Ecallantide

Ecallantide

Clinical data
Trade names	Kalbitor
AHFS/Drugs.com	Monograph
License data	US FDA: ECALLANTIDE
Pregnancy category	US: C (Risk not ruled out)
Routes of administration	Subcutaneous injection
ATC code	B06AC03 (WHO)
Legal status
Legal status	US: ℞-only
Pharmacokinetic data
Biological half-life	1.5–2.5 hours
Excretion	Renal
Identifiers
IUPAC name [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)
CAS Number	460738-38-9 Y
PubChem CID	118984459
IUPHAR/BPS	6955
DrugBank	DB05311 Y
ChemSpider	34983390 Y
UNII	5Q6TZN2HNM
ChEMBL	CHEMBL1201837 N
Chemical and physical data
Formula	C305H442N88O91S8
Molar mass	7053.83 g/mol
NY (what is this?)

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 in cardiothoracic surgery. It is an inhibitor of the protein kallikrein and a 60-amino acid polypeptide which was developed from a Kunitz domain through phage display to mimic antibodies inhibiting kallikrein.

On November 27, 2009, ecallantide was approved by the FDA for the treatment of acute attacks of hereditary angioedema for persons over 16 years of age.

For angioedema due to ACE inhibitors it does not appear to have a benefit.

If approved for cardiothoracic surgery, it could become a replacement for aprotinin, which was withdrawn in 2007 after being shown to cause complications.

The most common adverse effects are headache, nausea, fatigue and diarrhea. Less common, but observed in more than 5% of patients in clinical trials, are respiratory tract infections, fever, vomiting, itching and upper abdominal pain. Up to 4% of patients showed anaphylaxis, which led to a black box warning in the US.

As of 2011^[update], no interaction studies have been conducted.

HAE is caused by a mutation of the C1-inhibitor gene. Defective or missing C1-inhibitor permits activation of kallikrein, a protease that is responsible for liberating bradykinin from its precursor kininogen. An excess of bradykinin leads to fluid leakage from blood vessels, causing swelling of tissues typical of HAE.

...
Wikipedia