pasireotide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
peptides and glycopeptides 4329 396091-73-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • pasireotide
  • pasireotide disapartate
  • SOM 230
  • SOM230
  • signifor
  • pasireotide diaspartate
  • pasireotide embonate
  • pasireotide pamoate
a somatostatin analog with pharmacologic properties mimicking those of the natural hormone somatostatin binds and activates the SSTRs resulting in inhibition of ACTH secretion, which leads to decreased cortisol secretion
  • Molecular weight: 1047.23
  • Formula: C58H66N10O9
  • CLOGP: 6.74
  • LIPINSKI: 4
  • HAC: 19
  • HDO: 9
  • TPSA: 281.20
  • ALOGS: -5.71
  • ROTB: 18
  • Status: ONP
    • Legend:
    OFP - off patent
    OFM - off market
    ONP - on patent

Drug dosage:

DoseUnitRoute
1.20 mg P

ADMET properties:

PropertyValueReference
BDDCS (Biopharmaceutical Drug Disposition Classification System) 3 Hosey CM, Chan R, Benet LZ
S (Water solubility) 100 mg/mL Bocci G, Oprea TI, Benet LZ

Approvals:

DateAgencyCompanyOrphan
Dec. 14, 2012 FDA NOVARTIS

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
Hyperglycaemia 385.19 32.90 117 2401 41750 63444754
Diabetes mellitus 364.17 32.90 120 2398 55690 63430814
Glycosylated haemoglobin increased 89.89 32.90 29 2489 12369 63474135
Blood glucose increased 73.34 32.90 44 2474 83712 63402792
Cholelithiasis 66.00 32.90 33 2485 43892 63442612
Adrenal insufficiency 64.84 32.90 25 2493 17890 63468614
Hypoglycaemia 56.31 32.90 33 2485 60032 63426472
Insulin-like growth factor increased 46.20 32.90 10 2508 909 63485595
Polyuria 42.24 32.90 15 2503 8527 63477977
Insulin-like growth factor decreased 41.89 32.90 8 2510 388 63486116
Diabetes mellitus inadequate control 37.18 32.90 16 2502 15110 63471394
Polydipsia 37.06 32.90 11 2507 3553 63482951
Urine calcium/creatinine ratio increased 36.85 32.90 6 2512 114 63486390
Cortisol free urine increased 35.16 32.90 5 2513 36 63486468
Bite 34.37 32.90 7 2511 474 63486030

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
Hyperglycaemia 164.24 38.99 53 765 39427 34916686
Diabetes mellitus 132.02 38.99 47 771 46826 34909287

FDA Adverse Event Reporting System (Geriatric)

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
Hyperglycaemia 427.75 29.58 143 2980 70192 79671073
Diabetes mellitus 420.33 29.58 145 2978 78245 79663020
Glycosylated haemoglobin increased 96.42 29.58 34 3089 19226 79722039
Adrenal insufficiency 90.38 29.58 36 3087 28451 79712814
Cholelithiasis 80.89 29.58 40 3083 52624 79688641
Polyuria 69.43 29.58 25 3098 14989 79726276
Hypoglycaemia 68.41 29.58 45 3078 101549 79639716
Diabetes mellitus inadequate control 64.43 29.58 27 3096 24237 79717028
Blood glucose increased 63.36 29.58 45 3078 114930 79626335
Cortisol increased 57.74 29.58 11 3112 534 79740731
Hyperadrenocorticism 55.76 29.58 10 3113 347 79740918
Polydipsia 50.30 29.58 16 3107 6589 79734676
Type 2 diabetes mellitus 47.65 29.58 29 3094 57093 79684172
Glucocorticoid deficiency 43.74 29.58 9 3114 649 79740616
Cortisol free urine increased 41.94 29.58 6 3117 46 79741219
Insulin-like growth factor increased 39.17 29.58 10 3113 1876 79739389
Insulin-like growth factor decreased 38.88 29.58 8 3115 577 79740688
Urine calcium/creatinine ratio increased 35.67 29.58 6 3117 142 79741123
Bite 33.59 29.58 7 3116 537 79740728
Urethral caruncle 31.95 29.58 5 3118 74 79741191
Fatigue 31.14 29.58 93 3030 929634 78811631
Hepatic steatosis 31.05 29.58 19 3104 37719 79703546

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC H01CB05 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 D006728 Hormones
FDA EPC N0000175904 Somatostatin Analog
CHEBI has role CHEBI:35610 antineoplastic agents
CHEBI has role CHEBI:50266 Prodrugs

Drug Use | Suggest Off label Use Form| |View source of the data|

DiseaseRelationSNOMED_IDDOID
Hypercortisolism indication 47270006




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 12.8 acidic
pKa2 13.26 acidic
pKa3 13.4 acidic
pKa4 13.93 acidic
pKa5 10.31 Basic
pKa6 8.91 Basic

Orange Book patent data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRoutePatent numberPatent expiration datePatent use
EQ 20MG BASE/VIAL SIGNIFOR LAR KIT RECORDATI RARE N203255 Dec. 15, 2014 RX FOR SUSPENSION INTRAMUSCULAR 8822637 Aug. 6, 2023 METHOD OF TREATING ACROMEGALY
EQ 40MG BASE/VIAL SIGNIFOR LAR KIT RECORDATI RARE N203255 Dec. 15, 2014 RX FOR SUSPENSION INTRAMUSCULAR 8822637 Aug. 6, 2023 METHOD OF TREATING ACROMEGALY
EQ 60MG BASE/VIAL SIGNIFOR LAR KIT RECORDATI RARE N203255 Dec. 15, 2014 RX FOR SUSPENSION INTRAMUSCULAR 8822637 Aug. 6, 2023 METHOD OF TREATING ACROMEGALY

Orange Book exclusivity data (new drug applications)

Formulation strengthTrade nameApplicantApplication numberApproval dateTypeDose formRouteExclusivity dateDescription
EQ 10MG BASE/VIAL SIGNIFOR LAR KIT RECORDATI RARE N203255 June 29, 2018 RX FOR SUSPENSION INTRAMUSCULAR June 29, 2025 INDICATED FOR TREATMENT OF PATIENTS WITH CUSHINGS DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE
EQ 20MG BASE/VIAL SIGNIFOR LAR KIT RECORDATI RARE N203255 Dec. 15, 2014 RX FOR SUSPENSION INTRAMUSCULAR June 29, 2025 INDICATED FOR TREATMENT OF PATIENTS WITH CUSHINGS DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE
EQ 30MG BASE/VIAL SIGNIFOR LAR KIT RECORDATI RARE N203255 June 29, 2018 RX FOR SUSPENSION INTRAMUSCULAR June 29, 2025 INDICATED FOR TREATMENT OF PATIENTS WITH CUSHINGS DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE
EQ 40MG BASE/VIAL SIGNIFOR LAR KIT RECORDATI RARE N203255 Dec. 15, 2014 RX FOR SUSPENSION INTRAMUSCULAR June 29, 2025 INDICATED FOR TREATMENT OF PATIENTS WITH CUSHINGS DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE
EQ 60MG BASE/VIAL SIGNIFOR LAR KIT RECORDATI RARE N203255 Dec. 15, 2014 RX FOR SUSPENSION INTRAMUSCULAR June 29, 2025 INDICATED FOR TREATMENT OF PATIENTS WITH CUSHINGS DISEASE FOR WHOM PITUITARY SURGERY IS NOT AN OPTION OR HAS NOT BEEN CURATIVE

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])		Mechanism
action		Bioact sourceMoA source
Somatostatin receptor type 2 GPCR AGONIST IC50 9 IUPHAR CHEMBL
Somatostatin receptor type 3 GPCR AGONIST IC50 8.80 IUPHAR CHEMBL
Somatostatin receptor type 5 GPCR AGONIST IC50 9.80 IUPHAR CHEMBL
Somatostatin receptor type 1 GPCR AGONIST IC50 8 IUPHAR CHEMBL
Somatostatin receptor type 2 GPCR AGONIST EC50 9.07 IUPHAR

External reference:

IDSource
4032239 VUID
N0000186784 NUI
D10147 KEGG_DRUG
820232-50-6 SECONDARY_CAS_RN
4032239 VANDF
C1872203 UMLSCUI
CHEBI:72312 CHEBI
CHEMBL3039583 ChEMBL_ID
CHEMBL3039588 ChEMBL_ID
DB06663 DRUGBANK_ID
C517782 MESH_SUPPLEMENTAL_RECORD_UI
2018 IUPHAR_LIGAND_ID
8384 INN_ID
396091-79-5 SECONDARY_CAS_RN
98H1T17066 UNII
9941444 PUBCHEM_CID
1364104 RXNORM
192917 MMSL
28816 MMSL
29021 MMSL
30767 MMSL
d07903 MMSL
014802 NDDF
014803 NDDF
015818 NDDF
704266003 SNOMEDCT_US
704267007 SNOMEDCT_US
704269005 SNOMEDCT_US
734521009 SNOMEDCT_US
CHEMBL3545188 ChEMBL_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Signifor HUMAN PRESCRIPTION DRUG LABEL 1 0078-0633 INJECTION 0.30 mg SUBCUTANEOUS NDA 31 sections
Signifor HUMAN PRESCRIPTION DRUG LABEL 1 0078-0634 INJECTION 0.60 mg SUBCUTANEOUS NDA 31 sections
Signifor HUMAN PRESCRIPTION DRUG LABEL 1 0078-0635 INJECTION 0.90 mg SUBCUTANEOUS NDA 31 sections
Signifor HUMAN PRESCRIPTION DRUG LABEL 1 55292-131 INJECTION 0.30 mg SUBCUTANEOUS NDA 31 sections
Signifor HUMAN PRESCRIPTION DRUG LABEL 1 55292-131 INJECTION 0.30 mg SUBCUTANEOUS NDA 31 sections
Signifor HUMAN PRESCRIPTION DRUG LABEL 1 55292-132 INJECTION 0.60 mg SUBCUTANEOUS NDA 31 sections
Signifor HUMAN PRESCRIPTION DRUG LABEL 1 55292-132 INJECTION 0.60 mg SUBCUTANEOUS NDA 31 sections
Signifor HUMAN PRESCRIPTION DRUG LABEL 1 55292-133 INJECTION 0.90 mg SUBCUTANEOUS NDA 31 sections
Signifor HUMAN PRESCRIPTION DRUG LABEL 1 55292-133 INJECTION 0.90 mg SUBCUTANEOUS NDA 31 sections