Ziv-aflibercept
Other name
-
International/Other brands
Eylea
Groups
Approved
Structure
Prescription products
| Name | Dosage | Strength | Route | Labeller |
|---|---|---|---|---|
| Eylea | Injection, solution | 40 mg/ml | Intravitreal | Bayer Pharma Ag |
| Eylea | Injection, solution | 40 mg/mL | Intravitreal | Regeneron Pharmaceuticals |
| Zaltrap | Solution | 200 mg | Intravenous | Sanofi Aventis |
| Zaltrap | Injection, solution, concentrate | 25 mg/ml | Intravenous | Sanofi Aventis Groupe |
| Zaltrap | Solution | 100 mg | Intravenous | Sanofi Aventis |
| Zaltrap | Solution, concentrate | 100 mg/4mL | Intravenous | Sanofi Aventis |
Target
-
Description
Aflibercept is a recombinant fusion protein that comprises of two main components: the vascular endothelial growth factor (VEGF) binding portions from the extracellular domains of human VEGF receptors 1 and 2 which is then fused to the Fc portion of human 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 carbohydrate 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. Aflibercept, as an ophthalmic agent, is used in the treatment of macular edema following Central Retinal Vein Occlusion (CRVO) and neovascular Age-Related Macular Degeneration (AMD). Ziv-aflibercept, under the brand name Zaltrap, was developed as an injection for treatment of metastatic colorectal cancer. FDA approved in November 18, 2011 and EMA approved in November 2012.
Indications
Metastatic Colorectal Cancers
Other indications
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Mechaism of action
-
Absorption
In patients with wet AMD and CRVO, the mean peak plasma concentration (Cmax) was 0.02 mcg/mL and 0.05 mcg/mL respectively. These concentrations were reached in 1 to 3 days. Aflibercept did not accumulate when administered as repeated doses intravitreally every 4 weeks.
Metabolism
Because aflibercept is a protein, it is expected to be broken down via proteolysis into smaller peptides and amino acids. The cytochrome P450 enzyme system is not involved in the metabolism of aflibercept.
Toxicity
For all intravitreal VEGF inhibitors, there is increased risk of stroke and myocardial infarction. An increase in intraocular pressure may also occur. When used intravenously, most common adverse reactions were leukopenia, diarrhea, neutropenia, proteinuria, AST increased, stomatitis, fatigue, thrombocytopenia, ALT increased, hypertension, weight decreased, decreased appetite, epistaxis, abdominal pain, dysphonia, serum creatinine increased, and headache.