Icatibant Injection

Icatibant injection, a synthetic, highly selective peptidomimetic bradykinin B₂ receptor antagonist, is specifically designed to target and competitively inhibit the binding of endogenous bradykinin to its cognate B₂ receptor with high affinity and specificity. Unlike non-specific anti-edematous agents that only alleviate symptoms superficially, it acts by directly interrupting the ligand-receptor interaction, thereby rapidly blocking the final common pathway that leads to increased vascular permeability and tissue edema in HAE acute attacks. Through this precise mechanism of action, icatibant can quickly reverse the bradykinin-mediated pathological effects, including the disruption of endothelial cell junctions and the extravasation of fluid into interstitial spaces. As a result, it can reduce the severity of tissue edema within a short period (typically within 30 minutes to several hours after administration) and effectively relieve the full spectrum of acute HAE symptoms, ranging from cutaneous swellings and gastrointestinal distress to life-threatening upper airway obstruction. Administered via subcutaneous injection, it offers the advantages of rapid absorption, predictable pharmacokinetic profiles, and a favorable safety profile with minimal off-target effects. In clinical practice, it serves as a first-line rescue therapy for HAE acute attacks, providing patients with timely, targeted, and life-saving therapeutic intervention to mitigate acute symptoms and prevent potentially catastrophic complications.

 

Our Products Description

 

Icatibant peptide

Icatibant injection

Icatibant Acetate

Icatibant COA

Certificate of Analysis
Compound name	Icatibant
Grade	Pharmaceutical grade
CAS No.	130308-48-4
Quantity	40g
Packaging standard	PE bag+Al foil bag
Manufacturer	Shaanxi BLOOM TECH Co., Ltd
Lot No.	202501090088
MFG	Jan 9th 2025
EXP	Jan 8th 2028
Structure
Item	Enterprise standard	Analysis result
Appearance	White or almost white powder	Conformed
Water content	≤5.0%	0.54%
Loss on drying	≤1.0%	0.42%
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%	99.97%
Single impurity	<0.8%	0.52%
Total microbial count	≤750cfu/g	95
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 -20°C

Hereditary angioedema (HAE) is a rare autosomal dominant disorder, with acute attacks clinically characterized by excessive bradykinin accumulation as the core initiating pathological event. Unlike the transient fluctuations of bradykinin under normal physiological conditions, this sudden and unregulated surge of bradykinin triggers a series of pro-edema biological responses. Its primary mechanism of action involves disrupting the balance between vasoconstriction and vasodilation, directly leading to a rapid and abnormal increase in vascular endothelial permeability.

This pathological alteration in vascular permeability allows plasma components and interstitial fluid to leak into surrounding tissues, resulting in localized non-pitting edema. The most commonly affected sites include the skin, gastrointestinal tract, and upper respiratory tract. Among them, cutaneous edema typically presents as well-demarcated, painful swelling that may involve the face, limbs, or trunk; gastrointestinal edema is often accompanied by severe abdominal pain, nausea, vomiting, and diarrhea, making it easily misdiagnosed as an acute abdominal condition; the most dangerous manifestation is upper respiratory tract edema-particularly laryngeal edema-which can rapidly lead to airway obstruction and subsequent respiratory failure. Icatibant injection provides precise therapeutic intervention for this condition.

As a highly selective bradykinin B ₂ receptor antagonist, Icatibant's core logic for alleviating edema in different parts of the body is to competitively block the binding of bradykinin to B ₂ receptors on target tissue vascular endothelium and smooth muscle cells, inhibiting vascular dilation and increased permeability, thereby reducing interstitial fluid accumulation. However, due to the different anatomical structures and physiological functions of the skin, intestines, and upper respiratory tract, there are significant differences in the relief process and clinical effects.

Cutaneous edema is the most common type of hereditary angioedema (HAE) attack, frequently involving the extremities, trunk, face, or genitalia.

(II)Relief Process and Characteristics

Rapid Onset

Following subcutaneous injection, Icatibant injection is rapidly absorbed into the bloodstream via subcutaneous capillaries. It binds to target receptors in the skin within 15-30 minutes, blocking the ongoing effects of bradykinin. Initial relief of the tightness and burning sensation at the edema site is often observed first.

Pattern of Resolution

For mild to moderate cutaneous edema, the swelling typically begins to reduce within 1-2 hours after administration, with significant improvement seen within 4-6 hours. Complete resolution of severe edema (e.g., involving the face or genitalia) may require 12-24 hours. Importantly, it does not leave post-inflammatory hyperpigmentation or tissue fibrosis.

High Specificity

It specifically inhibits bradykinin-mediated edema and is ineffective against skin swelling caused by allergies (histamine-mediated) or infections. This differential efficacy can aid in the differential diagnosis of HAE.

Intestinal edema is the type of HAE acute attack most prone to misdiagnosis. The lesions primarily involve the submucosa of the small intestine, with some cases extending to the colon.

(I)Mechanism of Action

It targets the B₂ receptors on vascular endothelial cells and smooth muscle cells in the intestinal submucosa. The intestinal submucosa has a dense vascular network and a well-developed smooth muscle layer. In addition to increasing vascular permeability and causing edema, bradykinin also stimulates smooth muscle spasms, thereby triggering severe abdominal pain.

(II)Significant Advantage in Shortening Disease Course

Traditional antispasmodics (e.g., pinaverium bromide) only provide temporary pain relief and cannot halt edema progression, allowing intestinal attacks to last 2-5 days. In contrast, it can shorten the disease course to 1-2 days and helps prevent complications like dehydration and electrolyte imbalances caused by severe vomiting and diarrhea.

(III)Clinical Significance

The symptoms of an intestinal edema attack highly resemble those of acute abdominal conditions (e.g., appendicitis, intestinal obstruction), easily leading to unnecessary surgical interventions. The rapid pain relief and edema resolution provided by Icatibant can assist clinicians in quickly differentiating HAE intestinal attacks from surgical acute abdomen, thereby reducing the risk of misdiagnosis and inappropriate treatment.

(IV)Relief Process and Characteristics

Pain Relief Precedes Edema Resolution:

Unlike the sequence observed in cutaneous edema, the effect of Icatibant injection on intestinal edema first manifests as the relief of smooth muscle spasms. After binding to B₂ receptors on smooth muscle cells, the drug rapidly inhibits bradykinin-induced intestinal hypermotility and spasms. Most patients experience significant reduction or complete cessation of paroxysmal abdominal colic within 30-60 minutes after administration.

Edema Resolution Accompanies Restoration of Digestive Function:

The resolution of intestinal mucosal edema is slightly slower than pain relief. Typically, within 2-4 hours after administration, vascular permeability in the submucosa normalizes, intestinal wall edema decreases, and symptoms such as nausea, vomiting, diarrhea, and bloating gradually subside. Complete restoration of normal intestinal motility and absorption function usually requires 8-12 hours.

Upper respiratory tract edema is the most critical type of HAE attack, involving the pharynx, larynx, and upper trachea. In severe cases, it can lead to airway obstruction and suffocation.

 

 

It targets the B₂ receptors on submucosal blood vessels and tracheal smooth muscle cells in the upper respiratory tract. The submucosal tissue in this area is loose and highly vascularized. Bradykinin-mediated increase in vascular permeability rapidly causes mucosal swelling, compressing the airway. Simultaneously, bradykinin stimulates tracheal smooth muscle contraction, further narrowing the airway.

Emergency-Level Onset

For life-threatening attacks like laryngeal edema, this drug administered via subcutaneous injection can bind to target receptors within 15 minutes, halting edema progression. It first alleviates prodromal symptoms such as throat tightness, hoarseness, and dysphagia, preventing the spread of edema to the glottis.

Dual Mechanism of Action

It not only blocks increased vascular permeability to reduce mucosal edema but also inhibits tracheal smooth muscle spasms, alleviating symptoms like wheezing and dyspnea, achieving a dual emergency effect of "edema reduction + spasm relief."

Requirement for Combined Airway Support

For patients with severe airway narrowing, Icatibant should be used in conjunction with airway support measures such as endotracheal intubation or cricothyrotomy. While the drug takes time to resolve edema, airway support ensures patient ventilation during the critical intervention window, reducing mortality.

Short Treatment Course

The relief of upper respiratory tract edema is "non-recurrent." Once the drug blocks bradykinin's effects, the edema does not recur. Most patients achieve complete restoration of airway function within 6-12 hours after administration.

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