Ecallantide (DX-88) is a potent and specific inhibitor of plasma kallikrein. Ecallantide is a recombinantly produced and engineered small protein based on the first Kunitz domain of human tissue factor pathway inhibitor. It was identified through phage display technology. Ecallantide binds to plasma kallikrein and blocks its binding site, inhibiting the conversion of HMW kininogen to bradykinin. Hereditary angioedema (HAE) resulting from the deficiency of the C1 inhibitor protein is a rare disease, characterized by paroxysms of edema formation in the subcutis and in the submucosa. Edema can cause obstruction of the upper airway, which may lead to suffocation. Prompt elimination of edema is necessary to save patients from this life-threatening condition. Essentially, these edematous attacks are related to the activation of the kinin-kallikrein system and the consequent release of bradykinin. Ecallantide (KALBITOR) is a plasma kallikrein inhibitor indicated for treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: P03952 Gene ID: 3818.0 Gene Symbol: KLKB1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/18613770 |
25.0 pM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | KALBITOR Approved UseKalbitor® (ecallantide) is indicated for treatment of acute attacks of hereditary angioedema (HAE) in patients 12 years of age and older. Launch Date2009 |
Substance Class |
Protein
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Sequence Type | COMPLETE |
Record UNII |
5Q6TZN2HNM
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Validated (UNII)
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FDA ORPHAN DRUG |
160802
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WHO-VATC |
QB06AC03
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WHO-ATC |
B06AC03
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NCI_THESAURUS |
C783
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NDF-RT |
N0000192750
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5Q6TZN2HNM
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CHEMBL1201837
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4846
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C65505
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SUB31283
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PP-40
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C511194
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m4806
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ECALLANTIDE
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658708
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5Q6TZN2HNM
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DTXSID90196709
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118984459
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Related Record | Type | Details | ||
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TARGET -> INHIBITOR |
BINDING
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ACTIVE MOIETY |
Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
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Molecular Formula | CHEMICAL |
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Volume of Distribution | PHARMACOKINETIC |
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MOL_WEIGHT:NUMBER(CALCULATED) | CHEMICAL |
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Biological Half-life | PHARMACOKINETIC |
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