Aflibercept

Generic Name
Aflibercept
Brand Names
Eylea, Zaltrap, Yesafili
Drug Type
Biotech
Chemical Formula
-
CAS Number
862111-32-8
Unique Ingredient Identifier
15C2VL427D
Background

Aflibercept is a recombinant protein composed of the binding domains of two human vascular endothelial growth factor (VEGF) receptors, VEGFR1 and VEGFR2, fused with the Fc region of human immunoglobulin gamma 1 (IgG1). Structurally, Aflibercept is a dimeric glycoprotein with a protein molecular weight of 96.9 kilo Daltons (kDa). It contains approximately 15% glycosylation to give a total molecular weight of 115 kDa. All five putative N-glycosylation sites on each polypeptide chain predicted by the primary sequence can be occupied with carbohydrates and exhibit some degree of chain heterogeneity, including heterogeneity in terminal sialic acid residues, except at the single unsialylated site associated with the Fc domain. Due to the 2 fused VEGFR, aflibercept has a higher affinity to the cognate ligands than the endogenous individual receptor. However, it lacks the intracellular structure to propagate subsequent signal transduction, thus essentially sequestering the ligands to prevent activation of VEGFR.

Ziv-aflibercept, under the brand name Zaltrap, was developed as an intravenous injection for the treatment of metastatic colorectal cancer, and it was approved by the FDA and EMA in August 2012 and February 2013, respectively. The intravitreal formulation, under the brand name EYELEA, was approved by the FDA for the treatment of retinopathy of prematurity in preterm infants in February 2023 and for the treatment of wet age-related macular degeneration, diabetic macular edema, and diabetic retinopathy in August 2023.

Indication

The opthalmic agent is used for the treatment of neovascular (Wet) age-related macular degeneration (AMD), macular edema following retinal vein occlusion (RVO), diabetic macular edema (DME), diabetic retinopathy (DR), and retinopathy of prematurity (ROP).

The systemic injection, known as ziv-aflibercept, in combination with 5-fluorouracil, leucovorin, irinotecan-(FOLFIRI), is for the treatment of metastatic colorectal cancer that is resistant to or progressed following treatment with oxaliplatin.

Associated Conditions
Branch Retinal Vein Occlusion With Macular Edema, Diabetic Macular Edema (DME), Diabetic Retinopathy (DR), Macular Edema, Macular Edema With Central Retinal Vein Occlusions, Metastatic Colorectal Cancer (CRC), Myopic Choroidal Neovascularization, Neovascular Age-Related Macular Degeneration (nAMD), Retinopathy of Prematurity (ROP)
Associated Therapies
-

VITAL - Individualising Therapy for Neovascular AMD With Aflibercept

First Posted Date
2015-05-12
Last Posted Date
2018-05-23
Lead Sponsor
Moorfields Eye Hospital NHS Foundation Trust
Target Recruit Count
50
Registration Number
NCT02441816
Locations
🇬🇧

Moorfields Eye Hospital NHS Foundation Trust, London, United Kingdom

Laser Therapy Combined With Intravitreal Aflibercept vs Intravitreal Aflibercept Monotherapy (LADAMO)

First Posted Date
2015-05-04
Last Posted Date
2022-05-31
Lead Sponsor
University of Sydney
Target Recruit Count
48
Registration Number
NCT02432547
Locations
🇦🇺

Centre for Eye Research Australia, Melbourne, Victoria, Australia

🇦🇺

Save Sight Institute, Sydney, New South Wales, Australia

Intravitreal Aflibercept Injection for Symptomatic Macular Edema From Retinal Artery Macroaneurysms

First Posted Date
2015-03-31
Last Posted Date
2019-08-08
Lead Sponsor
Kamal Kishore, MD
Target Recruit Count
6
Registration Number
NCT02403128
Locations
🇺🇸

Illinois Retina and Eye Associates, Peoria, Illinois, United States

A Safety and Efficacy Study of DE-120 Injectable Solution for Age-related Macular Degeneration

First Posted Date
2015-03-30
Last Posted Date
2018-04-18
Lead Sponsor
Santen Inc.
Target Recruit Count
16
Registration Number
NCT02401945

Aflibercept +/- LV5FU2 in First Line of Non-resectalbe Metastatic Colorectal Cancers

Phase 2
Completed
Conditions
Interventions
First Posted Date
2015-03-10
Last Posted Date
2024-07-10
Lead Sponsor
Federation Francophone de Cancerologie Digestive
Target Recruit Count
117
Registration Number
NCT02384759
Locations
🇫🇷

CHU Amiens - Hôpital Nord, Amiens CEDEX 1, France

🇫🇷

ICO, Saint Herblain, France

🇫🇷

CH, Perpignan, France

and more 46 locations

Efficacy of Aflibercept (Eylea®) on Choroidal Neovascularization (Type 3)

Phase 4
Completed
Conditions
Interventions
First Posted Date
2014-12-19
Last Posted Date
2019-03-08
Lead Sponsor
Poitiers University Hospital
Target Recruit Count
26
Registration Number
NCT02320474
Locations
🇫🇷

Poitiers University Hospital, Poitiers, France

🇫🇷

Polyclinic of POITIERS, Poitiers, France

Long-Term Efficacy & Safety of Aflibercept IVT for the Treatment of DME in Subjects Who Completed the VISTA-DME Trial

First Posted Date
2014-11-24
Last Posted Date
2019-06-04
Lead Sponsor
Greater Houston Retina Research
Target Recruit Count
60
Registration Number
NCT02299336
Locations
🇺🇸

Retina Consultants of Houston/The Medical Center, Houston, Texas, United States

🇺🇸

Retina Consultants of Houston, The Woodlands, Texas, United States

🇺🇸

Retina Consultants of Houston/Katy office, Katy, Texas, United States

Testing the PD-1 Antibody, MK3475, Given With Ziv-aflibercept in Patients With Advanced Cancer

First Posted Date
2014-11-24
Last Posted Date
2024-12-04
Lead Sponsor
National Cancer Institute (NCI)
Target Recruit Count
78
Registration Number
NCT02298959
Locations
🇺🇸

National Institutes of Health Clinical Center, Bethesda, Maryland, United States

🇨🇦

University Health Network-Princess Margaret Hospital, Toronto, Ontario, Canada

🇺🇸

National Cancer Institute Developmental Therapeutics Clinic, Bethesda, Maryland, United States

and more 6 locations
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