Brolucizumab
Identification
- Name
- Brolucizumab
- Accession Number
- DB14864
- Description
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
- Associated Conditions
- Contraindications & Blackbox Warnings
Learn about our commercial Contraindications & Blackbox Warnings data.
Learn More- 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
Learn about our commercial Adverse Effects data.
Learn More- Toxicity
Data regarding the toxicity of brolucizumab is not readily available.6
- Affected organisms
- Not Available
- 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 Unlock Additional DataAbciximab 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. 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. 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. Antilymphocyte immunoglobulin (horse) The risk or severity of adverse effects can be increased when Antilymphocyte immunoglobulin (horse) is combined with Brolucizumab. Antithymocyte immunoglobulin (rabbit) The risk or severity of adverse effects can be increased when Antithymocyte immunoglobulin (rabbit) is combined with Brolucizumab. Asfotase alfa The risk or severity of adverse effects can be increased when Asfotase alfa is combined with Brolucizumab. Additional Data Available- Extended DescriptionExtended DescriptionAvailable for Purchase
Extended description of the mechanism of action and particular properties of each drug interaction.
Learn more - SeveritySeverityAvailable for Purchase
A severity rating for each drug interaction, from minor to major.
Learn more - Evidence LevelEvidence LevelAvailable for Purchase
A rating for the strength of the evidence supporting each drug interaction.
Learn more - ActionActionAvailable for Purchase
An effect category for each drug interaction. Know how this interaction affects the subject drug.
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- Food Interactions
- No interactions found.
Products
- Brand Name Prescription Products
Name Dosage Strength Route Labeller Marketing Start Marketing End Region Image Unlock Additional DataBeovu Solution 6 mg Intravitreal Novartis Not applicable Not applicable Canada Beovu Injection, solution Intravitreal Novartis Europharm Limited 2020-02-13 Not applicable EU Beovu Solution 6 mg Intravitreal Novartis 2020-05-15 Not applicable Canada Beovu Injection, solution 6 mg/0.05mL Intravitreal Novartis Pharmaceuticals Corporation 2019-10-07 Not applicable US Beovu Injection, solution Intravitreal Novartis Europharm Limited 2020-02-13 Not applicable EU Additional Data Available- Application NumberApplication NumberAvailable for Purchase
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
Learn more - Product CodeProduct CodeAvailable for Purchase
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
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Categories
- ATC Codes
- S01LA06 — Brolucizumab
- Drug Categories
- 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
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. [PubMed:23257829]
- 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. [PubMed:16478695]
- 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. [PubMed:28551167]
- 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. [PubMed:31413539]
- 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. [PubMed:28653357]
- FDA Approved Drug Products: Brolucizumab Intravitreal Injection [Link]
- Safety and Pharmacokinetics of RTH258 in Subjects With Age-Related Macular Degeneration [Link]
- External Links
- 2204915
- Wikipedia
- Brolucizumab
- AHFS Codes
- 52:92.00 — EENT Drugs, Miscellaneous
- FDA label
- Download (538 KB)
Clinical Trials
- Clinical Trials
Phase Status Purpose Conditions Count 4 Not Yet Recruiting Treatment Age-Related Macular Degeneration (ARMD) / Eye Diseases / Macular Degeneration / Retinal Degenerations / Retinal Diseases / Wet Macular Degeneration 1 4 Not Yet Recruiting Treatment Wet Macular Degeneration 1 4 Recruiting Treatment Dystrophy, Retinal 1 4 Recruiting Treatment Neovascular Age-Related Macular Degeneration 2 3 Active Not Recruiting Treatment Age-Related Macular Degeneration (ARMD) 1 3 Active Not Recruiting Treatment Diabetic Macular Edema (DME) 2 3 Completed Treatment Age-Related Macular Degeneration (ARMD) / Eye Diseases / Macular Degeneration / Retinal Degenerations / Retinal Diseases / Wet Macular Degeneration 1 3 Completed Treatment Neovascular Age Related Macular Degeneration / Neovascular Age-Related Macular Degeneration 1 3 Completed Treatment Neovascular Age-Related Macular Degeneration 1 3 Completed Treatment Neovascular Age-Related Macular Degeneration / Subfoveal Choroidal Neovascularization 2
Pharmacoeconomics
- Manufacturers
- Not Available
- Packagers
- Not Available
- Dosage Forms
Form Route Strength Injection, solution Intravitreal Injection, solution Intravitreal 120 MG/ML Injection, solution Intravitreal 6 mg/0.05mL Solution Intravitreal 6 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: Brolucizumab Intravitreal Injection [Link]
Drug created on May 20, 2019 08:31 / Updated on January 25, 2021 22:38