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 2448.29 25.59 448 5643 7114 63475817
Laryngeal oedema 217.83 25.59 59 6032 5659 63477272
Inappropriate schedule of product administration 214.95 25.59 130 5961 103835 63379096
Pharyngeal oedema 213.85 25.59 71 6020 13650 63469281
Prescribed overdose 166.65 25.59 76 6015 34077 63448854
Pharyngeal swelling 140.44 25.59 43 6048 6361 63476570
Product dose omission issue 130.54 25.59 135 5956 234178 63248753
Injection site pain 129.88 25.59 104 5987 129696 63353235
Product availability issue 126.91 25.59 36 6055 4085 63478846
No adverse event 123.77 25.59 66 6025 41339 63441592
Swollen tongue 78.15 25.59 46 6045 34754 63448177
Abdominal distension 77.28 25.59 65 6026 86550 63396381
COVID-19 75.41 25.59 72 6019 113031 63369900
Insurance issue 69.42 25.59 25 6066 6096 63476835
Stress 54.97 25.59 48 6043 67119 63415812
Hospitalisation 54.48 25.59 53 6038 85028 63397903
Injection site erythema 53.61 25.59 52 6039 83122 63399809
Localised oedema 50.06 25.59 19 6072 5359 63477572
Swelling face 47.25 25.59 43 6048 63432 63419499
Device related infection 44.97 25.59 28 6063 23364 63459567
Angioedema 44.82 25.59 37 6054 47928 63435003
Poor venous access 42.53 25.59 23 6068 14762 63468169
Weight decreased 36.13 25.59 81 6010 276717 63206214
Supernumerary teeth 33.01 25.59 4 6087 0 63482931
Nonspecific reaction 32.27 25.59 11 6080 2281 63480650
Injection site swelling 31.11 25.59 30 6061 47542 63435389
Expired product administered 30.87 25.59 14 6077 6167 63476764
COVID-19 immunisation 30.84 25.59 10 6081 1777 63481154
Pregnancy 29.46 25.59 26 6065 36810 63446121
Product distribution issue 28.88 25.59 9 6082 1407 63481524
Weight increased 27.21 25.59 70 6021 260722 63222209
Therapy interrupted 26.14 25.59 23 6068 32432 63450499
Unevaluable event 25.61 25.59 28 6063 51358 63431573

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 767.60 40.48 110 1205 937 34954679
Inappropriate schedule of product administration 67.90 40.48 37 1278 62259 34893357
Product availability issue 65.46 40.48 15 1300 1872 34953744
Injection site pain 50.44 40.48 26 1289 38979 34916637
Prescribed overdose 43.50 40.48 16 1299 10631 34944985
Angioedema 42.87 40.48 23 1292 37351 34918265
Weight increased 42.63 40.48 32 1283 93001 34862615
Product dose omission issue 41.63 40.48 35 1280 119676 34835940

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 2148.63 27.59 360 4890 4975 79734163
Pharyngeal oedema 195.12 27.59 63 5187 16209 79722929
Inappropriate schedule of product administration 190.49 27.59 115 5135 133513 79605625
Laryngeal oedema 164.08 27.59 47 5203 8082 79731056
Product availability issue 161.87 27.59 40 5210 3907 79735231
Product dose omission issue 149.17 27.59 126 5124 247411 79491727
Injection site pain 143.04 27.59 95 5155 129743 79609395
Prescribed overdose 111.73 27.59 53 5197 37830 79701308
No adverse event 103.49 27.59 50 5200 37142 79701996
COVID-19 80.15 27.59 73 5177 157601 79581537
Localised oedema 64.57 27.59 23 5227 7929 79731209
Weight increased 56.81 27.59 80 5170 277306 79461832
Angioedema 56.79 27.59 44 5206 75991 79663147
Swollen tongue 48.81 27.59 32 5218 42538 79696600
Injection site erythema 47.27 27.59 40 5210 78157 79660981
Expired product administered 44.70 27.59 17 5233 7034 79732104
Insurance issue 44.35 27.59 16 5234 5717 79733421
Body height increased 39.20 27.59 7 5243 138 79739000
Weight decreased 38.42 27.59 77 5173 355121 79384017
Hospitalisation 37.17 27.59 38 5212 94198 79644940
COVID-19 immunisation 36.98 27.59 10 5240 1389 79737749
Stress 36.78 27.59 35 5215 79577 79659561
Pharyngeal swelling 36.30 27.59 15 5235 7704 79731434
Product use issue 33.59 27.59 54 5196 209768 79529370
Pregnancy 27.92 27.59 19 5231 26832 79712306

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 ANTAGONIST Ki 9.60 IUPHAR
B2 bradykinin receptor GPCR Ki 10.11 CHEMBL
B2 bradykinin receptor GPCR Ki 9.96 CHEMBL
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 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 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
Firazyr HUMAN PRESCRIPTION DRUG LABEL 1 54092-702 INJECTION, SOLUTION 30 mg SUBCUTANEOUS NDA 34 sections
Icatibant Human Prescription Drug Label 1 55150-351 INJECTION, SOLUTION 30 mg SUBCUTANEOUS ANDA 28 sections
ICATIBANT HUMAN PRESCRIPTION DRUG LABEL 1 60505-6214 INJECTION, SOLUTION 30 mg SUBCUTANEOUS ANDA 29 sections
ICATIBANT HUMAN PRESCRIPTION DRUG LABEL 1 60505-6214 INJECTION, SOLUTION 30 mg SUBCUTANEOUS ANDA 29 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
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
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