brolucizumab

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Ligands
brolucizumab

GtoPdb Ligand ID: 8713

Synonyms: Beovu® | brolucizumab-dbll | ESBA-1008 | ESBA1008 | RTH258

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 degeneration 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.

References
1. Borras L, Urech D, Gunde T. (2013) Stable and soluble antibodies inhibiting VEGF. Patent number: US8349322 B2. Assignee: ESBATech, an Alcon Biomedical Research Unit, LLC.. Priority date: 25/06/2008. Publication date: 08/01/2013.
2. Borras L, Urech D. (2012) Humanization of rabbit antibodies using a universal antibody framework. Patent number: US8293235 B2. Assignee: ESBATech, an Alcon Biomedical Research Unit, LLC.. Priority date: 25/06/2008. Publication date: 23/10/2012.
3. Dugel PU, Koh A, Ogura Y, Jaffe GJ, Schmidt-Erfurth U, Brown DM, Gomes AV, Warburton J, Weichselberger A, Holz FG et al.. (2020) HAWK and HARRIER: Phase 3, Multicenter, Randomized, Double-Masked Trials of Brolucizumab for Neovascular Age-Related Macular Degeneration. Ophthalmology, 127 (1): 72-84. [PMID:30986442]
4. Sharma A, Reddy P, Kuppermann BD, Bandello F, Lowenstein A. (2018) Biosimilars in ophthalmology: "Is there a big change on the horizon?". Clin Ophthalmol, 12: 2137-2143. [PMID:30498330]

References

1. Borras L, Urech D, Gunde T. (2013)
Stable and soluble antibodies inhibiting VEGF.
Patent number: US8349322 B2. Assignee: ESBATech, an Alcon Biomedical Research Unit, LLC.. Priority date: 25/06/2008. Publication date: 08/01/2013.

2. Borras L, Urech D. (2012)
Humanization of rabbit antibodies using a universal antibody framework.
Patent number: US8293235 B2. Assignee: ESBATech, an Alcon Biomedical Research Unit, LLC.. Priority date: 25/06/2008. Publication date: 23/10/2012.

3. Dugel PU, Koh A, Ogura Y, Jaffe GJ, Schmidt-Erfurth U, Brown DM, Gomes AV, Warburton J, Weichselberger A, Holz FG et al.. (2020)
HAWK and HARRIER: Phase 3, Multicenter, Randomized, Double-Masked Trials of Brolucizumab for Neovascular Age-Related Macular Degeneration.
Ophthalmology, 127 (1): 72-84. [PMID:30986442]

4. Sharma A, Reddy P, Kuppermann BD, Bandello F, Lowenstein A. (2018)
Biosimilars in ophthalmology: "Is there a big change on the horizon?".
Clin Ophthalmol, 12: 2137-2143. [PMID:30498330]