pasireotide 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2B,AXL,BRAF,CAMK2D,CDK5,EGFR,EIF2AK3,ERBB2,GRK2,ITK,MAPK10,MET,NTRK2,PDK1,PDK2,PDK4,PRKDC 17
kinase-selectivity-class AXL,EIF2AK3,GRK2 3
pfas-class PFAS structural alert (1 = True, 0 = False) 0

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 434.94 33.10 126 2579 50844 90574898
Diabetes mellitus 400.72 33.10 125 2580 64750 90560992
Glycosylated haemoglobin increased 91.51 33.10 29 2676 15533 90610209
Blood glucose increased 90.89 33.10 48 2657 95198 90530544
Hypoglycaemia 74.64 33.10 38 2667 69810 90555932
Cholelithiasis 69.31 33.10 33 2672 52473 90573269
Adrenal insufficiency 62.66 33.10 26 2679 29895 90595847
Cortisol free urine increased 50.68 33.10 7 2698 55 90625687
Insulinoma 44.83 33.10 7 2698 136 90625606
Polyuria 44.04 33.10 15 2690 10025 90615717
Insulin-like growth factor decreased 43.85 33.10 8 2697 404 90625338
Nocturia 43.73 33.10 15 2690 10240 90615502
Insulin-like growth factor increased 42.66 33.10 9 2696 965 90624777
Diabetes mellitus inadequate control 41.70 33.10 17 2688 18667 90607075
Urine calcium/creatinine ratio increased 38.40 33.10 6 2699 117 90625625
Polydipsia 38.29 33.10 11 2694 4220 90621522
Bite 35.75 33.10 7 2698 517 90625225
Glucocorticoid deficiency 35.10 33.10 7 2698 568 90625174

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 166.38 36.82 55 902 45804 42574574
Diabetes mellitus 125.95 36.82 48 909 60039 42560339
Hyperadrenocorticism 44.71 36.82 7 950 187 42620191
Polyuria 40.06 36.82 13 944 9998 42610380
Neoplasm progression 39.25 36.82 17 940 28983 42591395
Diabetes mellitus inadequate control 38.27 36.82 14 943 15376 42605002

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 471.86 33.26 152 3238 84938 110500971
Diabetes mellitus 444.73 33.26 151 3239 99230 110486679
Glycosylated haemoglobin increased 97.76 33.26 34 3356 23585 110562324
Hypoglycaemia 88.67 33.26 51 3339 116053 110469856
Adrenal insufficiency 88.40 33.26 37 3353 42353 110543556
Cholelithiasis 83.12 33.26 40 3350 63382 110522527
Diabetes mellitus inadequate control 79.33 33.26 31 3359 29744 110556165
Blood glucose increased 77.38 33.26 49 3341 132447 110453462
Polyuria 75.19 33.26 26 3364 17712 110568197
Hyperadrenocorticism 65.75 33.26 12 3378 591 110585318
Cortisol increased 58.76 33.26 11 3379 623 110585286
Cortisol free urine increased 57.80 33.26 8 3382 62 110585847
Polydipsia 51.76 33.26 16 3374 7672 110578237
Glucocorticoid deficiency 46.26 33.26 10 3380 1172 110584737
Insulinoma 42.16 33.26 7 3383 197 110585712
Insulin-like growth factor decreased 40.46 33.26 8 3382 605 110585304
Neoplasm progression 40.45 33.26 25 3365 64570 110521339
Urine calcium/creatinine ratio increased 36.86 33.26 6 3384 149 110585760
Insulin-like growth factor increased 34.74 33.26 9 3381 2287 110583622
Bite 34.33 33.26 7 3383 618 110585291
Urethral caruncle 33.36 33.26 5 3385 71 110585838

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 agent
CHEBI has role CHEBI:76916 hyperglycemic agent

Related Drugs by ATC class:

H01CB Somatostatin and analogues 4 drugs
lanreotideoctreotidepaltusotinesomatostatin

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)

None

Orange Book exclusivity data (new drug applications)

None

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
4032239 VANDF
C1872203 UMLSCUI
CHEBI:72312 CHEBI
CHEMBL3349607 ChEMBL_ID
CHEMBL5314380 ChEMBL_ID
DB06663 DRUGBANK_ID
C517782 MESH_SUPPLEMENTAL_RECORD_UI
2018 IUPHAR_LIGAND_ID
8384 INN_ID
820232-50-6 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
CHEMBL5314382 ChEMBL_ID
396091-79-5 SECONDARY_CAS_RN
98H1T17066 INXIGHT DRUGS

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
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