Icatibant

Bradykinin B2 Receptor Antagonist — BLOOD AND BLOOD FORMING ORGANS

Key facts

Icatibant is a drug in the Bradykinin B2 Receptor Antagonist class catalogued in DrugCentral. It was first approved by the EMA in 2008. Its mechanism of action is classified as Bradykinin B2 Receptor Antagonists. DrugCentral lists 6 molecular targets, including BDKRB2, Bdkrb2 and BDKRB2. Recorded indications include Hereditary angioneurotic edema.

• Drug class: Bradykinin B2 Receptor Antagonist.
• Mechanism of action: Bradykinin B2 Receptor Antagonists.
• Molecular targets: BDKRB2, Bdkrb2, BDKRB2 and Bdkrb2 (6 listed in DrugCentral).
• Indications: Hereditary angioneurotic edema.
• ATC code: B06AC02 (Drugs used in hereditary angioedema).
• Molecular formula: C59H89N19O13S; molecular weight 1304.54 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (1)

• Hereditary angioneurotic edema

Mechanism & targets

• Mechanism of action (MoA): Bradykinin B2 Receptor Antagonists
• Established pharmacologic class: Bradykinin B2 Receptor Antagonist

Molecular targets (6)

Target	Gene	Action	Activity
B2 bradykinin receptor	BDKRB2	antagonist	Ki 10.22
B2 bradykinin receptor	Bdkrb2	unknown	Ki 10.11
B2 bradykinin receptor	BDKRB2	unknown	Ki 9.96
B2 bradykinin receptor	Bdkrb2	antagonist	Ki 9.60
B1 bradykinin receptor	BDKRB1	antagonist	Ki 7.00
B1 bradykinin receptor	Bdkrb1	antagonist	Ki 6.40

Regulatory approvals (3)

Date	Agency	Marketed as	Applicant	Orphan
2018-09-21	PMDA	—	Shire Japan KK	Yes
2011-08-25	FDA	—	SHIRE ORPHAN THERAP	Yes
2008-07-11	EMA	—	Shire Pharmaceuticals Ireland Limited	Yes

ATC classification

ATC code	Therapeutic hierarchy
B06AC02	BLOOD AND BLOOD FORMING ORGANS › OTHER HEMATOLOGICAL AGENTS › OTHER HEMATOLOGICAL AGENTS › Drugs used in hereditary angioedema

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Hereditary angioedema	5393.8
Pharyngeal swelling	385.3
Laryngeal oedema	296.4
Pharyngeal oedema	251.6
Insurance issue	233.7
Injection site pain	225.2
Inappropriate schedule of product administration	203.5
Product dose omission issue	191.1
No adverse event	181.4
Product availability issue	180.1
Weight increased	149.6
Angioedema	129.5

Chemical structure

Full physicochemical, ADMET and 3D-structure analysis of Icatibant is on its molecule page.

• Molecular formula: C₅₉H₈₉N₁₉O₁₃S
• Molecular weight: 1304.54 g/mol
• CAS number: 130308-48-4
• InChIKey: QURWXBZNHXJZBE-SKXRKSCCSA-N
• PubChem CID: 6918173

N[C@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N1CCC[C@H]1C(=O)N1C[C@H](O)C[C@H]1C(=O)NCC(=O)N[C@@H](CC1=CC=CS1)C(=O)N[C@@H](CO)C(=O)N1CC2=C(C[C@@H]1C(=O)N1[C@H]3CCCC[C@H]3C[C@H]1C(=O)N[C@@H](CCCNC(N)=N)C(O)=O)C=CC=C2

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Icatibant used for?

DrugCentral lists the following indications for Icatibant: Hereditary angioneurotic edema.

How does Icatibant work?

Icatibant is classified as Bradykinin B2 Receptor Antagonists; its molecular targets in DrugCentral include BDKRB2 (antagonist), Bdkrb2, BDKRB2 and Bdkrb2 (antagonist).

When was Icatibant first approved?

Icatibant was first approved by the EMA in 2008.

What drug class does Icatibant belong to?

Icatibant is in the Bradykinin B2 Receptor Antagonist class.

What is the chemical formula of Icatibant?

Icatibant has the molecular formula C59H89N19O13S and a molecular weight of 1304.54 g/mol.

Sources

• DrugCentral drug card 4186 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL2028850 — compound record and bioactivity
• PubChem CID 6918173 — chemical identifiers
• DrugBank DB06196 — drug record
• FDA UNII 7PG89G35Q7 — substance identity
• DailyMed: FDA labels for Icatibant — current prescribing information (label search)
• UniProt P30411 (BDKRB2) — target protein
• UniProt P46663 (BDKRB1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.