Brolucizumab

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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Associated Conditions

• Neovascular Age-Related Macular Degeneration (nAMD)

Contraindications & Blackbox Warnings

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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	inhibitor	Humans

Absorption

A 3mg dose of brolucizumab reaches a C_max of 20.7ng/mL with a T_max of 20.3h and an AUC of 2480ng*h/mL.⁷ A 6mg dose of brolucizumab reaches a C_max of 77.6ng/mL with a T_max 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

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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.

• Approved
• Vet approved
• Nutraceutical
• Illicit
• Withdrawn
• Investigational
• Experimental
• All Drugs

Drug	Interaction
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Abciximab	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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Food Interactions

No interactions found.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End	Region	Image
Beovu	Injection, solution	120 mg/ml	Intravitreal	Novartis Europharm Limited	2020-12-16	Not applicable
Beovu	Injection, solution	6 mg/0.05mL	Intravitreal	Novartis Pharmaceuticals Corporation	2019-10-07	Not applicable
Beovu	Solution	6 mg / 0.05 mL	Intravitreal	Novartis	Not applicable	Not applicable
Beovu	Injection, solution	120 mg/ml	Intravitreal	Novartis Europharm Limited	2020-12-16	Not applicable
Beovu	Solution	6 mg / 0.05 mL	Intravitreal	Novartis	2020-05-15	Not applicable

Categories

ATC Codes

S01LA06 — Brolucizumab

• S01LA — Antineovascularisation agents
• S01L — OCULAR VASCULAR DISORDER AGENTS
• S01 — OPHTHALMOLOGICALS
• S — SENSORY ORGANS

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

1. 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]
2. 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]
3. 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]
4. 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]
5. 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]
6. FDA Approved Drug Products: BEOVU (brolucizumab) intravitreal injection [Link]
7. Safety and Pharmacokinetics of RTH258 in Subjects With Age-Related Macular Degeneration [Link]

External Links

RxNav

2204915

Wikipedia

Brolucizumab

FDA label

Download (538 KB)

Clinical Trials

Clinical Trials

Phase	Status	Purpose	Conditions	Count
4	Active Not Recruiting	Treatment	Neovascular Age-Related Macular Degeneration (nAMD)	1
4	Recruiting	Treatment	Age - Related Macular Degeneration (AMD)	1
4	Recruiting	Treatment	Age - Related Macular Degeneration (AMD) / Eye Diseases / Macular Degeneration / Retinal Degenerations / Retinal Diseases / Wet Macular Degeneration	1
4	Recruiting	Treatment	Neovascular Age-Related Macular Degeneration (nAMD)	2
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	Neovascular Age-Related Macular Degeneration (nAMD)	1
3	Active Not Recruiting	Treatment	Proliferative Diabetic Retinopathy (PDR)	1
3	Completed	Treatment	Age - Related Macular Degeneration (AMD) / Eye Diseases / Macular Degeneration / Retinal Degenerations / Retinal Diseases / Wet Macular Degeneration	2

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	120 mg

Prices

Not Available

Patents

Not Available

Properties

State

Solid

Experimental Properties

Not Available

Targets

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Details1. Vascular endothelial growth factor A

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

1. FDA Approved Drug Products: BEOVU (brolucizumab) intravitreal injection [Link]

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Drug created at May 20, 2019 14:31 / Updated at July 02, 2022 14:09