icatibant 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: -5.89
  • 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 3339.90 35.01 528 2708 5725 53340105
Pharyngeal oedema 246.28 35.01 72 3164 14541 53331289
Prescribed overdose 210.40 35.01 63 3173 13796 53332034
Laryngeal oedema 194.93 35.01 49 3187 5596 53340234
Inappropriate schedule of product administration 137.81 35.01 74 3162 74804 53271026
No adverse event 101.90 35.01 49 3187 39216 53306614
Injection site pain 88.40 35.01 65 3171 113326 53232504
Swollen tongue 55.02 35.01 30 3206 31050 53314780
Localised oedema 50.79 35.01 17 3219 5292 53340538
Hospitalisation 47.05 35.01 37 3199 70975 53274855
Device related infection 45.97 35.01 24 3212 22762 53323068
Angioedema 41.72 35.01 28 3208 42048 53303782
Poor venous access 40.35 35.01 17 3219 9958 53335872
Injection site erythema 38.20 35.01 34 3202 77215 53268615

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 1333.38 51.22 163 541 717 32512105
Injection site pain 54.40 51.22 22 682 33036 32479786
Inappropriate schedule of product administration 53.83 51.22 24 680 45801 32467021

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-adrenoceptor antagonists
CHEBI has role CHEBI:63175 peptidomimetics
CHEBI has role CHEBI:68557 bradykinin receptor antagonists

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hereditary angioneurotic edema indication 82966003 DOID:14735

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 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
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 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