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

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 378.67 30.90 117 2327 36288 50566392
Diabetes mellitus 356.30 30.90 120 2324 48913 50553767
Glycosylated haemoglobin increased 88.73 30.90 29 2415 10577 50592103
Blood glucose increased 69.32 30.90 43 2401 71281 50531399
Adrenal insufficiency 65.64 30.90 25 2419 14218 50588462
Cholelithiasis 64.41 30.90 33 2411 37940 50564740
Hypoglycaemia 56.36 30.90 34 2410 53547 50549133
Polyuria 42.02 30.90 15 2429 7106 50595574
Insulin-like growth factor decreased 40.78 30.90 8 2436 366 50602314
Insulin-like growth factor increased 39.91 30.90 9 2435 809 50601871
Type 2 diabetes mellitus 39.21 30.90 23 2421 34352 50568328
Polydipsia 36.36 30.90 11 2433 3113 50599567
Diabetes mellitus inadequate control 36.32 30.90 16 2428 13129 50589551
Urine calcium/creatinine ratio increased 35.67 30.90 6 2438 114 50602566
Bite 34.62 30.90 7 2437 374 50602306
Cortisol free urine increased 34.18 30.90 5 2439 36 50602644
Glucocorticoid deficiency 31.37 30.90 6 2438 240 50602440

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 159.80 41.79 51 691 34236 29539549
Diabetes mellitus 132.54 41.79 46 696 39785 29534000

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 421.52 32.37 143 2905 60825 64434859
Diabetes mellitus 413.27 32.37 144 2904 66330 64429354
Glycosylated haemoglobin increased 96.30 32.37 34 3014 15985 64479699
Adrenal insufficiency 92.08 32.37 36 3012 22451 64473233
Cholelithiasis 79.31 32.37 40 3008 45466 64450218
Polyuria 69.04 32.37 25 3023 12618 64483066
Hypoglycaemia 68.12 32.37 46 3002 89846 64405838
Diabetes mellitus inadequate control 62.90 32.37 27 3021 21294 64474390
Blood glucose increased 62.19 32.37 45 3003 98028 64397656
Type 2 diabetes mellitus 56.61 32.37 29 3019 33991 64461693
Hyperadrenocorticism 55.10 32.37 10 3038 306 64495378
Cortisol increased 51.77 32.37 10 3038 431 64495253
Polydipsia 49.33 32.37 16 3032 5805 64489879
Glucocorticoid deficiency 43.57 32.37 9 3039 547 64495137
Cortisol free urine increased 40.81 32.37 6 3042 46 64495638
Insulin-like growth factor decreased 37.76 32.37 8 3040 550 64495134
Urine calcium/creatinine ratio increased 34.54 32.37 6 3042 142 64495542
Bite 33.96 32.37 7 3041 421 64495263
Insulin-like growth factor increased 33.82 32.37 9 3039 1643 64494041
Fatigue 32.81 32.37 93 2955 748637 63747047

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 55292-132 INJECTION 0.60 mg SUBCUTANEOUS NDA 31 sections
Signifor HUMAN PRESCRIPTION DRUG LABEL 1 55292-133 INJECTION 0.90 mg SUBCUTANEOUS NDA 31 sections