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

Stem definitionDrug idCAS RN
bradykinin receptors antagonists 4186 130308-48-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • icatibant accord
  • WIN-65365
  • WIN 65365
  • icatibant
  • firazyr
  • icatibant acetate
a potent bradykinin (B2) receptor antagonist; WIN 65365 is an L-Tic(7) stereoisomer
  • Molecular weight: 1304.54
  • Formula: C59H89N19O13S
  • CLOGP: -3.47
  • LIPINSKI: 3
  • HAC: 32
  • HDO: 18
  • TPSA: 516.22
  • ALOGS: -4.56
  • ROTB: 30

Drug dosage:

DoseUnitRoute
30 mg P

ADMET properties:

None

Approvals:

DateAgencyCompanyOrphan
Sept. 21, 2018 PMDA Shire Japan KK
July 11, 2008 EMA Shire Pharmaceuticals Ireland Limited
Aug. 25, 2011 FDA SHIRE ORPHAN THERAP

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
Hereditary angioedema 1683.60 32.19 293 3061 5149 50596621
Pharyngeal oedema 242.94 32.19 71 3283 13094 50588676
Prescribed overdose 210.06 32.19 65 3289 14535 50587235
Laryngeal oedema 195.99 32.19 49 3305 5004 50596766
Inappropriate schedule of product administration 168.63 32.19 86 3268 71745 50530025
No adverse event 111.31 32.19 51 3303 33527 50568243
Injection site pain 91.12 32.19 68 3286 110956 50490814
Product availability issue 69.81 32.19 18 3336 2070 50599700
Swollen tongue 60.44 32.19 32 3322 28598 50573172
Localised oedema 50.76 32.19 17 3337 4850 50596920
Hospitalisation 49.88 32.19 39 3315 67898 50533872
Device related infection 46.09 32.19 24 3330 20711 50581059
Product dose omission issue 45.00 32.19 58 3296 183780 50417990
Injection site erythema 40.42 32.19 36 3318 74900 50526870
Poor venous access 38.31 32.19 17 3337 10323 50591447
Pharyngeal swelling 36.21 32.19 13 3341 4553 50597217

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
Hereditary angioedema 595.23 46.29 80 632 681 29573134
Inappropriate schedule of product administration 55.24 46.29 25 687 44447 29529368
Injection site pain 52.54 46.29 22 690 32424 29541391

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
Hereditary angioedema 1510.17 35.43 239 2520 3637 64492336
Pharyngeal oedema 225.16 35.43 63 2696 15468 64480505
Laryngeal oedema 155.74 35.43 40 2719 7073 64488900
Inappropriate schedule of product administration 138.93 35.43 71 2688 92215 64403758
Prescribed overdose 133.81 35.43 45 2714 20286 64475687
Injection site pain 112.92 35.43 66 2693 111342 64384631
No adverse event 90.65 35.43 37 2722 28524 64467449
Localised oedema 68.08 35.43 21 2738 7170 64488803
Product dose omission issue 63.33 35.43 58 2701 194689 64301284
Product availability issue 61.79 35.43 15 2744 2101 64493872
Swollen tongue 61.61 35.43 30 2729 34924 64461049
Injection site erythema 46.63 35.43 32 2727 70768 64425205
Hospitalisation 40.33 35.43 30 2729 75177 64420796

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC B06AC02 BLOOD AND BLOOD FORMING ORGANS
OTHER HEMATOLOGICAL AGENTS
OTHER HEMATOLOGICAL AGENTS
Drugs used in hereditary angioedema
MeSH PA D000700 Analgesics
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D018501 Antirheumatic Agents
MeSH PA D065094 Bradykinin B2 Receptor Antagonists
MeSH PA D065168 Bradykinin Receptor Antagonists
MeSH PA D051056 Complement Inactivating Agents
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018689 Sensory System Agents
FDA MoA N0000182964 Bradykinin B2 Receptor Antagonists
FDA EPC N0000182965 Bradykinin B2 Receptor Antagonist
CHEBI has role CHEBI:35530 beta-adrenergic blockers
CHEBI has role CHEBI:63175 peptidomimetics
CHEBI has role CHEBI:68557 bradykinin receptor antagonists

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

DiseaseRelationSNOMED_IDDOID
Hereditary angioneurotic edema indication 82966003 DOID:14735




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 3.3 acidic
pKa2 13.85 acidic
pKa3 12.18 Basic
pKa4 10.88 Basic
pKa5 10.16 Basic
pKa6 7.56 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
B2 bradykinin receptor GPCR ANTAGONIST Ki 10.22 CHEMBL CHEMBL
B1 bradykinin receptor GPCR ANTAGONIST Ki 7 IUPHAR
B2 bradykinin receptor GPCR Ki 10.11 CHEMBL
B2 bradykinin receptor GPCR Ki 9.96 CHEMBL
B2 bradykinin receptor GPCR ANTAGONIST Ki 9.60 IUPHAR
B1 bradykinin receptor GPCR ANTAGONIST Ki 6.40 IUPHAR

External reference:

IDSource
4031108 VUID
N0000183562 NUI
D04492 KEGG_DRUG
138614-30-9 SECONDARY_CAS_RN
4031108 VANDF
C0246269 UMLSCUI
CHEBI:68556 CHEBI
CHEMBL2028850 ChEMBL_ID
CHEMBL2028852 ChEMBL_ID
DB06196 DRUGBANK_ID
C065679 MESH_SUPPLEMENTAL_RECORD_UI
667 IUPHAR_LIGAND_ID
6922 INN_ID
7PG89G35Q7 UNII
6918173 PUBCHEM_CID
1148138 RXNORM
160761 MMSL
320534 MMSL
d07393 MMSL
012894 NDDF
012895 NDDF
703834005 SNOMEDCT_US
703835006 SNOMEDCT_US
715582002 SNOMEDCT_US

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Icatibant HUMAN PRESCRIPTION DRUG LABEL 1 0093-3066 INJECTION, SOLUTION 10 mg SUBCUTANEOUS ANDA 27 sections
Icatibant HUMAN PRESCRIPTION DRUG LABEL 1 24201-207 INJECTION, SOLUTION 30 mg SUBCUTANEOUS ANDA 29 sections
Icatibant HUMAN PRESCRIPTION DRUG LABEL 1 24201-207 INJECTION, SOLUTION 30 mg SUBCUTANEOUS ANDA 29 sections
Icatibant HUMAN PRESCRIPTION DRUG LABEL 1 54092-135 INJECTION, SOLUTION 30 mg SUBCUTANEOUS NDA authorized generic 34 sections
Firazyr HUMAN PRESCRIPTION DRUG LABEL 1 54092-702 INJECTION, SOLUTION 30 mg SUBCUTANEOUS NDA 34 sections
Firazyr HUMAN PRESCRIPTION DRUG LABEL 1 54092-702 INJECTION, SOLUTION 30 mg SUBCUTANEOUS NDA 34 sections
ICATIBANT HUMAN PRESCRIPTION DRUG LABEL 1 60505-6214 INJECTION, SOLUTION 30 mg SUBCUTANEOUS ANDA 29 sections
Icatibant HUMAN PRESCRIPTION DRUG LABEL 1 63323-574 INJECTION, SOLUTION 10 mg SUBCUTANEOUS ANDA 29 sections
Icatibant HUMAN PRESCRIPTION DRUG LABEL 1 68462-828 INJECTION, SOLUTION 30 mg SUBCUTANEOUS ANDA 29 sections
Icatibant HUMAN PRESCRIPTION DRUG LABEL 1 68462-828 INJECTION, SOLUTION 30 mg SUBCUTANEOUS ANDA 29 sections
ICATIBANT HUMAN PRESCRIPTION DRUG LABEL 1 69097-664 INJECTION 30 mg SUBCUTANEOUS ANDA 25 sections
SAJAZIR HUMAN PRESCRIPTION DRUG LABEL 1 70709-013 INJECTION 30 mg SUBCUTANEOUS ANDA 25 sections
Icatibant Human Prescription Drug Label 1 71225-114 INJECTION 30 mg SUBCUTANEOUS ANDA 26 sections