHASE2	2
PHASE2/PHASE3	1

Top trials by phase / activity

NCT	Phase	Status	Title
NCT02775227	PHASE4	ACTIVE_NOT_RECRUITING	HYPAR Trial - Hydrocortisone vs. Pasireotide in Reducing Pancreatic Surgery Complications
NCT01794793	PHASE4	COMPLETED	Study to Allow Access to Pasireotide for Patients Benefiting From Pasireotide Treatment in Novartis-sponsored Studies
NCT02060383	PHASE4	COMPLETED	Study of Management of Pasireotide-induced Hyperglycemia in Adult Patients With Cushing’s Disease or Acromegaly
NCT02527993	PHASE4	COMPLETED	Treatment of Hypoglycemia Following Gastric Bypass Surgery
NCT02779257	PHASE4	WITHDRAWN	Pasireotide Treatment for Neuroendocrine Tumor
NCT03080181	PHASE4	COMPLETED	Adipokine Profile in Patients With Cushing’s Disease on Pasireotide Treatment
NCT03514576	PHASE4	UNKNOWN	Pasireotide in the Treatment of Hypoglycemia Following Gastric Bypass Surgery
NCT00434148	PHASE3	COMPLETED	Safety and Efficacy of Different Dose Levels of Pasireotide in Patients With de Novo, Persistent or Recurrent Cushing’s Disease
NCT00600886	PHASE3	COMPLETED	Safety and Efficacy of Pasireotide Long Acting Release (LAR) vs. Octreotide LAR in Patients With Active Acromegaly
NCT00690430	PHASE3	COMPLETED	Efficacy and Safety of Pasireotide Long Acting Release vs. Octreotide Long Acting Release in Patients With Metastatic Carcinoid Disease
NCT00994110	PHASE3	COMPLETED	Placebo Controlled Trial of SOM230 for the Reduction of Post-Pancreatectomy Fistula, Leak, and Abscess
NCT01137682	PHASE3	COMPLETED	Efficacy and Safety of Pasireotide Long Acting Release (LAR) Versus Octreotide LAR or Lanreotide Autogel (ATG) in Patients With Inadequately Controlled Acromegaly
NCT01582061	PHASE3	COMPLETED	An Open-label, Multi-center, Expanded Access Study of Pasireotide s.c. in Patients With Cushing’s Disease.
NCT01620138	PHASE2/PHASE3	COMPLETED	Response to Cabergoline and Pasireotide in Non-functioning Pituitary Adenomas and Resistant Prolactinomas
NCT06295952	PHASE2	RECRUITING	A Study of Pasireotide in People With Prolactinoma
NCT06456359	PHASE2	RECRUITING	Pasireotide as Maintenance Treatment in Synovial Sarcoma and Desmoplastic Small Round Cell Tumor
NCT00088582	PHASE2	COMPLETED	Study Comparing SOM230 Subcutaneously and Sandostatin Subcutaneously in Acromegalic Patients
NCT00088595	PHASE2	COMPLETED	Study Evaluating SOM230 in Patients With Metastatic Carcinoid Tumors
NCT00088608	PHASE2	COMPLETED	A Study to Assess SOM230 in Patients With Pituitary Cushing’s Disease
NCT00171730	PHASE2	COMPLETED	An Extension Study to Assess the Long-Term Safety and Efficacy of Pasireotide in Participants With Acromegaly
NCT00171951	PHASE2	COMPLETED	Extension Study to Assess the Safety and Efficacy of Pasireotide in Participants With Cushing’s Disease
NCT01128192	PHASE2	COMPLETED	Somatostatin Analogue SOM230 (Pasireotide) in Healthy Male Volunteers
NCT01234974	PHASE2	WITHDRAWN	IGF-1 Inhibitor Pasireotide Lar in Combination With the m-TOR Inhibitor Everolimus
NCT01252251	PHASE2	COMPLETED	RAD001 (Everolimus) and Pasireotide (SOM230) LAR in Patients With Advanced Uveal Melanoma
NCT01270321	PHASE2	COMPLETED	Pasireotide & Everolimus in Adult Patients With Radioiodine-Refractory Differentiated & Medullary Thyroid Cancer
NCT01313559	PHASE2	TERMINATED	Pasireotide (SOM230) With or Without Everolimus in Treating Patients With Hormone Resistant, Chemotherapy Naive Prostate Cancer
NCT01329289	PHASE2	WITHDRAWN	SOM230 LAR With Bortezomib and Dexamethasone for Refractory or Relapsed Multiple Myeloma
NCT01356862	PHASE2	COMPLETED	Pasireotide LAR Administration in Lymphocele Prevention After Axillary Node Dissection for Breast Cancer
NCT01372618	PHASE1/PHASE2	TERMINATED	Breast Cancer Chemoprevention by SOM230, an IGF-I Action Inhibitor
NCT01417806	PHASE2	UNKNOWN	Trial of pasireotideLAR and Topotecan in Relapsed or Refractory Small Cell Lung Cancer
NCT01468532	PHASE1/PHASE2	COMPLETED	Docetaxel, Prednisone, and Pasireotide in Treating Patients With Metastatic Hormone-Resistant Prostate Cancer
NCT01488487	PHASE2	COMPLETED	Everolimus and Pasireotide (SOM230) in Patients With Advanced or Metastatic Hepatocellular Carcinoma
NCT01617733	PHASE2	TERMINATED	Pasireotide Therapy in Patients With Nelson’s Syndrome
NCT01637272	PHASE2	COMPLETED	Phase II Study Evaluating Efficacy, Safety and Pharmacokinetics of Pasireotide in Patients With Dumping Syndrome
NCT01639352	PHASE2	COMPLETED	Phase II Trial of SOM230 in Patients With Unresectable Hepatocellular Carcinoma
NCT01895296	PHASE2	COMPLETED	Study to Assess Safety and Efficacy of sc Pasireotide in Patients With Dumping Syndrome
NCT02215070	PHASE2	COMPLETED	Pasireotide in Prevention of GI Toxicity
NCT02619617	PHASE2	TERMINATED	Safety and Efficacy Study of SOM230 s.c. in Cluster Headache
NCT02622906	PHASE2	COMPLETED	Pasireotide for the Treatment of Gastrointestinal Angiodysplasia in Endoscopic Treatment Failure
NCT02713776	PHASE2	COMPLETED	Reduction by Pasireotide of the Effluent Volume in High-output Enterostomy in Patients Refractory to Usual Medical Treatment

Clinical evidence (CIViC)

Variant × indication × effect (1 predictive associations from 1 curated evidence items):

Variant	Indication	Effect	Therapy	Level	CIViC
SSTR5 Overexpression	Neuroendocrine Tumor	Sensitivity/Response	Pasireotide	CIViC B	EID10193

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)	SSTR1, SSTR2, SSTR3, SSTR5
SOMATOSTATIN	ChEMBL	Phase 3	SSTR1, SSTR2, SSTR3, SSTR5
VAPREOTIDE	ChEMBL	Phase 3	SSTR1, SSTR2, SSTR3, SSTR5
oxodotreotide	PubChem	Approved	SSTR1, SSTR2, SSTR3, SSTR5
EDOTREOTIDE	ChEMBL	Phase 3	SSTR2, SSTR3, SSTR5
EDOTREOTIDE YTTRIUM	ChEMBL	Phase 2	SSTR2, SSTR3, SSTR5
SEGLITIDE	ChEMBL	Phase 2	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