ecallantide Chemical Properties

Sequence

Glu-Ala-Met-His-Ser-Phe-Cys-Ala-Phe-Lys-Ala-Asp-Asp-Gly-Pro-Cys-Arg-Ala-Ala-His-Pro-Arg-Trp-Phe-Phe-Asn-Ile-Phe-Thr-Arg-Gln-Cys-Glu-Glu-Phe-Ile-Tyr-Gly-Gly-Cys-Glu-Gly-Asn-Gln-Asn-Arg-Phe-Glu-Ser-Leu-Glu-Glu-Cys-Lys-Lys-Met-Cys-Thr-Arg-Asp (Disulfide bond:Cys1-Cys6, Cys2-Cys4, Cys3-Cys5)

Safety Information

Hazardous Substances Data

460738-38-9(Hazardous Substances Data)

ecallantide Usage And Synthesis

Description

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.

Originator

Dyax Corp. (United States)

Uses

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

brand name

Kalbitor

Synthesis

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 the room temperature with stirring for 36 hours, and quench it by adding glacial acetic acid to adjust the pH=3-5, then the eicosapentin crude peptide solution was obtained, and purify it with reference to the method of Example 12. It was prepared and lyophilized, and 35.7 g of white peptide solid was obtained, the cyclization yield was 23.8%, and the mass spectral signal was 8387.654.

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