Brolucizumab

Brolucizumab is a human vascular endothelial growth factor (VEGF) inhibitor indicated for the treatment of:

• Neovascular (Wet) Age-Related Macular Degeneration (AMD)
• Diabetic Macular Edema (DME)

Brolucizumab is a human VEGF inhibitor. Brolucizumab binds to the three major isoforms of VEGF-A (e.g., VEGF 110, VEGF 121, and VEGF 165), thereby preventing interaction with receptors VEGFR-1 and VEGFR-2. By inhibiting VEGF-A, brolucizumab suppresses endothelial cell proliferation, neovascularization, and vascular permeability. Leakage of blood and fluid from choroidal neovascularization (CNV) may cause retinal thickening or edema. Increased retinal thickness and accumulation of intraretinal fluid (IRF)/subretinal fluid (SRF), assessed by optical coherence tomography (OCT), is associated with nAMD and DME. Reductions in central retinal subfield thickness (CST) were observed across all treatment arms.

Neovascular (Wet) Age-Related Macular Degeneration (AMD): The recommended dose for BEOVU is 6 mg (0.05 mL of 120 mg/mL solution) monthly (approximately every 25-31 days) for the first three doses, followed by one dose of 6 mg (0.05 mL) every 8-12 weeks.

Diabetic Macular Edema (DME): The recommended dose for BEOVU is 6 mg (0.05 mL of 120 mg/mL solution) every six weeks (approximately every 39-45 days) for the first five doses, followed by one dose of 6 mg (0.05 mL of 120 mg/mL solution) every 8-12 weeks.

Pediatric Use: The safety and efficacy of BEOVU in pediatric patients has not been established.

Ocular or Periocular Infections: Brolucizumab is contraindicated in patients with ocular or periocular infections.

Active Intraocular Inflammation: Brolucizumab is contraindicated in patients with active intraocular inflammation.

Hypersensitivity: Brolucizumab is contraindicated in patients with known hypersensitivity to brolucizumab or any of the excipients in Brolucizumab. Hypersensitivity reactions may manifest as rash, pruritus, urticaria, erythema, or severe intraocular inflammation.

The most common adverse reactions reported in patients receiving Brolucizumab are vision blurred, cataract, conjunctival hemorrhage, eye pain, and vitreous floaters.

There are no adequate and well-controlled studies of BEOVU administration in pregnant women. In an animal reproduction study, intravitreal administration of brolucizumab to pregnant monkeys once every 4 weeks in one eye from organogenesis to birth caused fetal loss and a structural abnormality (bilateral absent metatarsal) in offspring at 10-fold the maximum recommended human dose (MRHD) on a mg/kg basis. 

There is no information 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 one month after the last dose when stopping treatment with Brolucizumab.

• Endophthalmitis and retinal detachment may occur following intravitreal injections. Patients should be instructed to report any symptoms suggestive of endophthalmitis or retinal detachment without delay.
• Retinal vasculitis and/or retinal vascular occlusion, typically in the presence of intraocular inflammation, have been reported following BEOVU injections. Patients should be instructed to report any change in vision without delay.
• Increases in intraocular pressure (IOP) have been seen within 30 minutes of an intravitreal injection.
• There is a potential risk of arterial thromboembolic events (ATE) following intravitreal use of VEGF inhibitors

Refrigerate Brolucizumab between 2°C to 8°C. Do not freeze. Store Brolucizumab in the outer carton to protect from light. Prior to use, the unopened glass vial or sealed blister pack of Brolucizumab may be kept at room temperature, 20°C to 25°C for up to 24 hours.