Brolucizumab
Brolucizumab is made from a human antibody fragment. It works by keeping new blood vessels from forming under the retina (a sensory membrane that lines the inside of the eye). In people with certain types of eye disorders, new blood vessels grow under the retina where they leak blood and fluid
Brolucizumab ophthalmic (for the eyes) is used to treat the "wet form" of age-related macular degeneration
Brolucizumab ophthalmic (for the eyes) is used to treat the "wet form" of age-related macular degeneration
Mechanism of effect
Brolucizumab is a recombinant humanized monoclonal antibody vascular endothelial growth factor (VEGF) inhibitor that binds to the 3 major isoforms of VEGF-A, thereby suppressing endothelial cell proliferation, neovascularization, and vascular permeability to slow vision loss
Pharmacokinetics
Metabolism
Not fully characterized; free brolucizumab is expected to undergo proteolysis
Time to reach the peak
Serum: 24 hours (free brolucizumab
Half life: 4.4 ± 2 days
Not fully characterized; free brolucizumab is expected to undergo proteolysis
Time to reach the peak
Serum: 24 hours (free brolucizumab
Half life: 4.4 ± 2 days
Drug indications
Neovascular (wet) age-related macular degeneration: Treatment of neovascular (wet) age-related macular degeneration
Dosage
Usual Adult Dose for Macular Degeneration
Initial dose: 6 mg by intravitreal injection once a month for the first 3 doses
Maintenance dose: 6 mg by intravitreal injection once every 8 to 12 weeks
Initial dose: 6 mg by intravitreal injection once a month for the first 3 doses
Maintenance dose: 6 mg by intravitreal injection once every 8 to 12 weeks
Drug contraindications
Patients with ocular or periocular infections
Patients with active intraocular inflammation
Hypersensitivity to the active drug or any product excipients
Safety and efficacy have not been established in patients younger than 18 years
Hypersensitivity (eg, rash, pruritus, urticaria, erythema, severe intraocular inflammation) to brolucizumab or any component of the formulation; ocular or periocular infections; active intraocular inflammation
Patients with active intraocular inflammation
Hypersensitivity to the active drug or any product excipients
Safety and efficacy have not been established in patients younger than 18 years
Hypersensitivity (eg, rash, pruritus, urticaria, erythema, severe intraocular inflammation) to brolucizumab or any component of the formulation; ocular or periocular infections; active intraocular inflammation
Side effects
>10%
Immunologic: Antibody development
1%
to 10%
Cardiovascular: Arterial thromboembolism
Hypersensitivity: Hypersensitivity reaction
Ophthalmic: Abnormal sensation in eyes, blindness, blurred vision, cataract, conjunctival hemorrhage, conjunctival hyperemia, conjunctivitis, corneal abrasion, endophthalmitis, eye pain, increased intraocular pressure, increased lacrimation, intraocular inflammation, punctate keratitis, retinal artery occlusion, retinal detachment, retinal hemorrhage, retinal hole without detachment, retinal pigment epithelium detachment, retinal pigment epithelium tear, vitreous detachment, vitreous opacity
Postmarketing: Ophthalmic: Retinal vein occlusion
Immunologic: Antibody development
1%
to 10%
Cardiovascular: Arterial thromboembolism
Hypersensitivity: Hypersensitivity reaction
Ophthalmic: Abnormal sensation in eyes, blindness, blurred vision, cataract, conjunctival hemorrhage, conjunctival hyperemia, conjunctivitis, corneal abrasion, endophthalmitis, eye pain, increased intraocular pressure, increased lacrimation, intraocular inflammation, punctate keratitis, retinal artery occlusion, retinal detachment, retinal hemorrhage, retinal hole without detachment, retinal pigment epithelium detachment, retinal pigment epithelium tear, vitreous detachment, vitreous opacity
Postmarketing: Ophthalmic: Retinal vein occlusion
Interactions
There are no known significant interactions
Alerts
This medicine may cause blurred vision and may impair your reactions. Avoid driving or hazardous activity until you know how this medicine will affect you
Intravitreal injections may be associated with endophthalmitis and retinal detachment. Use proper aseptic injection technique. Monitor for and report symptoms (eg, eye pain, redness of the eye, photophobia, blurred vision) immediately
Acute (within 30 minutes) and sustained increases in increased intraocular pressure (IOP) have occurred. Monitor IOP (via tonometry) and optic nerve head perfusion immediately following administration and manage appropriately
Cases of retinal vasculitis and/or retinal vascular occlusion have been reported; usually associated with intraocular inflammation. Monitor for and report any changes in vision immediately
Risk of arterial thromboembolic events (eg, nonfatal stroke, nonfatal myocardial infarction, vascular death) may be increased with intravitreal use of vascular endothelial growth factor inhibitors
Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect
Vision changes
Eye pain
Severe eye irritation
Eye redness
Cataracts
Sensitivity to light
Heart attack like chest pain; pain in arms, back, neck, jaw, or abdomen; shortness of breath; cold sweats; severe dizziness; passing out; or severe nausea or vomiting
Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight
Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat
Intravitreal injections may be associated with endophthalmitis and retinal detachment. Use proper aseptic injection technique. Monitor for and report symptoms (eg, eye pain, redness of the eye, photophobia, blurred vision) immediately
Acute (within 30 minutes) and sustained increases in increased intraocular pressure (IOP) have occurred. Monitor IOP (via tonometry) and optic nerve head perfusion immediately following administration and manage appropriately
Cases of retinal vasculitis and/or retinal vascular occlusion have been reported; usually associated with intraocular inflammation. Monitor for and report any changes in vision immediately
Risk of arterial thromboembolic events (eg, nonfatal stroke, nonfatal myocardial infarction, vascular death) may be increased with intravitreal use of vascular endothelial growth factor inhibitors
Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect
Vision changes
Eye pain
Severe eye irritation
Eye redness
Cataracts
Sensitivity to light
Heart attack like chest pain; pain in arms, back, neck, jaw, or abdomen; shortness of breath; cold sweats; severe dizziness; passing out; or severe nausea or vomiting
Weakness on 1 side of the body, trouble speaking or thinking, change in balance, drooping on one side of the face, or blurred eyesight
Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat
Points of recommendation
You should not use brolucizumab if you are allergic to it, or if you have
inflammation inside your eye
an infection in or around your eye
Tell your doctor if you have ever had
glaucoma
cataracts
a stroke
Do not use brolucizumab if you are pregnant. It could harm the unborn baby or cause birth defects. Use effective birth control to prevent pregnancy while you are receiving brolucizumab ophthalmic and for at least 1 month after your last dose
Do not breastfeed while receiving this medicine, and for at least 1 month after your last dose
Brolucizumab is given as an injection into your eye. Your doctor will use a medicine to numb your eye before giving you the injection. You will receive this injection in your doctor's office or other clinic setting
For a short time after your injection, your eyes will be checked periodically to make sure the injection has not caused any side effects
Brolucizumab is usually given once per month for 3 months, and then once every 8 to 12 weeks
Follow your doctor's dosing instructions very carefully. The timing of your monthly injections is very important for this medication to be effective
This drug should be administered by a qualified physician
Once monthly injections should be administered approximately every 25 to 31 days
In clinical trials, the maintenance dosing interval was guided by visual and anatomical measures of disease activity; the utility of these measures has not been established
Store refrigerated 2C to 8C; do not freeze
Prior to use, keep in outer carton to protect from light
Prior to use, the unopened vial may be kept at room temperature 20C to 25C for up to 24 hours
Injection should occur immediately after dose preparation; the product labeling may be consulted for injection procedure
A single vial should be used to treat a single eye; if the 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 administration to the other eye
inflammation inside your eye
an infection in or around your eye
Tell your doctor if you have ever had
glaucoma
cataracts
a stroke
Do not use brolucizumab if you are pregnant. It could harm the unborn baby or cause birth defects. Use effective birth control to prevent pregnancy while you are receiving brolucizumab ophthalmic and for at least 1 month after your last dose
Do not breastfeed while receiving this medicine, and for at least 1 month after your last dose
Brolucizumab is given as an injection into your eye. Your doctor will use a medicine to numb your eye before giving you the injection. You will receive this injection in your doctor's office or other clinic setting
For a short time after your injection, your eyes will be checked periodically to make sure the injection has not caused any side effects
Brolucizumab is usually given once per month for 3 months, and then once every 8 to 12 weeks
Follow your doctor's dosing instructions very carefully. The timing of your monthly injections is very important for this medication to be effective
This drug should be administered by a qualified physician
Once monthly injections should be administered approximately every 25 to 31 days
In clinical trials, the maintenance dosing interval was guided by visual and anatomical measures of disease activity; the utility of these measures has not been established
Store refrigerated 2C to 8C; do not freeze
Prior to use, keep in outer carton to protect from light
Prior to use, the unopened vial may be kept at room temperature 20C to 25C for up to 24 hours
Injection should occur immediately after dose preparation; the product labeling may be consulted for injection procedure
A single vial should be used to treat a single eye; if the 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 administration to the other eye
Pregnancy level
Brolucizumab is a vascular endothelial growth factor (VEGF) inhibitor; VEGF is required to achieve and maintain normal pregnancies. Based on findings in animal reproduction studies and on the mechanism of action, brolucizumab may cause fetal harm if administered to a pregnant female
Drug forms
Beovu
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