Icatibant Acetate is a synthetic bradykinin B2 receptor antagonist and peptide-based active pharmaceutical ingredient used in the treatment of acute attacks of hereditary angioedema. It is the acetate salt of icatibant, a synthetic decapeptide structurally related to bradykinin.
Icatibant Acetate has the molecular formula C59H91N19O16·C2H4O2 and a molecular weight of approximately 1320.53 g/mol. The CAS Number commonly associated with Icatibant Acetate is 138614-30-9.
Icatibant is a synthetic decapeptide designed to selectively block the bradykinin B2 receptor. Bradykinin is an important mediator in the pathophysiology of hereditary angioedema, where excessive bradykinin activity contributes to increased vascular permeability and swelling.
Icatibant Acetate is therefore an important peptide API for pharmaceutical formulations intended for the acute treatment of hereditary angioedema attacks.
Icatibant selectively antagonizes the bradykinin B2 receptor.
By blocking bradykinin from binding to this receptor, icatibant reduces bradykinin-mediated vasodilation and increased vascular permeability, thereby helping reduce the swelling associated with acute hereditary angioedema attacks.
Icatibant Acetate API is used in the development and manufacture of:
Icatibant Acetate is a synthetic peptide API manufactured using controlled peptide-synthesis processes followed by purification, typically involving chromatographic purification and controlled isolation of the acetate salt.
Because it is a peptide, quality evaluation requires comprehensive analytical characterization. Testing may include identity, peptide purity, related peptides, water content, acetate content, residual solvents, elemental impurities and other applicable quality attributes.
Icatibant Acetate is generally supplied as a white to off-white powder. As a peptide acetate salt, it is soluble in water and suitable for preparation of aqueous pharmaceutical formulations.
Icatibant Acetate should be stored according to the manufacturer's validated stability requirements, generally in a tightly closed container under controlled temperature conditions, protected from excessive moisture and direct light.
Depending on the intended pharmaceutical application, documentation may include:
Icatibant Acetate is a synthetic decapeptide API and selective bradykinin B2 receptor antagonist. Its targeted inhibition of bradykinin signaling makes it an important pharmaceutical ingredient for products used in the acute treatment of hereditary angioedema.
| Parameter | Specification |
|---|---|
| Appearance | White to off-white crystalline powder |
| Identification | IR & HPLC compliant |
| Assay (HPLC) | 95.0% – 105.0% |
| Loss on Drying | NMT 2.0% |
| Residue on Ignition | NMT 0.5% |
| pH (1% Solution) | 4.0 – 6.0 |
| Individual Impurity | NMT 0.5% |
| Total Impurities | NMT 2.0% |
| Water Content | NMT 2.0% |