Identification
- Summary
Brolucizumab is an anti VEGF-A monoclonal antibody indicated to treat neovascular age related macular degeneration.
- Brand Names
- Beovu
- Generic Name
- Brolucizumab
- DrugBank Accession Number
- DB14864
- Background
Brolucizumab, also known as RTH258 or ESBA1008,4 is a monoclonal antibody indicated to treat neovascular age related macular degeneration.6
Brolucizumab was granted FDA approval in October 2019.6
- Type
- Biotech
- Groups
- Approved, Investigational
- Biologic Classification
- Protein Based Therapies
Monoclonal antibody (mAb) - Protein Chemical Formula
- Not Available
- Protein Average Weight
- 26000.0 Da (approximate)
- Sequences
- Not Available
- Synonyms
- Brolucizumab
- brolucizumab-dbll
- External IDs
- ESBA-1008
- ESBA1008
- RTH-258
- RTH258
Pharmacology
- Indication
Brolucizumab is a monoclonal antibody indicated to treat neovascular age related macular degeneration.3,6
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- Contraindications & Blackbox Warnings
Avoid life-threatening adverse drug eventsImprove clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more.Avoid life-threatening adverse drug events & improve clinical decision support.- Pharmacodynamics
Brolucizumab is a vascular endothelial growth factor (VEGF) inhibitor which reduces proliferation of endothelial cells, vascularization of the tissue, and permeability of the vasculature.6 It has a long duration of action as it is given monthly.6 Patients should be counselled regarding the risk of endophthalmitis, retinal detachment, and arterial thromboembolic events following administration of this medication.6
- Mechanism of action
Brolucizumab is a vascular endothelial growth factor (VEGF) inhibitor which targets the major VEGF-A isoforms: VEGF110, VEGF121, and VEGF165.1,3,6 Inhibition of these VEGF-A isoforms reduce proliferation of endothelial cells, vascularization of the tissue, and permeability of the vasculature.6
Target Actions Organism AVascular endothelial growth factor A inhibitorHumans - Absorption
A 3mg dose of brolucizumab reaches a Cmax of 20.7ng/mL with a Tmax of 20.3h and an AUC of 2480ng*h/mL.7 A 6mg dose of brolucizumab reaches a Cmax of 77.6ng/mL with a Tmax of 17.4h and an AUC of 9169ng*h/mL.7
- Volume of distribution
Data regarding the volume of distribution is not readily available.6
- Protein binding
Monoclonal antibodies are generally not protein bound in serum.2
- Metabolism
Monoclonal antibodies are expected to undergo proteolysis to smaller peptides and amino acids.2
- Route of elimination
Data regarding the route of elimination is not readily available.6 Monoclonal antibodies are generally not eliminated in the urine, and only a small amount is excreted in bile.5
- Half-life
The systemic half life of bolucizumab is 4.4±2.0 days.6 The elimination half life is 108h for a 3mg dose and 103h for a 6mg dose.7
- Clearance
Data regarding the clearance of brolucizumab is not readily available.6
- Adverse Effects
Improve decision support & research outcomesWith structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates.Improve decision support & research outcomes with our structured adverse effects data.- Toxicity
Data regarding the toxicity of brolucizumab is not readily available.6
- Pathways
- Not Available
- Pharmacogenomic Effects/ADRs
- Not Available
Interactions
- Drug Interactions
- This information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
Drug Interaction Integrate drug-drug
interactions in your softwareAbciximab The risk or severity of adverse effects can be increased when Abciximab is combined with Brolucizumab. Adalimumab The risk or severity of adverse effects can be increased when Adalimumab is combined with Brolucizumab. Aducanumab The risk or severity of adverse effects can be increased when Aducanumab is combined with Brolucizumab. Alemtuzumab The risk or severity of adverse effects can be increased when Alemtuzumab is combined with Brolucizumab. Alendronic acid The risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Brolucizumab is combined with Alendronic acid. Alirocumab The risk or severity of adverse effects can be increased when Alirocumab is combined with Brolucizumab. Amivantamab The risk or severity of adverse effects can be increased when Brolucizumab is combined with Amivantamab. Anifrolumab The risk or severity of adverse effects can be increased when Anifrolumab is combined with Brolucizumab. Ansuvimab The risk or severity of adverse effects can be increased when Brolucizumab is combined with Ansuvimab. Anthrax immune globulin human The risk or severity of adverse effects can be increased when Anthrax immune globulin human is combined with Brolucizumab. 
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- No interactions found.
Products
Drug product information from 10+ global regionsOur datasets provide approved product information including:dosage, form, labeller, route of administration, and marketing period.Access drug product information from over 10 global regions.- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Beovu Injection, solution 6 mg/0.05mL Intravitreal Novartis Pharmaceuticals Corporation 2019-10-07 Not applicable US 
Beovu Solution 6 mg / 0.05 mL Intravitreal Novartis Not applicable Not applicable Canada 
Beovu Injection, solution 120 mg/ml Intravitreal Novartis Europharm Limited 2020-12-16 Not applicable EU 
Beovu Solution 6 mg / 0.05 mL Intravitreal Novartis 2020-05-15 Not applicable Canada Beovu Injection, solution 120 mg/ml Intravitreal Novartis Europharm Limited 2020-12-16 Not applicable EU
Categories
- ATC Codes
- S01LA06 — Brolucizumab
- Drug Categories
- Amino Acids, Peptides, and Proteins
- Angiogenesis Inhibitors
- Antibodies
- Antibodies, Monoclonal
- Antibodies, Monoclonal, Humanized
- Antineovascularisation Agents
- Blood Proteins
- EENT Drugs, Miscellaneous
- Globulins
- Immunoglobulins
- Immunoproteins
- Ocular Vascular Disorder Agents
- Ophthalmologicals
- Proteins
- Sensory Organs
- Serum Globulins
- Vascular Endothelial Growth Factor Inhibitor
- Chemical TaxonomyProvided by Classyfire
- Description
- Not Available
- Kingdom
- Organic Compounds
- Super Class
- Organic Acids
- Class
- Carboxylic Acids and Derivatives
- Sub Class
- Amino Acids, Peptides, and Analogues
- Direct Parent
- Peptides
- Alternative Parents
- Not Available
- Substituents
- Not Available
- Molecular Framework
- Not Available
- External Descriptors
- Not Available
- Affected organisms
- Not Available
Chemical Identifiers
- UNII
- XSZ53G39H5
- CAS number
- 1531589-13-5
References
- General References
- Perrot-Applanat M: VEGF isoforms. Cell Adh Migr. 2012 Nov-Dec;6(6):526-7. doi: 10.4161/cam.23256. Epub 2012 Nov 1. [Article]
- Tabrizi MA, Tseng CM, Roskos LK: Elimination mechanisms of therapeutic monoclonal antibodies. Drug Discov Today. 2006 Jan;11(1-2):81-8. doi: 10.1016/S1359-6446(05)03638-X. [Article]
- Dugel PU, Jaffe GJ, Sallstig P, Warburton J, Weichselberger A, Wieland M, Singerman L: Brolucizumab Versus Aflibercept in Participants with Neovascular Age-Related Macular Degeneration: A Randomized Trial. Ophthalmology. 2017 Sep;124(9):1296-1304. doi: 10.1016/j.ophtha.2017.03.057. Epub 2017 May 24. [Article]
- Yannuzzi NA, Freund KB: Brolucizumab: evidence to date in the treatment of neovascular age-related macular degeneration. Clin Ophthalmol. 2019 Jul 24;13:1323-1329. doi: 10.2147/OPTH.S184706. eCollection 2019. [Article]
- Ryman JT, Meibohm B: Pharmacokinetics of Monoclonal Antibodies. CPT Pharmacometrics Syst Pharmacol. 2017 Sep;6(9):576-588. doi: 10.1002/psp4.12224. Epub 2017 Jul 29. [Article]
- FDA Approved Drug Products: BEOVU (brolucizumab) intravitreal injection [Link]
- Safety and Pharmacokinetics of RTH258 in Subjects With Age-Related Macular Degeneration [Link]
- External Links
- 2204915
- Wikipedia
- Brolucizumab
- FDA label
- Download (538 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Active Not Recruiting Treatment Age - Related Macular Degeneration (AMD) 1 4 Active Not Recruiting Treatment Neovascular Age-Related Macular Degeneration (nAMD) 2 4 Recruiting Treatment Age - Related Macular Degeneration (AMD) 1 4 Recruiting Treatment Retinal Dystrophies 1 4 Terminated Treatment Neovascular Age-Related Macular Degeneration (nAMD) 1 4 Withdrawn Treatment Wet Macular Degeneration 1 3 Active Not Recruiting Treatment Proliferative Diabetic Retinopathy (PDR) 1 3 Completed Treatment Age - Related Macular Degeneration (AMD) 1 3 Completed Treatment Age - Related Macular Degeneration (AMD) / Eye Diseases / Macular Degeneration / Retinal Degenerations / Retinal Diseases / Wet Macular Degeneration 1 3 Completed Treatment Diabetic Macular Edema (DME) 4
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Intravitreal 120 MG/ML Injection, solution Intravitreal 6 mg/0.05mL Solution Intravitreal 6 mg / 0.05 mL Solution Intravitreal 120 mg/ml Solution Intraocular 6.000 mg Solution Intraocular 120 mg - Prices
- Not Available
- Patents
- Not Available
Properties
- State
- Solid
- Experimental Properties
- Not Available
Targets
- Kind
- Protein
- Organism
- Humans
- Pharmacological action
- Yes
- Actions
- Inhibitor
- General Function
- Vascular endothelial growth factor receptor binding
- Specific Function
- Growth factor active in angiogenesis, vasculogenesis and endothelial cell growth. Induces endothelial cell proliferation, promotes cell migration, inhibits apoptosis and induces permeabilization of...
- Gene Name
- VEGFA
- Uniprot ID
- P15692
- Uniprot Name
- Vascular endothelial growth factor A
- Molecular Weight
- 27042.205 Da
References
- FDA Approved Drug Products: BEOVU (brolucizumab) intravitreal injection [Link]
Drug created at May 20, 2019 14:31 / Updated at July 02, 2022 14:09