460738-38-9

Ecallantide, also known as DX-88, was approved in 2009 in the United States for treatment of hereditary angioedema (HAE), a condition characterized by episodic attacks of localized edema in cutaneous and mucosal tissues. HAE results from deficiencies or disorders of C1-esterase inhibitor protein (C1- 1NH). Mutation of the gene that encodes C1-1NH causes the lack or altered activity of the serine protease, C1-1NH. C1-1NH regulates the kallikrein–kinin (contact activation) and complement cascade systems. Ecallantide (DX-88) was designed to inhibit the action of plasma kallikrein. Ecallantide is a potent and selective inhibitor of plasma kallikrein with a Ki= 25 pM. The discovery program that identified ecallantide used phage display technology and a library of designed variants of the first Kunitz domain of TFPI. Ecallantide, a 60-amino acid peptide, with 3-disulfide bonds, differs from TFPI by 7-amino acids. Ecallantide has been developed as a subcutaneous administered formulation.

Dyax Corp. (United States)

Treatment of hereditary angioedema; reduction of blood loss during cardiothoracic surgery (plasma kallikrein inhibitor).

Kalbitor

Dissolve 150 g of the linear crude peptide of eicosapentin in 150 L of buffer system, which was an aqueous solution of 0.1 mM ammonium acetate, 3 times the amount of DTT of the linear crude peptide (in substance), pH 7.8, and place it in the open mouth at