icatibant 🐶 Veterinary Use | 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: -3.47
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	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 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	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 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	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:

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-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|

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

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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	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