Stewart M W, Rosenfeld P J
Mayo Clinic College of Medicine, Jacksonville, Florida, USA.
Br J Ophthalmol. 2008 May;92(5):667-8. doi: 10.1136/bjo.2007.134874. Epub 2008 Mar 20.
To compare the intravitreal binding activity of VEGF Trap with that of ranibizumab against vascular endothelial growth factor (VEGF) using a time-dependent and dose-dependent mathematical model.
Intravitreal half-lives and relative equimolar VEGF-binding activities of VEGF Trap and ranibizumab were incorporated into a first-order decay model. Time-dependent VEGF Trap activities (relative to ranibizumab) for different initial doses (0.5, 1.15, 2 and 4 mg) were calculated and plotted.
Seventy-nine days after a single VEGF Trap (1.15 mg) injection, the intravitreal VEGF-binding activity would be comparable to ranibizumab at 30 days. After injection of 0.5, 2 and 4 mg VEGF Trap, the intravitreal VEGF-binding activities (comparable to ranibizumab at 30 days) would occur at 73, 83 and 87 days, respectively
On the basis of this mathematical model, VEGF Trap maintains significant intravitreal VEGF-binding activity for 10-12 weeks after a single injection.
使用时间依赖性和剂量依赖性数学模型比较VEGF Trap与雷珠单抗在玻璃体内对血管内皮生长因子(VEGF)的结合活性。
将VEGF Trap和雷珠单抗在玻璃体内的半衰期及相对等摩尔VEGF结合活性纳入一级衰变模型。计算并绘制不同初始剂量(0.5、1.15、2和4mg)下时间依赖性VEGF Trap活性(相对于雷珠单抗)。
单次注射VEGF Trap(1.15mg)79天后,玻璃体内VEGF结合活性在30天时将与雷珠单抗相当。注射0.5、2和4mg VEGF Trap后,玻璃体内VEGF结合活性(在30天时与雷珠单抗相当)分别在73、83和87天时出现。
基于该数学模型,单次注射后VEGF Trap在玻璃体内可维持显著的VEGF结合活性达10至12周。