Identification

Name
Brolucizumab
Accession Number
DB14864
Type
Biotech
Groups
Approved, Investigational
Biologic Classification
Protein Based Therapies
Monoclonal antibody (mAb)
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

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
Prescription Products
NameDosageStrengthRouteLabellerMarketing StartMarketing End
BeovuInjection, solution6 mg/0.05mLIntravitrealNovartis Pharmaceuticals Corporation2019-10-07Not applicableUs
Additional Data Available
  • Application Number
    Application Number

    A unique ID assigned by the FDA when a product is submitted for approval by the labeller.

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  • Product Code
    Product Code

    A governmentally-recognized ID which uniquely identifies the product within its regulatory market.

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Categories
UNII
XSZ53G39H5
CAS number
1531589-13-5

Pharmacology

Indication

Brolucizumab is a monoclonal antibody indicated to treat neovascular age related macular degeneration.3,6

Associated Conditions
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

TargetActionsOrganism
AVascular endothelial growth factor A
inhibitor
Humans
Additional Data Available
Adverse Effects

Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.

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Additional Data Available
Contraindications

Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.

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Additional Data Available
Blackbox Warnings

Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.

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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

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.
DrugInteraction
AbciximabThe risk or severity of adverse effects can be increased when Abciximab is combined with Brolucizumab.
AbituzumabThe risk or severity of adverse effects can be increased when Abituzumab is combined with Brolucizumab.
AbrilumabThe risk or severity of adverse effects can be increased when Brolucizumab is combined with Abrilumab.
AdalimumabThe risk or severity of adverse effects can be increased when Adalimumab is combined with Brolucizumab.
AdecatumumabThe risk or severity of adverse effects can be increased when Adecatumumab is combined with Brolucizumab.
AducanumabThe risk or severity of adverse effects can be increased when Aducanumab is combined with Brolucizumab.
AfelimomabThe risk or severity of adverse effects can be increased when Afelimomab is combined with Brolucizumab.
AlemtuzumabThe risk or severity of adverse effects can be increased when Alemtuzumab is combined with Brolucizumab.
Alendronic acidThe risk or severity of jaw osteonecrosis and anti-angiogenesis can be increased when Brolucizumab is combined with Alendronic acid.
AlirocumabThe risk or severity of adverse effects can be increased when Alirocumab is combined with Brolucizumab.
Additional Data Available
  • Extended Description
    Extended Description

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  • Severity
    Severity

    A severity rating for each drug interaction, from minor to major.

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  • Evidence Level
    Evidence Level

    A rating for the strength of the evidence supporting each drug interaction.

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  • Action
    Action

    An effect category for each drug interaction. Know how this interaction affects the subject drug.

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Food Interactions
No interactions found.

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. [PubMed:23257829]
  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. [PubMed:16478695]
  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. [PubMed:28551167]
  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. [PubMed:31413539]
  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. [PubMed:28653357]
  6. FDA Approved Drug Products: 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
PhaseStatusPurposeConditionsCount
1, 2CompletedTreatmentNeovascular Age-Related Macular Degeneration1
2CompletedOtherNeovascular Age-Related Macular Degeneration1
2CompletedTreatmentNeovascular Age-Related Macular Degeneration2
3Active Not RecruitingTreatmentAge-Related Macular Degeneration (ARMD)1
3Active Not RecruitingTreatmentDiabetic Macular Edema (DME)2
3CompletedTreatmentAge-Related Macular Degeneration (ARMD) / Eye Diseases / Macular Degeneration / Retinal Degenerations / Retinal Diseases / Wet Macular Degeneration1
3CompletedTreatmentNeovascular Age Related Macular Degeneration1
3CompletedTreatmentNeovascular Age-Related Macular Degeneration1
3CompletedTreatmentNeovascular Age-Related Macular Degeneration / Subfoveal Choroidal Neovascularization2
3Not Yet RecruitingTreatmentDiabetic Macular Edema (DME)1
3Not Yet RecruitingTreatmentNeovascular Age Related Macular Degeneration1
3Not Yet RecruitingTreatmentNeovascular Age-Related Macular Degeneration1
3Not Yet RecruitingTreatmentProliferative Diabetic Retinopathy (PDR)1
3RecruitingTreatmentAge-Related Macular Degeneration (ARMD) / Eye Diseases / Macular Degeneration / Retinal Degenerations / Retinal Diseases / Wet Macular Degeneration1
3RecruitingTreatmentBranch Retinal Vein Occlusion1
3RecruitingTreatmentCentral Retinal Vein Occlusion (CRVO)1
3RecruitingTreatmentDiabetic Macular Edema (DME)2
3RecruitingTreatmentNeovascular Age-Related Macular Degeneration1
4Not Yet RecruitingTreatmentNeovascular Age-Related Macular Degeneration1
Not AvailableNot Yet RecruitingTreatmentPolypoidal Choroidal Vasculopathy (PCV) / Treatment Naive Patients With Polypoidal Choroidal Vasculopathy (PCV) Diagnosis That Would Likely Benefit From Any Insights Gained From This Study1

Pharmacoeconomics

Manufacturers
Not Available
Packagers
Not Available
Dosage forms
FormRouteStrength
Injection, solutionIntravitreal6 mg/0.05mL
Prices
Not Available
Patents
Not Available

Properties

State
Solid
Experimental Properties
Not Available

Taxonomy

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

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
  1. FDA Approved Drug Products: Brolucizumab Intravitreal Injection [Link]

Drug created on May 20, 2019 08:31 / Updated on March 21, 2020 21:18

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