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

Stem definition	Drug id	CAS RN
bradykinin receptors antagonists	4186	130308-48-4

Description:

Molecule

Description

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:

Dose	Unit	Route
30	mg	P

ADMET properties:

None

Approvals:

Date	Agency	Company	Orphan
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients 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:

Source	Code	Description
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)

Disease	Relation	SNOMED_ID	DOID
Hereditary angioneurotic edema	indication	82966003	DOID:14735

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
B2 bradykinin receptor	GPCR	P30411	BKRB2_HUMAN	ANTAGONIST	Ki	10.22		CHEMBL	CHEMBL
B1 bradykinin receptor	GPCR	P46663	BKRB1_HUMAN	ANTAGONIST	Ki	7		IUPHAR
B2 bradykinin receptor	GPCR		BKRB2_RAT		Ki	10.11		CHEMBL
B2 bradykinin receptor	GPCR		BKRB2_CAVPO		Ki	9.96		CHEMBL
B2 bradykinin receptor	GPCR		BKRB2_MOUSE	ANTAGONIST	Ki	9.60		IUPHAR
B1 bradykinin receptor	GPCR		BKRB1_RAT	ANTAGONIST	Ki	6.40		IUPHAR

External reference:

ID	Source
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:

Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
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