aflibercept

aflibercept

Eylea

Pharmacologic class: Vascular endothelial growth factor (VEGF) inhibitor

Therapeutic class: Ophthalmic agent

Pregnancy risk category C

Action

VEGF-A and placental growth factor (PlGF) are members of the VEGF family of angiogenic factors that can act as mitogenic, chemotactic, and vascular permeability factors for endothelial cells. VEGF acts via two receptor tyrosine kinases, VEGFR-1 and VEGFR-2, present on the surface of endothelial cells. PlGF binds only to VEGFR-1, which is also present on the surface of leucocytes. Activation of these receptors by VEGF-A can result in neovascularization and vascular permeability. Aflibercept acts as a soluble decoy receptor that binds VEGF-A and PlGF, and thereby can inhibit the binding and activation of these cognate VEGF receptors.

Availability

Solution for ophthalmic injection: 40 mg/ml in 3-ml (0.278-ml fill) single-use vials

Indications and dosages

Neovascular (wet) age-related macular degeneration

Adults: 2 mg (0.05 ml) by intravitreal injection into affected eye q 4 weeks for the first 3 months, followed by 2 mg (0.05 ml) once q 8 weeks

Contraindications

• Hypersensitivity to drug or its components
• Ocular or periocular infection
• Active intraocular inflammation

Precautions

Use cautiously in:
• pregnant or breastfeeding patients
• children (safety and efficacy not established).

Administration

• Be aware that drug should be administered by ophthalmic intravitreal injection only under controlled aseptic conditions by a qualified health care professional.
• Provide adequate anesthesia and a topical broad-spectrum anti-infective before the injection, as prescribed.
• Inspect drug for particulate matter and discoloration before administering.
• Use a filter needle to draw up the prescribed dose; remove the filter needle from syringe, and attach a 30G, ½-inch injection needle for the intravitreal injection. Discard unused drug after injection.
• Be aware that each vial should only be used for the treatment of a single eye. If the contralateral eye requires treatment, use a new vial and change all equipment.
• Immediately following the intravitreal injection, assess patient for increased intraocular pressure (IOC).

Adverse reactions

CNS: nonfatal stroke

CV: nonfatal MI, vascular death

EENT: conjunctival hyperemia, conjunctival hemorrhage, eye pain, cataract, vitreous detachment, vitreous floaters, increased IOC, endophthalmitis, corneal erosion, corneal edema, retinal detachment, retinal tear, retinal pigment epithelium tear, injection-site pain, injection-site hemorrhage, foreign body sensation in eye, increased lacrimation, blurred vision, eyelid edema

Other: hypersensitivity

Interactions

None

Patient monitoring

• Continue to monitor patient for increased IOP, endophthalmitis, retinal detachment, and arterial thromboembolic events and be prepared to treat appropriately.

Patient teaching

Instruct patient to contact ophthalmologist immediately if treated eye becomes red, light sensitive, or painful, or if vision change occurs.

Instruct patient to immediately report signs and symptoms of stroke (such as weakness on one side of body or slurred speech), chest pain, or other new signs and symptoms.
• Caution patient to avoid driving and other hazardous activities until visual function has recovered sufficiently.
• As appropriate, review all other significant and life-threatening adverse reactions mentioned above.

Mentioned in ?
References in periodicals archive ?
Contract notice: Ranibizumab drug delivery and drug aflibercept.
The antivascular endothelial growth factor (VEGF) ranibizumab (Lucentis) and aflibercept (EYLEA) and the intraocular corticosteroids dexamethasone (Ozurdex) and fluocinolone acetonide (ILUVIEN) are approved for treating diabetic macular edema (DME) in the US.
In the UK, the first prominent approved anti-VEGF drug was pegaptanib (Macugen), which has now been replaced by the more effective anti-VEGF agents ranibizumab (Lucentis) and aflibercept (VEGF-trap, Eylea) (14) although pegaptanib is still available for about 9,000[pounds sterling] for a two-year course.
Addition of aflibercept to fluorouracil, leucovorin, and irinotecan improves survival in a phase III randomized trial in patients with metastatic colorectal cancer previously treated with an oxaliplatin-based regimen.
The drug, aflibercept (marketed as Eylea or Zaltrap), is used to treat metastatic colorectal cancer and a form of macular degeneration.
In the recent months it reached important milestones with products such as anticoagulant Xarelto, cancer drugs Stivarga and Radium-223 dichloride (Alpharadin), eye medicine Aflibercept as well as Riociguat -- a therapy for pulmonary hypertension.
Aflibercept is among six medicines that Regeneron, with one approved drug, has in the last stages of human tests needed to begin selling another product.
Given the positive recommendation by the Committee for Medicinal Products for Human Use (CHMP) for the approval of Bayer's aflibercept (VEGF Trap-Eye) for the treatment of wet AMD during study fielding, it is interesting to note that 69 percent of retinal specialists who report unaided awareness of products in development for wet AMD specifically mention aflibercept.
Contract notice: Medication delivery of the drug program: alfaglucosidase alpha and aflibercept.
You should not use EYLEA if you have an infection in or around the eye, eye pain or redness, or known allergies to any of the ingredients in EYLEA, including aflibercept.
The drug, called Aflibercept, which is administered as a 30-minute infusion alongside chemotherapy, uses a novel mechanism that effectively fools tumours into becoming dormant.
The results of the Phase III study were very encouraging with the majority of patients experiencing a significant two-line improvement in visual acuity on a standard eye chart with aflibercept solution for injection , said Dr.