Introduction
Zaltrap IV Infusion 100 mg/4 ml is a recombinant fusion protein that binds vascular endothelial growth factor (VEGF), preventing it from activating its receptors and thereby inhibiting abnormal blood vessel growth and vascular leakage. It is used as an ophthalmic agent for the treatment of neovascular age-related macular degeneration (AMD), diabetic macular edema (DME), diabetic retinopathy, and macular edema following retinal vein occlusion.
Zaltrap IV Infusion 100 mg/4 ml is also available as ziv-aflibercept for the treatment of metastatic colorectal cancer. By blocking VEGF-mediated angiogenesis, it helps slow tumor growth and reduce disease progression.
Uses
Zaltrap IV Infusion 100 mg/4 ml is a vascular endothelial growth factor (VEGF) inhibitor used to treat Neovascular (Wet) Age-Related Macular Degeneration (AMD), various types of macular edema and diabetic retinopathy.
The opthalmic agent is used for the treatment of neovascular (wet) age-related mascular degeneration (AMD) and macular edema following central retinal vein occulsion (CRVO). 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
Pharmacodynamics
Compared to other anti-VEGF drugs like bevacizumab and ranibizumab, aflibercept has a higher binding affinity to VEGF-A (Kd = 0.5 pM).
Mechanism of Action
Ablibercept is a recombinant fusion protein that acts as a decoy receptor for the ligands, vascular endothelial growth factor-A (VEGF-A) and placental growth factor (PIGF). It prevents these ligands to binding to endothelial receptors, VEGFR-1 and VEGFR-2, to suppress neovascularization and decrease vascular permeability. This ultimately will slow vision loss or the progression of metastatic colorectal cancer.
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. Zaltrap IV Infusion 100 mg/4 ml did not accumulate when administered as repeated doses intravitreally every 4 weeks.
Volume of Distribution
After intravenous injection of aflibercept, the volume of distribution is 6 L.
Route of Elimination
Via kidney and liver
Half Life
Intravitreal half-life= 7.13 days in humans; Terminal elimination half-life of free aflibercept in plasma was 5 to 6 days after IV injection of 2 - 4 mg/kg dose.
Clearance
When cancer patients were given 2-9 mg/kg every 2 or 3 week; 1 hour IV infusion of aflibercept the typical estimated clearances were as follows: CL of free aflibercept (CLf) = 0.88 L/day; CL of bound aflibercept (CLf) = 0.19 L/day; Patients clear free aflibercept faster if they had low albumin or high alkaline phosphatase levels.
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.
Food Interactions
No interactions found.
