Icatibant Acetate

The active pharmaceutical ingredient icatibant in Icatibant acetate salt form is a chemically modified version of icatibant designed to meet formulation requirements, with the two forms being completely equivalent in clinical efficacy. This conclusion is grounded in the core logic of drug development, which involves the adaptation between the "active ingredient" and the "pharmaceutical dosage form," as well as the optimization of the physicochemical properties of the drug through salt formation. As a synthetically produced decapeptide compound, the free base form of it contains multiple basic amino groups in its molecular structure. However, due to the steric hindrance of peptide bonds and the polarity distribution of the molecule, its water solubility is poor, making it difficult to directly formulate into injectable preparations commonly used in clinical practice. In drug development, injection is the preferred route of administration for emergency medications treating hereditary angioedema (HAE)-addressing the clinical need for "rapid absorption and quick onset of action," where water solubility is a fundamental prerequisite for formulation development. Its acetate is designed precisely to meet this requirement by forming a stable salt compound between the free base of it and acetic acid molecules through ionic bonding. This chemical modification does not alter the core peptide chain structure of icatibant. Instead, by introducing acetate ions, the hydrophilicity of the molecule is significantly enhanced, enabling its dissolution in injection solvents. This allows for the preparation of a lyophilized powder for subcutaneous injection, thereby meeting the basic requirements for clinical administration.

 

Our Products Form

 

Icatibant peptide

Icatibant injection

Icatibant Acetate

Icatibant Acetate COA

Certificate of Analysis
Compound name	Icatibant Acetate
Grade	Pharmaceutical grade
CAS No.	138614-30-9
Quantity	40g
Packaging standard	PE bag+Al foil bag
Manufacturer	Shaanxi BLOOM TECH Co., Ltd
Lot No.	202501090089
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

Whether it is icatibant free base or icatibant acetate, the same molecule ·exerts the pharmacological effect-its binding affinity to the bradykinin B₂ receptor, its mechanism of action as a competitive antagonist, and its pharmacological effect of inhibiting increased vascular permeability are entirely identical. In clinical studies, this acetate shows no statistically significant differences compared to the theoretical this drug free base in terms of onset of action (symptom relief within 15–30 minutes after administration), duration of efficacy, or adverse reaction profile. This serves as direct evidence of their clinical equivalence. Furthermore, as a weak acid, acetate forms salts that exhibit lower irritation to local human tissues after injection, reducing the incidence of adverse reactions such as injection site pain and redness. This further enhances the clinical applicability of the drug.

Therefore, this drug is not a completely new drug molecule but a rationally designed chemical modification of it to meet clinical formulation needs. The two share the same core active ingredient and mechanism of action, ultimately achieving complete equivalence in clinical efficacy and safety.

Icatibant is not a conventional first-line drug for asthma treatment. Its potential role in asthma is based on its core mechanism of blocking the bradykinin B₂ receptor, making it suitable only for specific pathological subtypes of asthma. The specific characteristics of its action are detailed below:

(I)Targeting the Bradykinin-Mediated Pathway in Asthma Pathogenesis

 

The processes of airway inflammation and bronchospasm in asthma involve various inflammatory mediators, among which bradykinin is a significant pro-inflammatory factor. It can directly stimulate airway smooth muscle contraction, promote increased vascular permeability in the airway submucosa (leading to mucosal exudation and edema, which worsens airway narrowing), and induce the infiltration of inflammatory cells such as eosinophils into the airways, thereby amplifying the inflammatory response.

By competitively binding to bradykinin B₂ receptors on airway smooth muscle cells and vascular endothelial cells, Icatibant acetate blocks the binding of endogenous bradykinin to these receptors. This action inhibits the aforementioned pathological processes at their source, thereby reducing the degree of bronchospasm, decreasing mucosal exudation, and alleviating symptoms such as wheezing, chest tightness, and dyspnea in patients.

This pathway of action does not affect targets commonly used in asthma treatment, such as adrenergic receptors or glucocorticoid receptors, and does not overlap with the mechanisms of conventional asthma medications.

(II)Applicability to Specific Asthma Subtypes with Abnormal Bradykinin Pathway Activation

(III)Limitations and Principles of Use in Asthma Applications

Lack of extensive clinical evidence

The core indication for it is hereditary angioedema. Its use in asthma is primarily based on small-scale clinical studies and case reports, and it has not been incorporated into mainstream asthma treatment guidelines. Therefore, it should not be used as a routine or first-choice medication for asthma.

Route of administration limits use in emergency settings

Icatibant acetate is primarily administered via subcutaneous injection. While it has a relatively rapid onset of action, its convenience of use is inferior to nebulized formulations commonly employed for asthma emergencies. It is not suitable for the immediate, on-site management of severe acute asthma attacks requiring instant relief.

Requirement for strict safety monitoring

During treatment, patient airway function parameters (e.g., FEV1) and systemic responses should be monitored. Concomitant use with other vasoactive drugs should be avoided to prevent blood pressure fluctuations. Injection site reactions (pain, redness) generally do not affect airway function but should be differentiated from symptoms of asthma exacerbation.

Icatibant is not a conventional therapeutic agent for acute pancreatitis. Its potential role in this condition is based on its core mechanism as a bradykinin B₂ receptor antagonist, targeting specific pathological stages of acute pancreatitis to exert adjunctive therapeutic effects. The detailed characteristics of its action are as follows:

Targeted Modulation of the Local Inflammatory Cascade in Acute Pancreatitis

The core pathological process of acute pancreatitis involves damage to pancreatic acinar cells, which triggers the release of substantial amounts of bradykinin. This mediator can directly induce increased vascular permeability in the pancreas and surrounding tissues, leading to pancreatic interstitial edema and congestion. Simultaneously, it promotes the release of pro-inflammatory factors such as tumor necrosis factor and interleukins, amplifying the local inflammatory response and thereby exacerbating ischemia and necrosis of pancreatic tissue.

This competitively binds to the bradykinin B₂ receptors on pancreatic parenchymal cells and interstitial vascular endothelial cells, blocking the binding of endogenous bradykinin to these receptors. This action inhibits the aforementioned pathological processes at their source, reducing the degree of local congestion and edema in the pancreas, decreasing the infiltration and spread of inflammatory factors to surrounding tissues, and delaying the progression of pancreatic tissue from edema to necrosis.

This pathway of action targets only the bradykinin-mediated inflammatory pathway. It does not affect pancreatic secretory function nor interfere with the effects of conventional treatments such as inhibiting pancreatic enzyme activity or fluid resuscitation.

Applicability in Adjunctive Scenarios for Specific Types of Acute Pancreatitis

 

• For early-stage severe acute pancreatitis:A critical juncture in the progression of severe acute pancreatitis is microcirculatory dysfunction within the first 48 hours of onset. During this period, excessive activation of the bradykinin pathway exacerbates insufficient pancreatic perfusion. Icatibant may serve as an adjunctive therapy alongside fluid resuscitation and vasoactive drugs to improve local pancreatic microcirculation and reduce the risk of multiple organ dysfunction syndrome.
• For moderate acute pancreatitis with increased local exudation: In some patients with moderate acute pancreatitis, pancreatic exudation continues to increase despite foundational treatments such as fasting, acid suppression, and inhibition of pancreatic enzyme secretion, often accompanied by unrelieved abdominal pain. In such cases, it can be used in combination to block bradykinin-mediated exudative responses, accelerate the absorption of peritoneal fluid, and shorten the duration of abdominal pain and hospitalization.

• For non-biliary, non-alcoholic acute pancreatitis:The triggers for this type of pancreatitis are often more closely associated with abnormal inflammatory responses, and the involvement of bradykinin pathway activation is more significant. Therefore, the targeted intervention with this can more precisely address the core pathological mechanisms, potentially yielding more substantial benefits compared to other types of pancreatitis.

• What is icatibant acetate used for?

Icatibant injection is used to treat sudden attacks of hereditary angioedema (HAE). Icatibant works by blocking a chemical in the body that causes swelling, inflammation, and pain for patients with HAE. This medicine is not a cure for HAE. This medicine is available only with your doctor's prescription.

• What should I tell my doctor before taking icatibant?

Before using icatibant,ask your pharmacist for a list of the ingredients. tell your doctor and pharmacist what prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. you should know that icatibant may make you drowsy.

Hot Tags: icatibant acetate, China icatibant acetate manufacturers, suppliers, Botulinum Toxin Injection 100iu, Nad Capsule, Nad Peptide Injection, Nad Tablet, BPC 157 Peptide Cream, BPC 157 Peptide Capsules