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玻璃体内注射VEGF Trap的预测生物学活性。

Predicted biological activity of intravitreal VEGF Trap.

作者信息

Stewart M W, Rosenfeld P J

机构信息

Mayo Clinic College of Medicine, Jacksonville, Florida, USA.

出版信息

Br J Ophthalmol. 2008 May;92(5):667-8. doi: 10.1136/bjo.2007.134874. Epub 2008 Mar 20.

Abstract

AIM

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.

METHODS

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.

RESULTS

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

CONCLUSION

On the basis of this mathematical model, VEGF Trap maintains significant intravitreal VEGF-binding activity for 10-12 weeks after a single injection.

摘要

目的

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。

方法

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)。

结果

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。

结论

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。

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