General Information

Icatibant Impurities and Icatibant

Daicel Pharma synthesizes high-quality Icatibant impurities, (1-6)-Icatibant, (7-10)-Icatibant, Ac-Icatibant, Des-D-Arg(1)-Icatibant, Des-L-Arg(2)-Icatibant, and L-Arg(1)-Icatibant, that help in the quality, stability, and biological safety analysis of Icatibant. We also offer custom synthesis of Icatibant impurities and supply worldwide.

Icatibant [CAS: 130308-48-4] is a synthetic peptidomimetic consisting of ten amino acids, which is a selective and specific antagonist of bradykinin B2 receptors. It is used for the symptomatic treatment of acute attacks of hereditary angioedema (HAE) in adults with C1-esterase-inhibitor deficiency.

Icatibant: Use and Commercial Availability 

Icatibant, a drug, is a competitive antagonist selective for bradykinin B2 receptor (B2R), and commonly prescribed to treat acute attacks of swelling and inflammation in individuals with hereditary angioedema (HAE). It is under research for its potential to treat angioedema, joint disease, and chronic kidney disease. Icatibant is marketed under the brand names Firazyr and Sajazir.

Icatibant Structure and Mechanism of Action

The chemical formula for Icatibant is C₅₉H₈₉N₁₉O₁₃ and its molecular weight is approximately 1304.5 g/mol.

A C1-esterase inhibitor is the main regulator of the Factor XII I/kallikrein proteolytic cascade that leads to bradykinin production. The absence or dysfunction of a C1-esterase inhibitor causes Hereditary angioedema (HAE).  Bradykinin is responsible for the characteristic HAE symptoms of localized swelling, inflammation, and pain. Icatibant prevents bradykinin from binding the B2 receptors and treats acute attacks of HAE.

Icatibant Impurities and Synthesis

Icatibant is synthesized¹ from the protected L- and D- amino acids and protected glycine. The synthesis is by a solid phase peptide synthesis (SPPS) process. Icatibant may contain impurities² such as related peptide impurities, organic impurities, residual solvents, and degradation products. These impurities must be monitored and controlled during the manufacturing process to ensure that the final product meets the quality standards.

At Daicel, we provide a Certificate of Analysis (CoA) from a cGMP-compliant analytical facility for Icatibant impurity standards, (1-6)-Icatibant, Icatibant (7-10), Ac-Icatibant, Des-D-Arg(1)-Icatibant, Des-L-Arg(2)-Icatibant, and L-Arg(1)-Icatibant, along with complete characterization data including 1H NMR, 13C NMR, IR, MASS, and HPLC purity. Upon request, we provide 13C-DEPT and CHN. Also, we provide a complete characterization report upon delivery. Daicel offers highly pure isotope-labeled standards of Icatibant in bioanalytical research and BA/BE studies with isotope data in CoA.