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, long form	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.

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.

Food Interactions

No interactions found.

Products

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Brand Name Prescription Products

Name	Dosage	Strength	Route	Labeller	Marketing Start	Marketing End
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

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

RxNav: 2204915
Wikipedia: Brolucizumab

FDA label

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Clinical Trials

Clinical Trials Clinical Trial & Rare Diseases Add-on Data Package Explore 4,000+ rare diseases, orphan drugs & condition pairs, clinical trial why stopped data, & more. Preview package

Phase	Status	Purpose	Conditions	Count	Start Date	Why Stopped	100+ additional columns
Unlock 175K+ rows when you subscribe.View sample data
Not Available	Active Not Recruiting	Not Available	Diabetic Macular Edema (DME) / Neovascular Age-Related Macular Degeneration (nAMD)	1	somestatus	stop reason	just information to hide
Not Available	Completed	Not Available	Age - Related Macular Degeneration (AMD)	3	somestatus	stop reason	just information to hide
Not Available	Completed	Not Available	Neovascular Age-Related Macular Degeneration (nAMD)	3	somestatus	stop reason	just information to hide
Not Available	Enrolling by Invitation	Treatment	Neovascular Age-Related Macular Degeneration (nAMD)	1	somestatus	stop reason	just information to hide
Not Available	Unknown Status	Not Available	Age - Related Macular Degeneration (AMD)	1	somestatus	stop reason	just information to hide

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

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Details1. Vascular endothelial growth factor A, long form

Kind: Protein
Organism: Humans
Pharmacological action: Yes
Actions: Inhibitor

General Function: Participates in the induction of key genes involved in the response to hypoxia and in the induction of angiogenesis such as HIF1A (PubMed:35455969). Involved in protecting cells from hypoxia-mediated cell death (By similarity)
Specific Function: chemoattractant activity
Gene Name: VEGFA
Uniprot ID: P15692
Uniprot Name: Vascular endothelial growth factor A, long form
Molecular Weight: 43596.94 Da

References

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

Drug created at May 20, 2019 14:31 / Updated at September 06, 2024 11:54

Brolucizumab

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Pharmacology

Interactions

Products

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Clinical Trials

Clinical Trial & Rare Diseases Add-on Data Package

Pharmacoeconomics

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References