Dosing & Uses
Dosage Forms & Strengths
injectable solution for intravitreal use
- 6mg/0.05mL (single-dose vial or prefilled syringe)
Macular Degeneration
Indicated for treatment of neovascular (wet) age-related macular degeneration (AMD)
6 mg (0.05 mL of 120 mg/mL solution) by intravitreal injection monthly (~q25-31 days) x3 doses, THEN 6 mg q8-12weeks
Diabetic Macular Edema
Indicated for treatment of diabetic macular edema (DME)
6 mg (0.05 mL of 120 mg/mL solution) by intravitreal injection q6Weeks (~39-45 days) for first 5 doses, followed by 6 mg q8-12Weeks
Dosage Modifications
Hepatic or renal impairment
- Effect of severe renal impairment or any degree of hepatic impairment on the pharmacokinetics of brolucizumab is unknown
- Significant increases in serum brolucizumab exposures are not expected with intravitreal route of administration; no dosage adjustment is needed based on renal or hepatic impairment status
Safety and efficacy not established
Adverse Effects
1-10%
Blurred vision (10%)
Cataract (7%)
Conjunctival hemorrhage (6%)
Vitreous floaters (5%)
Eye pain (5%)
Intraocular inflammation (4%)
Intraocular pressure increased (4%)
Retinal hemorrhage (4%)
Vitreous detachment (4%)
Conjunctivitis (3%)
Retinal pigment epithelial tear (3%)
Corneal abrasion (2%)
Hypersensitivity (2%)
Punctate keratitis (1%)
Retinal tear (1%)
Endophthalmitis (1%)
Blindness (1%)
Retinal artery occlusion (1%)
Retinal detachment (1%)
Conjunctival hyperemia (1%)
Lacrimation increased (1%)
Abnormal sensation in eye (1%)
Detachment of retinal pigment epithelium (1%)
Postmarketing Reports
Endophthalmitis and retinal detachment
Retinal vasculitis and/or retinal vascular occlusion
Vitreous hemorrhage
Warnings
Contraindications
Ocular or periocular infections
Active intraocular inflammation
Hypersensitivity
Cautions
Hypersensitivity reactions may manifest as rash, pruritus, urticaria, erythema, or severe intraocular inflammation
Intravitreal injections are associated with endophthalmitis and retinal detachments; instruct patients to immediately report any symptoms suggestive of endophthalmitis or retinal detachment
Acute increases in intraocular pressure (IOP) have been seen within 30 minutes of intravitreal injection; sustained IOP increases have also been reported; both IOP and perfusion of the optic nerve head must be monitored and managed appropriately
A low rate of arterial thromboembolic events observed during clinical trials following intravitreal use of vascular endothelial growth factor (VEGF) inhibitors
Retinal vasculitis
- Retinal vasculitis and/or retinal vascular occlusion, typically in presence of intraocular inflammation, reported with therapy
- Retinal vasculitis and/or retinal vascular occlusion, typically in presence of intraocular inflammation, are immune-mediated adverse events related to exposure to the drug; this treatment-emergent antibody response may develop following the first intravitreal injection
- The immune-mediated adverse events may occur following first intravitreal injection; discontinue treatment in patients who develop these events
- Patients who experience intraocular inflammation following treatment may be at risk of developing retinal vasculitis and/or retinal vascular occlusion and should be closely monitored; patients should be instructed to report any change in vision without delay
Pregnancy & Lactation
Pregnancy
There are no adequate and well-controlled studies in pregnant women
Based on anti-VEGF mechanism of action, treatment may pose risk to human embryofetal development
Use during pregnancy only if the potential benefit outweighs the potential fetal risk
Animal data
- Intravitreal administration to pregnant monkeys once every 4 weeks in one eye from organogenesis to birth did not indicate any harmful effects with respect to pre- or postnatal development at 10-fold the maximum recommended human dose (MRHD) on a mg/kg basis
- VEGF inhibition has also been shown to affect follicular development, corpus luteum function, and fertility
Contraception
- Females of reproductive potential should use highly effective contraception (methods that result in <1% pregnancy rates) during treatment and for at least 1 month after the last dose following brolucizumab discontinuation
Infertility
- No studies have been conducted and it is not known whether brolucizumab can affect reproductive capacity
- Based on its anti-VEGF mechanism of action, treatment may pose a risk to reproductive capacity
Lactation
No data are available regarding the presence of brolucizumab in human milk, the effects of the drug on the breastfed infant, or the effects of the drug on milk production/excretion
Because many drugs are transferred in human milk and because of the potential for absorption and adverse reactions in the breastfed child, breastfeeding is not recommended during treatment and for at least 1 month after the last dose following discontinuation
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Human VEGF inhibitor; binds to the 3 major VEGF-A isoforms (eg, VEGF110, VEGF121, VEGF165), thereby preventing interaction with receptors VEGFR-1 and VEGFR-2
By inhibiting VEGF-A, brolucizumab suppresses endothelial cell proliferation, neovascularization, and vascular permeability
Absorption
Peak plasma time: 24 hr
Peak plasma level: 49 ng/mL
Metabolism
Not fully characterized; however, free brolucizumab is expected to undergo metabolism via proteolysis
Elimination
Half-life: 4.4 days
Excretion: Not fully characterized; however, free brolucizumab is expected to undergo target-mediated disposition and/or passive renal excretion
Administration
Intravitreal Preparation
Before use, unopened glass vial or prefilled syringe may be kept at room temperature (20-25ºC [68-77ºF]) for up to 24 hr
See prescribing information with diagrams for precise steps to aseptically prepare dose
Vial
- After vial is opened, proceed under aseptic conditions
- Inspect visually before administration; discard if particulates, cloudiness, or discoloration are visible
- Kit includes sterile glass vial and filter needle which are for single use only
- Do not use if packaging, vial and/or filter needle are damaged or expired
Prefilled syringe
- Inspect visually before administration; discard if packaging, or prefilled syringe are opened, damaged or expired
- Snap off syringe cap and discard it; do not turn or twist syringe cap
- Aseptically and firmly assemble a 30-gauge x 0.5-inch sterile injection needle (not included) onto syringe
- If there are any air bubbles, gently tap syringe with finger until bubbles rise to the top; carefully remove needle cap by pulling it straight off
Intravitreal Administration
Administer immediately after dose preparation
Intravitreal injection procedure must be carried out under aseptic conditions, which includes surgical hand disinfection, sterile gloves, a sterile drape, and a sterile eyelid speculum (or equivalent), and availability of sterile paracentesis equipment (if required)
Administer adequate anesthesia and a broad-spectrum topical microbicide to disinfect the periocular skin, eyelid, and ocular surface beforehand
Inject slowly until rubber stopper reaches the end of the syringe to deliver the volume of 0.05 mL; confirm delivery of the full dose by checking that the rubber stopper has reached the end of the syringe barrel
Immediately following the intravitreal injection, monitor for elevated IOP; check for perfusion of the optic nerve head or tonometry; if required, a sterile paracentesis needle should be available
Following injection, instruct patient to report any symptoms suggestive of endophthalmitis or retinal detachment (eg, eye pain, redness of the eye, photophobia, blurring of vision) without delay
Vial is for treatment of a single eye; if contralateral eye requires treatment, a new vial should be used and the sterile field, syringe, gloves, drapes, eyelid speculum, filter, and injection needles should be changed before brolucizumab is administered to the other eye
Dispose of unused medicinal product or waste material according to local regulations
Storage
Vial and prefilled syringe
- Refrigerate at 2-8ºC (36-46ºF)
- Unopened glass vial or prefilled syringe may be kept at room temperature (20-25ºC [68-77ºF]) for up to 24 hr
- Do not freeze
- Protect from light
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Formulary
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