Conestat alfa 2,100unit powder for solution for injection vials
C1 Esterase Inhibitor (Recombinant) is a recombinant analogue of endogenous complement component-1 esterase inhibitor (rhC1INH), purified from the milk of transgenic rabbits.
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1 branded products available
Therapeutically similar medicines
Similarity based on WHO Anatomical Therapeutic Chemical (ATC) classification and NHS BNF section grouping. Source data: NHS dm+d via TRUD (OGL v3.0), WHO ATC/DDD Index.
Clinical guidelines and formulary information
British National Formulary
Conestat alfa
Source: British National Formulary, NICE. Joint Formulary Committee. Contains public sector information licensed under the Open Government Licence v3.0.
NICE clinical guidance(1)
Source: National Institute for Health and Care Excellence (NICE). Contains public sector information licensed under the Open Government Licence v3.0.
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Codes for healthcare professionals and prescribing systems
These codes are used by healthcare IT systems and prescribers to identify this medicine.
NHS UK identifiers
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SNOMED CT and dm+d codes from NHS TRUD (Technology Reference data Update Distribution), licensed under the Open Government Licence v3.0. BNF codes from NHS Business Services Authority (NHSBSA). ATC codes from the WHO Collaborating Centre for Drug Statistics Methodology (whocc.no).
Active and completed clinical studies from ClinicalTrials.gov
Source: ClinicalTrials.gov, a database of the U.S. National Library of Medicine (NLM), National Institutes of Health (NIH). Data accessed via ClinicalTrials.gov API v2. Trial information is provided for research purposes and does not constitute medical advice.
Pharmacology and chemical data from DrugBank
Key facts
Drug status
Approved
Major interactions
None known
Half-life
Not available
Mechanism
The primary function of endogenous C1INH is to regulate the activation of the complement and contact system pathways.
Food interactions
None known
Human targets
7 targets
Data: DrugBank · CC BY-NC 4.0
Pharmacokinetics at a glance
Absorption
0.10 hr
Elimination
2.5 hours
Clearance
414 mL
Pharmacokinetic data: DrugBank · CC BY-NC 4.0
Marketed as the product Ruconest (FDA), this drug is indicated for the treatment of acute attacks of hereditary angioedema (HAE) due to C1 esterase inhibitor deficiency in adults. Intravenous replacement of C1 esterase inhibitor results in reversal of acute symptoms of HAE.
Known interactions with other medications. Always consult a healthcare professional.
Showing 37 of 37 interactions
Serious arterial and venous thromboembolic (TE) events have been reported at the recommended dose of plasma derived C1 esterase inhibitor products in patients with risk factors. Risk factors may include the presence of an indwelling venous catheter/access device, prior history of thrombosis, underlying atherosclerosis, use of oral contraceptives or certain androgens, morbid obesity, and immobility. Monitor patients with known risk factors for TE events during and after administration.
How the body processes this drug — absorption, distribution, metabolism, and elimination
Proteins and enzymes this drug interacts with in the body
PMID:17996945 PMID:19473974 PMID:29449492
C1R catalyzes the first enzymatic step in the classical complement pathway: it is activated by the C1Q subcomplex of the C1 complex, which associates with IgG or IgM immunoglobulins complexed with antigens to form antigen-antibody complexes on the surface of pathogens .
PMID:29449492 PMID:34155115
Immunoglobulin-binding promotes the autocatalytic cleavage and activation of C1R .
PMID:11445589 PMID:11673533 PMID:17996945 PMID:20178990 PMID:6254570 PMID:6271784
Activated C1R then cleaves and activates C1S, the second protease of the classical complement pathway .
PMID:11445589 PMID:11673533 PMID:6271784
It is unclear if C1R activates C1S within single, strained C1 complexes or between neighboring C1 complexes on surfaces PMID:28104818 PMID:29311313 PMID:29449492
PMID:11445589 PMID:16169853 PMID:417728 PMID:467643 PMID:6271784 PMID:6282646 PMID:6319179 PMID:70787 PMID:9422791
C1S is activated following association of the C1 complex with immunoglobulins (IgG or IgM) complexed with antigens to form antigen-antibody complexes on the surface of pathogens .
PMID:34155115
C1S is cleaved and activated by C1R to generate C1s subcomponent heavy and light chains .
PMID:11445589 PMID:6271784
C1s subcomponent light chain then cleaves and activates C2 and C4, the next components of the classical complement pathway PMID:16169853 PMID:467643 PMID:6282646 PMID:6319179 PMID:6906228 PMID:70787 PMID:9422791
PMID:2019570 PMID:21976677
Triggers the production of pro-inflammatory cytokines, such as MCP-1/CCL2 and IL8/CXCL8, in endothelial cells PMID:30568593 PMID:9780208
ATC B06AC04
Chemical identifiers
CAS, UNII, InChI Key and database cross-references
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Chemical identifiers
CAS, UNII, InChI Key and database cross-references
Linked compound data from DrugBank Open Data (CC BY-NC 4.0)
Conestat alfa
Additional database identifiers
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1246
GenAtlas
C1R
GeneCards
C1R
GenBank Gene Database
X04701
GenBank Protein Database
29539
Guide to Pharmacology
2334
UniProt Accession
C1R_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:1247
GenAtlas
C1S
GeneCards
C1S
GenBank Gene Database
X06596
GenBank Protein Database
763110
Guide to Pharmacology
2335
UniProt Accession
C1S_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:6371
GenAtlas
KLKB1
GeneCards
KLKB1
GenBank Gene Database
M13143
Guide to Pharmacology
2379
UniProt Accession
KLKB1_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3530
GeneCards
F12
Guide to Pharmacology
2361
UniProt Accession
FA12_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3535
GenAtlas
F2
GeneCards
F2
GenBank Gene Database
M17262
GenBank Protein Database
339641
Guide to Pharmacology
2362
UniProt Accession
THRB_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:3529
GenAtlas
F11
GeneCards
F11
GenBank Gene Database
M13142
GenBank Protein Database
182833
Guide to Pharmacology
2360
UniProt Accession
FA11_HUMAN
HUGO Gene Nomenclature Committee (HGNC)
HGNC:9051
GenAtlas
PLAT
GeneCards
PLAT
GenBank Gene Database
L00153
GenBank Protein Database
339834
Guide to Pharmacology
2392
UniProt Accession
TPA_HUMAN
DrugBank citations
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