Ecallantide It is an inhibitor of the protein kallikrein and a 60-amino acid polypeptide.

• Ecallantide

• CAS No.:460738-38-9
• Formula:C₃₀₅H₄₄₂N₈₈O₉₁S₈
• Molecular Weight:7053.82798
• [Glu²⁰,Ala²¹,Arg³⁶,Ala³⁸,His³⁹,Pro⁴⁰,Trp⁴²]tissue factor pathway inhibitor (human)-(20-79)-peptide (modified on reactive bond region Kunitz inhibitor 1 domain containing fragment)

KALBITOR (ecallantide) is a human plasma kallikrein inhibitor for injection for subcutaneous use.

11 FEB 2013

Dyax Corp.  a developer of novel biotherapeutics for unmet medical needs, and CVie Therapeutics (CVie), a subsidiary of Lee’s Pharmaceutical Holdings Ltd., announced today a strategic partnership for the development and commercialization of KALBITOR® (ecallantide) in the treatment of hereditary angioedema (HAE) and other angioedema indications in China, Hong Kong and Macau.

KALBITOR is currently marketed in United States for the treatment of acute attacks of HAE in

patients 16 years of age and older. Under the terms of the exclusive license agreement, Dyax will receive an upfront payment and is eligible to receive future development, regulatory and sales milestones. Dyax is also eligible to receive royalty on net product sales. CVie is solely responsible for all costs associated with development, regulatory activities, and the commercialization of KALBITOR in China, Hong Kong
and Macau. Additionally, CVie will purchase drug product from Dyax on a cost-plus basis for
commercial supply.
If approved in China, KALBITOR would become the first novel therapy available for HAE in China, where presently only steroids are used.

KALBITOR (ecallantide injection) is a clear and colorless, sterile, and nonpyrogenic solution. Each vial contains 10 mg ecallantide as the active ingredient, and the following inactive ingredients: 0.76 mg disodium hydrogen orthophosphate (dihydrate), 0.2 mg monopotassium phosphate, 0.2 mg potassium chloride, and 8 mg sodium chloride in water for injection, USP. KALBITOR (ecallantide injection) is preservative free, with a pH of approximately 7.0. A 30 mg dose is supplied as 3 vials each containing 1 mL of 10 mg/mL KALBITOR (ecallantide injection) . Each vial contains a slight overfill. Vials are intended for single use. Ecallantide is a 60-amino-acid protein produced in Pichia pastoris yeast cells by recombinant DNA technology.

The Ecallantide, with the IUPAC name of [Glu20,Ala21,Arg36,Ala38,His39,Pro40,Trp42]tissue factor pathway inhibitor (human)-(20-79)-peptide (modified on reactive bond region Kunitz inhibitor 1 domain containing fragment), is one kind of inhibitor. This chemical’s classification codes are Plasma Kallikrein Inhibitor; Reduction of Blood Loss During Cardiothoracic Surgery (Plasma Kallikrein Inhibitor); Treatment of Hereditary Angioedema. Ecallantide (trade name Kalbitor, investigational name DX-88) is an inhibitor of the protein kallikrein used for hereditary angioedema (HAE) and in the prevention of blood loss in cardiothoracic surgery. If approved for cardiothoracic surgery, it could become a replacement for aprotinin, which was withdrawn in 2007 after being shown to cause complications.

Ecallantide (trade name Kalbitor, investigational name DX-88) is a drug used for the treatment of hereditary angioedema (HAE) and in the prevention of blood loss incardiothoracic surgery.^[1] It is an inhibitor of the protein kallikrein and a 60-amino acidpolypeptide which was developed from a Kunitz domain through phage display to mimic antibodies inhibiting kallikrein.^[1] On November 27, 2009, ecallantide was approved by theU.S. Food and Drug Administration for the treatment of acute attacks of hereditary angioedema for persons over 16 years of age.^[2]

If approved for cardiothoracic surgery, it could become a replacement foraprotinin, which was withdrawn in 2007 after being shown to cause complications.

1.  Lehmann A (August 2008). “Ecallantide (DX-88), a plasma kallikrein inhibitor for the treatment of hereditary angioedema and the prevention of blood loss in on-pump cardiothoracic surgery”. Expert Opin Biol Ther 8 (8): 1187–99. doi:10.1517/14712598.8.8.1187.PMID 18613770.
2. Waknine, Yael (December 4, 2009). “FDA Approves Ecallantide for Hereditary Angioedema”. Medscape. Retrieved 2009-12-07.
3. Dyax Corp. (2009). “Full prescibing information Kalbitor”. Retrieved 2010-05-02.
4. Bhoola, K. D.; Figueroa, C. D.; Worthy, K. (1992). “Bioregulation of kinins: Kallikreins, kininogens, and kininases”. Pharmacological reviews 44 (1): 1–80. PMID 1313585. edit
5. Stefan Offermanns; Walter Rosenthal (2008). Encyclopedia of Molecular Pharmacology. Springer. pp. 673–. ISBN 978-3-540-38916-3. Retrieved 11 December 2010.