Icatibant Injection

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Icatibant injection is an innovative drug specifically designed to treat acute episodes of hereditary angioedema (HAE). HAE is a rare and potentially life-threatening genetic disease, in which patients lack or have abnormal function of C1 esterase inhibitors, leading to overactivation of the kallikrein system and excessive production of bradykinin, which in turn causes vasodilation, increased permeability, and non pruritic edema in the skin, mucous membranes, and internal organs. Throat edema can even cause suffocation and be life-threatening. It is administered by subcutaneous injection and can be quickly absorbed into the bloodstream, quickly reaching the site of action. The drug competes with bradykinin to bind to the B ₂ receptor, blocking the biological effects of bradykinin, inhibiting downstream signaling pathways, reducing vasodilation and increased permeability, thereby rapidly alleviating edema symptoms.

Icatibant COA

Certificate of Analysis
Compound name	Icatibant
Grade	Pharmaceutical grade
CAS No.	130308-48-4
Quantity	50g
Packaging standard	PE bag+Al foil bag
Manufacturer	Shaanxi BLOOM TECH Co., Ltd
Lot No.	202512090051
MFG	Dec 9th 2025
EXP	Dec 8th 2028
Structure
Item	Enterprise standard	Analysis result
Appearance	White or almost white powder	Conformed
Water content	≤5.0%	0.32%
Loss on drying	≤1.0%	0.17%
Heavy Metals	Pb≤0.5ppm	N.D.
	As≤0.5ppm	N.D.
	Hg≤0.5ppm	N.D.
	Cd≤0.5ppm	N.D.
Purity (HPLC)	≥99.0%	99.8%
Single impurity	<0.8%	0.54%
Total microbial count	≤750cfu/g	90
E. Coli	≤2MPN/g	N.D.
Salmonella	N.D.	N.D.
Ethanol (by GC)	≤5000ppm	500ppm
Storage	Store in a sealed, dark, and dry place below 2-8°C

Icatibant injection is a selective antagonist targeting the bradykinin B ₂ receptor, with its core use focused on the treatment of acute episodes of Hereditary Angioedema (HAE) and potential application value in exploratory indications.

1. Disease mechanism and drug targets

 

HAE is a rare autosomal dominant genetic disease, with a global incidence rate of about 1:50000. The core pathological mechanism is the deficiency or abnormal function of C1 esterase inhibitor (C1-INH), which leads to excessive production of bradykinin. Bradykinin activates B ₂ receptors, causing vasodilation, increased vascular permeability, and release of inflammatory mediators, ultimately resulting in recurrent subcutaneous or submucosal non pruritic edema. Common sites include the face, limbs, genitals, gastrointestinal tract, and upper respiratory tract. Throat edema may cause suffocation and is the main cause of death in HAE.

 

As a potent selective antagonist of bradykinin B ₂ receptors, it competitively binds to B ₂ receptors to block the biological effects of bradykinin, thereby rapidly alleviating vasodilation, plasma extravasation, and inflammatory reactions, effectively reducing local tissue edema, pain, and inflammation. Its affinity is similar to that of bradykinin and it can resist degradation by bradykinin lyase. Its efficacy is 2-3 times higher than previous B ₂ receptor antagonists.

3. Application in special circumstances

 

(1) Laryngeal edema
Throat edema is the most dangerous complication of HAE, which may lead to suffocation. The patient needs to go to the emergency room immediately after injecting Icatibant to ensure airway patency.

 

(2) Preventive treatment
For patients with frequent episodes, Icatibant can be used before exposure to known triggering factors (such as specific foods, medications, emotional stress) to prevent episodes. In addition, it can be used in combination with Lanadelumab, a long-acting monoclonal antibody, or C1 INH replacement therapy such as Berinet ®) Combined use to form a combination strategy of "on-demand treatment+long-term prevention".

1. Acquired angioedema (AAE)

AAE is a non hereditary vascular edema with a pathogenesis different from HAE, but with similar clinical manifestations. Partial case reports indicate that it is effective against ACE inhibitor induced AAE. ACE inhibitors reduce angiotensin II production by inhibiting angiotensin-converting enzyme (ACE), while also inhibiting bradykinin degradation, leading to bradykinin accumulation and causing edema. Icatibant may become a potential therapeutic drug for AAE by blocking the action of bradykinin. However, the current evidence is limited and further large-scale clinical trials are needed for validation.

2. Capillary leakage syndrome

Capillary leakage syndrome is characterized by increased capillary permeability, leading to the infiltration of plasma proteins and fluids into tissue gaps, causing hypovolemic shock and multiple organ dysfunction. Bradykinin may play an important role in this process. Icatibant, as a B ₂ receptor antagonist, is expected to alleviate capillary leakage by blocking the bradykinin effect, but it is currently in the research stage and lacks clinical evidence to support it.

3. Pain management after myocardial infarction

Pain after myocardial infarction involves multiple inflammatory mediators and neurotransmitters, and bradykinin may be involved. Blocking the action of bradykinin may alleviate pain after myocardial infarction. However, currently only a few studies have explored its application in this field, and further research is needed to clarify its effectiveness and safety.

4. Other bradykinin mediated diseases

In theory, any disease with bradykinin overproduction as the pathological basis may become a potential indication for Icatibant. For example:
Rheumatoid arthritis: bradykinin may be involved in joint inflammation and pain.
Chronic pain syndrome: bradykinin is associated with neuropathic pain.
However, these applications are currently in the theoretical stage and lack clinical research support.

The core use of Icatibant injection is to treat acute attacks of HAE, which rapidly alleviates symptoms and significantly improves patients' quality of life by blocking bradykinin B ₂ receptors. In special populations, dose adjustment and monitoring strategies ensure the safety of treatment. Exploratory indications such as AAE and capillary leak syndrome have potential, but further research and verification are needed.

Icatibant is a selective bradykinin B ₂ receptor antagonist developed based on a deep understanding of the pathological mechanisms of hereditary angioedema (HAE). HAE is a rare autosomal dominant genetic disorder caused by a deficiency or dysfunction of C1 esterase inhibitor (C1-INH), leading to overproduction of bradykinin. Bradykinin activates B ₂ receptors, causing vasodilation, increased permeability, and inflammatory response, ultimately resulting in recurrent subcutaneous or submucosal edema, which can be life-threatening in severe cases (such as laryngeal edema).
By competitively binding to B ₂ receptors and blocking the biological effects of bradykinin, edema, pain, and inflammation can be rapidly relieved. Its molecular structure is similar to that of bradykinin, with high affinity (IC ₅₀ and Ki values of 1.07 nM and 0.798 nM, respectively), and it can resist degradation by bradykinin lyase, with significantly improved efficacy compared to previous generation antagonists.

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