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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

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 3723.29 24.51 648 7060 8717 90612022
Laryngeal oedema 227.93 24.51 62 7646 6819 90613920
Pharyngeal oedema 217.81 24.51 70 7638 13701 90607038
Pharyngeal swelling 196.79 24.51 60 7648 9884 90610855
Insurance issue 191.05 24.51 60 7648 10898 90609841
Inappropriate schedule of product administration 183.16 24.51 129 7579 149804 90470935
Product dose omission issue 143.94 24.51 149 7559 291538 90329201
No adverse event 141.62 24.51 82 7626 67900 90552839
Injection site pain 140.57 24.51 117 7591 173582 90447157
Product availability issue 118.52 24.51 38 7670 7366 90613373
Abdominal distension 118.31 24.51 94 7614 130507 90490232
Weight decreased 105.83 24.51 145 7563 379765 90240974
Weight increased 103.84 24.51 151 7557 417776 90202963
Stress 103.81 24.51 72 7636 81323 90539416
Swollen tongue 94.51 24.51 55 7653 45901 90574838
Prescribed overdose 83.53 24.51 68 7640 97557 90523182
Nonspecific reaction 82.32 24.51 23 7685 2786 90617953
Swelling face 81.07 24.51 62 7646 81290 90539449
Angioedema 63.65 24.51 49 7659 64827 90555912
Injection site erythema 58.91 24.51 56 7652 98446 90522293
Poor venous access 58.53 24.51 30 7678 19497 90601242
Hospitalisation 51.71 24.51 59 7649 128041 90492698
Product use issue 47.99 24.51 94 7614 329825 90290914
Therapy interrupted 47.30 24.51 37 7671 50071 90570668
Device related infection 43.02 24.51 27 7681 25759 90594980
COVID-19 41.73 24.51 61 7647 168782 90451957
Product distribution issue 39.44 24.51 14 7694 3691 90617048
Localised oedema 39.16 24.51 16 7692 6178 90614561
Product dose omission in error 38.10 24.51 23 7685 20480 90600259
Lip swelling 37.50 24.51 29 7679 38581 90582158
Injection site bruising 35.64 24.51 32 7676 52275 90568464
Supernumerary teeth 33.49 24.51 4 7704 0 90620739
Injection site swelling 31.97 24.51 32 7676 59807 90560932
Weight fluctuation 31.24 24.51 20 7688 19729 90601010
Mouth swelling 30.34 24.51 13 7695 5649 90615090
Therapy change 28.51 24.51 14 7694 8308 90612431
Drug intolerance 27.53 24.51 3 7705 447588 90173151
Laryngeal disorder 27.38 24.51 8 7700 1135 90619604
Unevaluable event 26.88 24.51 28 7680 54820 90565919
Infusion site pain 26.40 24.51 18 7690 19720 90601019
Vulvovaginal swelling 25.54 24.51 7 7701 789 90619950

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 1130.77 44.64 161 1439 1320 42618415
Angioedema 65.86 44.64 32 1568 42445 42577290
Weight increased 65.48 44.64 44 1556 107939 42511796
Injection site pain 64.84 44.64 35 1565 57763 42561972
Inappropriate schedule of product administration 55.53 44.64 38 1562 95864 42523871
Product use issue 53.10 44.64 34 1566 76717 42543018
Product availability issue 51.29 44.64 14 1586 3553 42616182
Insurance issue 44.83 44.64 13 1587 4103 42615632

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 3571.12 28.58 575 6322 6539 110575863
Pharyngeal oedema 193.67 28.58 62 6835 16366 110566036
Insurance issue 193.42 28.58 56 6841 10556 110571846
Product dose omission issue 177.10 28.58 152 6745 321630 110260772
Laryngeal oedema 170.97 28.58 50 6847 9757 110572645
Injection site pain 163.44 28.58 114 6783 177808 110404594
Inappropriate schedule of product administration 160.79 28.58 119 6778 203518 110378884
Weight increased 139.19 28.58 150 6747 419494 110162908
Product availability issue 132.14 28.58 39 6858 7851 110574551
Weight decreased 111.17 28.58 141 6756 467916 110114486
No adverse event 101.44 28.58 61 6836 73778 110508624
Angioedema 87.70 28.58 62 6835 98438 110483964
Stress 77.28 28.58 59 6838 105289 110477113
Product use issue 77.19 28.58 96 6801 311599 110270803
Prescribed overdose 68.55 28.58 51 6846 87530 110494872
Injection site erythema 60.96 28.58 49 6848 94127 110488275
Pharyngeal swelling 59.96 28.58 24 6873 12008 110570394
Swollen tongue 58.39 28.58 40 6857 60322 110522080
Product dose omission in error 56.10 28.58 28 6869 23484 110558918
Localised oedema 55.15 28.58 21 6876 9202 110573200
Injection site bruising 47.29 28.58 33 6864 51230 110531172
Expired product administered 46.38 28.58 18 6879 8302 110574100
COVID-19 41.68 28.58 63 6834 244997 110337405
Poor venous access 40.91 28.58 23 6874 24499 110557903
Therapy interrupted 38.93 28.58 29 6868 49793 110532609
Abdominal distension 38.64 28.58 51 6846 175052 110407350
Hospitalisation 38.62 28.58 46 6851 142447 110439955
Swelling face 35.81 28.58 36 6861 92285 110490117
Off label use 34.61 28.58 184 6713 1500001 109082401
Product distribution issue 33.77 28.58 12 6885 4334 110578068
Body height increased 32.26 28.58 6 6891 158 110582244
Influenza 29.48 28.58 44 6853 169057 110413345
Injection site swelling 29.46 28.58 27 6870 61763 110520639

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 D000893 Anti-Inflammatory Agents
MeSH PA D000894 Anti-Inflammatory Agents, Non-Steroidal
MeSH PA D007155 Immunologic Factors
MeSH PA D007166 Immunosuppressive Agents
MeSH PA D018373 Peripheral Nervous System Agents
MeSH PA D018501 Antirheumatic Agents
MeSH PA D018689 Sensory System Agents
MeSH PA D018712 Analgesics, Non-Narcotic
MeSH PA D051056 Complement Inactivating Agents
MeSH PA D065094 Bradykinin B2 Receptor Antagonists
MeSH PA D065168 Bradykinin Receptor Antagonists
FDA MoA N0000182964 Bradykinin B2 Receptor Antagonists
FDA EPC N0000182965 Bradykinin B2 Receptor Antagonist
CHEBI has role CHEBI:35530 β-adrenergic antagonist
CHEBI has role CHEBI:63175 peptidomimetic
CHEBI has role CHEBI:68557 bradykinin receptor antagonist

Related Drugs by ATC class:

B06AC Drugs used in hereditary angioedema 7 drugs
berotralstatconestat alfadonidalorsenecallantidegaradacimablanadelumabsebetralstat

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 28 sections
Icatibant HUMAN PRESCRIPTION DRUG LABEL 1 24201-207 INJECTION, SOLUTION 30 mg SUBCUTANEOUS ANDA 29 sections
Icatibant Human Prescription Drug Label 1 46708-654 INJECTION 30 mg SUBCUTANEOUS ANDA 27 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 62332-654 INJECTION 30 mg SUBCUTANEOUS ANDA 27 sections
Icatibant HUMAN PRESCRIPTION DRUG LABEL 1 63323-574 INJECTION, SOLUTION 10 mg SUBCUTANEOUS ANDA 32 sections
ICATIBANT HUMAN PRESCRIPTION DRUG LABEL 1 69097-664 INJECTION 30 mg SUBCUTANEOUS ANDA 26 sections
SAJAZIR HUMAN PRESCRIPTION DRUG LABEL 1 70709-013 INJECTION 30 mg SUBCUTANEOUS ANDA 26 sections