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 ?
0 million related to the aflibercept collaboration and $85.
Tenders are invited for Inj Aflibercept Eylea Vial With Needle
In May 2008, Regeneron and sanofi-aventis reported results of a randomized, double-blind, Phase 2 study of 215 women with advanced ovarian cancer (AOC) who were treated with aflibercept as a single-agent at a dose of either 2 milligrams per kilogram (mg/kg) or 4 mg/kg every two weeks.
Nasdaq: REGN) today provided an update on the clinical development program for aflibercept, including results from a Phase 2 study in advanced ovarian cancer.
today announced topline results from the Phase 2 CAPELLA study evaluating aflibercept co-formulated with rinucumab, an anti-plateletderived growth factor receptor beta (anti-PDGFR-beta) antibody, in patients with neovascular age-related macular degeneration (wet AMD).
Contract research and development revenue in the first quarter of 2008 principally related to the Company's aflibercept and antibody collaborations with sanofi-aventis and the Company's VEGF Trap-Eye collaboration with Bayer HealthCare.
Procurement of aflibercept and ranibizumab ( anti-VEGF ) on the requisition in 2017 , SLL450 , the Stockholm County Council and Region Gotland .
M2 EQUITYBITES-August 1, 2014-Bayer receives approval for aflibercept eye injection solution
M2 PHARMA-August 1, 2014-Bayer receives approval for aflibercept eye injection solution
Regeneron has three late-stage clinical development programs: ARCALYST[TM] (rilonacept; also known as IL-1 Trap) in Cryopyrin-Associated Periodic Syndromes (CAPS), aflibercept (the VEGF Trap) in oncology in collaboration with the sanofi-aventis Group, and the VEGF Trap-Eye in eye diseases in collaboration with Bayer HealthCare.
Emerging antiangiogenic agents: Adnexus's Angiocept, Amgen's AMG-386, AstraZeneca's cediranib, AstraZeneca's Zactima, Celgene's thalidomide derivatives, GlaxoSmithKline's pazopanib, MedImmune's abegrin, Merck KGaA's cilengitide, Novartis's vatalanib, PDL BioPharma/Biogen Idec's volociximab, Pfizer's axitinib, Regeneron/Sanofi -Aventis's aflibercept, UCB/ImClone's CDP- 791.
1 Ophthalmological - active ingredient - Aflibercept.