brolucizumab   Click here for help

GtoPdb Ligand ID: 8713

Synonyms: Beovu® | brolucizumab-dbll | ESBA-1008 | ESBA1008 | RTH258
Approved drug
brolucizumab is an approved drug (FDA (2019), EMA (2020))
Compound class: Antibody
Comment: Brolucizumab is a single-chain variable fragment (scFv) anti-VEGF antibody targeting vascular endothelial growth factor A (VEGFA). This immunobinder was derived from a humanised anti-VEGFA rabbit monoclonal [2].
Peptide sequence and secondary structural information are available from brolucizumab's IMGT/mAb-DB record.
Peptide sequence alignment analysis of patented peptide sequences using the heavy chain variable region of brolucizumab identifies a 100% match with SEQ ID NO: 164 in patent US8349322 B2 [1].

Following regulatory approval brolucizumab took its place as a wet age-related macular degeneraton therapy alongside aflibercept (Eylea®) and ranibizumab (Lucentis®), which were previously the main drugs used for this indication. However, with patent protection for both of these older dugs due to expire in the next 2-5 years [4], brolucizumab will likely face competition from aflibercept and ranibizumab biosimilars.
Bioactivity Comments
Given the research code assigned, it is likely that brolucizumab is the derivative designated 578minmaxT84N_V89L (protein1008) in patent US8349322 B2 [1]. Data for 578min_max (protein1008) is provided in the interaction table below.
Selectivity at ligand targets
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Target Sp. Type Action Value Parameter Concentration range (M) Reference
VEGFA Primary target of this compound Hs Antibody Binding 8.8 pKd - 1
pKd 8.8 (Kd 1.59x10-9 M) [1]