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

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