emicizumab   Click here for help

GtoPdb Ligand ID: 9744

Synonyms: ACE-910 | ACE910 | emicizumab-kxwh | Hemlibra® | RG6013
Approved drug
emicizumab is an approved drug (FDA (2017), EMA (2018))
Compound class: Antibody
Comment: Emicizumab, is a humanised bispecific antibody that binds blood coagulation factors IXa and X and acts as a factor VIII mimetic to bring about activation of factor X, and promote coagulation [2-3,5]. In essence, emicizumab works by bridging between coagulation factors IX and X and is the first-in-class drug for haemophilia A prevention with this mechanism of action.
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Ligand Activity Visualisation Charts

These are box plot that provide a unique visualisation, summarising all the activity data for a ligand taken from ChEMBL and GtoPdb across multiple targets and species. Click on a plot to see the median, interquartile range, low and high data points. A value of zero indicates that no data are available. A separate chart is created for each target, and where possible the algorithm tries to merge ChEMBL and GtoPdb targets by matching them on name and UniProt accession, for each available species. However, please note that inconsistency in naming of targets may lead to data for the same target being reported across multiple charts.

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View interactive charts of activity data across species
References
1. FDA. 
FDA approves emicizumab-kxwh for prevention and reduction of bleeding in patients with hemophilia A with factor VIII inhibitors.
Accessed on 03/01/2018. Modified on 03/01/2018. fda.gov, https://www.fda.gov/Drugs/InformationOnDrugs/ApprovedDrugs/ucm585650.htm
2. Kitazawa T, Esaki K, Tachibana T, Ishii S, Soeda T, Muto A, Kawabe Y, Igawa T, Tsunoda H, Nogami K et al.. (2017)
Factor VIIIa-mimetic cofactor activity of a bispecific antibody to factors IX/IXa and X/Xa, emicizumab, depends on its ability to bridge the antigens.
Thromb Haemost, 117 (7): 1348-1357. [PMID:28451690]
3. Muto A, Yoshihashi K, Takeda M, Kitazawa T, Soeda T, Igawa T, Sakamoto Y, Haraya K, Kawabe Y, Shima M et al.. (2014)
Anti-factor IXa/X bispecific antibody (ACE910): hemostatic potency against ongoing bleeds in a hemophilia A model and the possibility of routine supplementation.
J Thromb Haemost, 12 (2): 206-213. [PMID:24735117]
4. Oldenburg J, Mahlangu JN, Kim B, Schmitt C, Callaghan MU, Young G, Santagostino E, Kruse-Jarres R, Negrier C, Kessler C et al.. (2017)
Emicizumab Prophylaxis in Hemophilia A with Inhibitors.
N Engl J Med, 377 (9): 809-818. [PMID:28691557]
5. Sampei Z, Igawa T, Soeda T, Okuyama-Nishida Y, Moriyama C, Wakabayashi T, Tanaka E, Muto A, Kojima T, Kitazawa T et al.. (2013)
Identification and multidimensional optimization of an asymmetric bispecific IgG antibody mimicking the function of factor VIII cofactor activity.
PLoS ONE, 8 (2): e57479. [PMID:23468998]
6. Yousphi AS, Bakhtiar A, Cheema MA, Nasim S, Ullah W. (2019)
Acquired Hemophilia A: A Rare but Potentially Fatal Bleeding Disorder.
Cureus, 11 (8): e5442. [PMID:31632887]