lanreotide Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
peptides and glycopeptides 1546 108736-35-2

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lanreotide
  • angiopeptin
  • ipstyl
  • lanreotide autogel
  • somatulin-autogel
  • somatuline
  • lanreotide acetate
synthetic octapeptide analog of somatostatin; inhibits accelerated transplant atherosclerosis in rabbit heart arteries
  • Molecular weight: 1096.33
  • Formula: C54H69N11O10S2
  • CLOGP: 3.40
  • LIPINSKI: 3
  • HAC: 21
  • HDO: 13
  • TPSA: 355.08
  • ALOGS: -5.34
  • ROTB: 17

  • Status: OFP

  • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
3 mg P

ADMET properties:

PropertyValueReference
Vd (Volume of distribution) 0.20 L/kg Lombardo F, Berellini G, Obach RS
CL (Clearance) 5.70 mL/min/kg Lombardo F, Berellini G, Obach RS
t_half (Half-life) 1.03 hours Lombardo F, Berellini G, Obach RS

Approvals:

DateAgencyCompanyOrphan
Aug. 30, 2007 FDA IPSEN PHARMA

FDA Adverse Event Reporting System (Female)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Inappropriate schedule of product administration 309.59 20.43 165 7000 64848 46614049
Insulin-like growth factor increased 164.25 20.43 35 7130 738 46678159
Injection site mass 161.27 20.43 67 7098 14973 46663924
Diarrhoea 128.74 20.43 271 6894 559331 46119566
Injection site pain 101.11 20.43 102 7063 107050 46571847
Cholelithiasis 84.94 20.43 60 7105 38621 46640276
Blood growth hormone increased 83.81 20.43 18 7147 394 46678503
Flatulence 75.74 20.43 50 7115 28828 46650069
Abdominal distension 74.99 20.43 73 7092 73278 46605619
Abdominal pain 71.48 20.43 127 7038 229904 46448993
Neoplasm progression 59.97 20.43 42 7123 26641 46652256
Off label use 45.03 20.43 144 7021 379697 46299200
Injection site nodule 42.90 20.43 17 7148 3354 46675543
Carcinoid crisis 40.16 20.43 9 7156 241 46678656
Disease progression 37.12 20.43 57 7108 91243 46587654
Intestinal obstruction 36.52 20.43 31 7134 26044 46652853
Incorrect route of product administration 34.97 20.43 25 7140 16358 46662539
Blood glucose decreased 33.97 20.43 26 7139 18866 46660031
Pancreatic neuroendocrine tumour 33.05 20.43 8 7157 302 46678595
Abdominal pain upper 32.53 20.43 70 7095 145235 46533662
Needle issue 31.12 20.43 16 7149 5788 46673109
Steatorrhoea 31.03 20.43 8 7157 392 46678505
Terminal state 30.91 20.43 12 7153 2242 46676655
Blood glucose increased 30.74 20.43 46 7119 71967 46606930
Insulinoma 29.37 20.43 6 7159 102 46678795
Carcinoid syndrome 28.59 20.43 6 7159 117 46678780
Injection site haemorrhage 27.73 20.43 24 7141 20685 46658212
Product dose omission issue 26.71 20.43 71 7094 168449 46510448
Nausea 26.59 20.43 188 6977 687266 45991631
Hypoglycaemia 26.52 20.43 37 7128 54312 46624585
Gastroenteropancreatic neuroendocrine tumour disease 26.41 20.43 5 7160 56 46678841
Blood chromogranin A increased 26.35 20.43 6 7159 173 46678724
Weight decreased 25.85 20.43 81 7084 210768 46468129
Postoperative adhesion 24.93 20.43 6 7159 221 46678676
Faeces pale 24.22 20.43 9 7156 1493 46677404
Neuroendocrine tumour 23.47 20.43 7 7158 588 46678309
Vomiting 23.11 20.43 133 7032 452661 46226236
Thyroid neoplasm 22.27 20.43 11 7154 3658 46675239
Injection site hypoaesthesia 22.13 20.43 6 7159 357 46678540
Malignant neoplasm progression 21.56 20.43 37 7128 64889 46614008
Constipation 21.43 20.43 67 7098 174030 46504867
Metastases to liver 20.93 20.43 20 7145 19565 46659332
Muscle neoplasm 20.88 20.43 4 7161 48 46678849
Gallbladder neoplasm 20.65 20.43 4 7161 51 46678846
Lymphatic system neoplasm 20.51 20.43 4 7161 53 46678844
Pituitary tumour 20.51 20.43 7 7158 908 46677989

FDA Adverse Event Reporting System (Male)

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Inappropriate schedule of product administration 225.61 22.16 116 4803 39612 29907947
Diarrhoea 150.39 22.16 225 4694 333878 29613681
Injection site pain 139.40 22.16 77 4842 30233 29917326
Insulin-like growth factor increased 125.29 22.16 30 4889 1011 29946548
Neoplasm progression 108.96 22.16 55 4864 17968 29929591
Injection site mass 105.19 22.16 37 4882 4916 29942643
Abdominal pain 79.21 22.16 104 4815 135550 29812009
Off label use 75.34 22.16 141 4778 249149 29698410
Injection site haemorrhage 72.14 22.16 32 4887 7823 29939736
Flatulence 67.03 22.16 40 4879 18089 29929470
Cholelithiasis 65.51 22.16 41 4878 20184 29927375
Pituitary tumour removal 54.01 22.16 7 4912 0 29947559
Carcinoid heart disease 50.84 22.16 7 4912 4 29947555
Disease progression 49.23 22.16 63 4856 79811 29867748
Incorrect route of product administration 41.89 22.16 25 4894 11290 29936269
Injection site nodule 35.23 22.16 12 4907 1446 29946113
Injection site abscess 30.27 22.16 9 4910 699 29946860
Abdominal pain upper 28.95 22.16 43 4876 62508 29885051
Nausea 26.19 22.16 107 4812 296850 29650709
Steatorrhoea 26.00 22.16 8 4911 698 29946861
Keratitis 25.90 22.16 9 4910 1151 29946408
Hepatic neoplasm 25.21 22.16 10 4909 1849 29945710
Abdominal distension 24.94 22.16 34 4885 45675 29901884
Pituitary tumour benign 24.64 22.16 8 4911 831 29946728

Pharmacologic Action:

SourceCodeDescription
ATC H01CB03 SYSTEMIC HORMONAL PREPARATIONS, EXCL. SEX HORMONES AND INSULINS
PITUITARY AND HYPOTHALAMIC HORMONES AND ANALOGUES
HYPOTHALAMIC HORMONES
Somatostatin and analogues
FDA MoA N0000000194 Somatostatin Receptor Agonists
MeSH PA D000970 Antineoplastic Agents
FDA EPC N0000175904 Somatostatin Analog

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Acromegaly indication 74107003 DOID:2449
Hypersomatotropic gigantism indication 86073008
Hypertensive disorder contraindication 38341003 DOID:10763
Disorder of gallbladder contraindication 39621005 DOID:0060262
Hypothyroidism contraindication 40930008 DOID:1459
Bradycardia contraindication 48867003
Hyperglycemia contraindication 80394007 DOID:4195
Impaired renal function disorder contraindication 197663003
Disease of liver contraindication 235856003 DOID:409
Hypoglycemic disorder contraindication 237630007
Calculus in biliary tract contraindication 266474003

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 9.65 acidic
pKa2 12.16 acidic
pKa3 12.71 acidic
pKa4 13.18 acidic
pKa5 13.43 acidic
pKa6 13.67 acidic
pKa7 10.31 Basic
pKa8 6.97 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 120MG BASE/0.5ML (EQ 120MG BASE/0.5ML) SOMATULINE DEPOT IPSEN PHARMA N022074 Aug. 30, 2007 RX SOLUTION SUBCUTANEOUS Dec. 16, 2021 TREATMENT OF PATIENTS WITH UNRESECTABLE,WELL- OR MODERATELY-DIFFERENTIATED LOCALLY ADVANCED OR METASTATIC GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS TO IMPROVE PROGRESSION-FREE SURVIVAL
EQ 60MG BASE/0.2ML (EQ 60MG BASE/0.2ML) SOMATULINE DEPOT IPSEN PHARMA N022074 Aug. 30, 2007 RX SOLUTION SUBCUTANEOUS Dec. 16, 2021 TREATMENT OF PATIENTS WITH UNRESECTABLE,WELL- OR MODERATELY-DIFFERENTIATED LOCALLY ADVANCED OR METASTATIC GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS TO IMPROVE PROGRESSION-FREE SURVIVAL
EQ 90MG BASE/0.3ML (EQ 90MG BASE/0.3ML) SOMATULINE DEPOT IPSEN PHARMA N022074 Aug. 30, 2007 RX SOLUTION SUBCUTANEOUS Dec. 16, 2021 TREATMENT OF PATIENTS WITH UNRESECTABLE,WELL- OR MODERATELY-DIFFERENTIATED LOCALLY ADVANCED OR METASTATIC GASTROENTEROPANCREATIC NEUROENDOCRINE TUMORS TO IMPROVE PROGRESSION-FREE SURVIVAL
EQ 120MG BASE/0.5ML (EQ 120MG BASE/0.5ML) SOMATULINE DEPOT IPSEN PHARMA N022074 Aug. 30, 2007 RX SOLUTION SUBCUTANEOUS Sept. 15, 2024 TREATMENT OF ADULTS WITH CARCINOID SYNDROME; WHEN USED, IT REDUCES THE FREQUENCY OF SHORT-ACTING SOMATOSTATIN ANULLLOG RESCUE THERAPY
EQ 60MG BASE/0.2ML (EQ 60MG BASE/0.2ML) SOMATULINE DEPOT IPSEN PHARMA N022074 Aug. 30, 2007 RX SOLUTION SUBCUTANEOUS Sept. 15, 2024 TREATMENT OF ADULTS WITH CARCINOID SYNDROME; WHEN USED, IT REDUCES THE FREQUENCY OF SHORT-ACTING SOMATOSTATIN ANULLLOG RESCUE THERAPY
EQ 90MG BASE/0.3ML (EQ 90MG BASE/0.3ML) SOMATULINE DEPOT IPSEN PHARMA N022074 Aug. 30, 2007 RX SOLUTION SUBCUTANEOUS Sept. 15, 2024 TREATMENT OF ADULTS WITH CARCINOID SYNDROME; WHEN USED, IT REDUCES THE FREQUENCY OF SHORT-ACTING SOMATOSTATIN ANULLLOG RESCUE THERAPY

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Somatostatin receptor type 5 GPCR AGONIST Ki 9.30 IUPHAR CHEMBL
Somatostatin receptor type 2 GPCR AGONIST Ki 9.60 IUPHAR CHEMBL
Somatostatin receptor type 3 GPCR AGONIST Ki 8 IUPHAR
Somatostatin receptor type 4 GPCR Ki 7.18 PDSP
Somatostatin receptor type 1 GPCR Ki 6.30 PDSP
Somatostatin receptor type 2 Unclassified AGONIST Ki 8.80 IUPHAR
Somatostatin receptor type 3 GPCR AGONIST IC50 8.20 IUPHAR
Somatostatin receptor type 3 Unclassified AGONIST Ki 6.90 IUPHAR
Somatostatin receptor type 5 GPCR AGONIST Ki 7.60 IUPHAR
Somatostatin receptor type 2 GPCR AGONIST Ki 9.10 IUPHAR

External reference:

IDSource
4026631 VUID
N0000179366 NUI
D04666 KEGG_DRUG
127984-74-1 SECONDARY_CAS_RN
4026631 VANDF
C0051846 UMLSCUI
CHEBI:135901 CHEBI
CHEMBL1201185 ChEMBL_ID
CHEMBL1201184 ChEMBL_ID
DB06791 DRUGBANK_ID
C060347 MESH_SUPPLEMENTAL_RECORD_UI
2031 IUPHAR_LIGAND_ID
6649 INN_ID
0G3DE8943Y UNII
6918010 PUBCHEM_CID
236167 RXNORM
18121 MMSL
d04961 MMSL
005272 NDDF
005273 NDDF
327379003 SNOMEDCT_US
395765000 SNOMEDCT_US
429611006 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
SOMATULINE DEPOT HUMAN PRESCRIPTION DRUG LABEL 1 15054-1060 INJECTION 60 mg SUBCUTANEOUS NDA 29 sections
SOMATULINE DEPOT HUMAN PRESCRIPTION DRUG LABEL 1 15054-1090 INJECTION 90 mg SUBCUTANEOUS NDA 29 sections
SOMATULINE DEPOT HUMAN PRESCRIPTION DRUG LABEL 1 15054-1120 INJECTION 120 mg SUBCUTANEOUS NDA 29 sections