April 2010
Volume 51, Issue 13
Free
ARVO Annual Meeting Abstract  |   April 2010
Pharmacokinetics of Bevacizumab and Its Effect on Vascular Endothelial Growth Factor After Intravitreal Injection of Bevacizumab in Macaque Eyes
Author Affiliations & Notes
  • T. Miyake
    Ophthalmology,
    Shiga University of Medical Science, Otsu, Japan
  • O. Sawada
    Ophthalmology, Shiga Univ of Medical Science, Otsu, Japan
  • M. Kakinoki
    Ophthalmology,
    Shiga University of Medical Science, Otsu, Japan
  • T. Sawada
    Ophthalmology,
    Shiga University of Medical Science, Otsu, Japan
  • H. Kawamura
    Ophthalmology,
    Shiga University of Medical Science, Otsu, Japan
  • M. Ohji
    Department of Ophthalmology,
    Shiga University of Medical Science, Otsu, Japan
Investigative Ophthalmology & Visual Science April 2010, Vol.51, 4505. doi:
  • Views
  • Share
  • Tools
    • Alerts
      ×
      This feature is available to authenticated users only.
      Sign In or Create an Account ×
    • Get Citation

      T. Miyake, O. Sawada, M. Kakinoki, T. Sawada, H. Kawamura, M. Ohji; Pharmacokinetics of Bevacizumab and Its Effect on Vascular Endothelial Growth Factor After Intravitreal Injection of Bevacizumab in Macaque Eyes. Invest. Ophthalmol. Vis. Sci. 2010;51(13):4505.

      Download citation file:


      © ARVO (1962-2015); The Authors (2016-present)

      ×
  • Supplements
Abstract

Purpose: : To evaluate the pharmacokinetics of intravitreally injected bevacizumab in the systemic circulation and the aqueous humor and its effect on vascular endothelial growth factor (VEGF) in the aqueous humor.

Methods: : Bevacizumab (1.25 mg/50 µl) was injected into the vitreous cavity of the right eyes of three cynomolgus macaques. Aqueous humor and serum were obtained from the macaques just before injection and on days 1, 3, and 7, and weeks 2, 4, 6, 8 after the injection. The bevacizumab and VEGF concentrations were measured using enzyme-linked immunosorbent assay.

Results: : The aqueous VEGF concentrations ranged from 63.2 to 106 pg/ml (mean, 80.0 ± 22.6 pg/ml) before the injection; decreased to less than 31.2 pg/ml, the lower limit of detection, in all eyes between 1 and 28 days after the injection; and returned to the pre-injection level at 42 days. The aqueous VEGF concentrations in the fellow eyes did not change throughout the experiment. Aqueous bevacizumab concentrations in the treated eyes reached a mean peak concentration of 49,500 ± 10,900 ng/ml the day after the injection and gradually declined, while those in the untreated eyes peaked at 3 days with a mean concentration of 18.5 ± 25.5 ng/ml and declined to below 0.156 ng/ml, the limit of detection at 2 weeks. A maximum mean bevacizumab concentration of 1,430 ± 186 ng/ml was achieved in the serum 1 week after the injection. The half-life of 1.25 mg of intravitreally injected bevacizumab was 2.8±0.6 days(n=3;range2.3-3.5) in the aqueous humor and 12.3±2.6 days (n=3; range, 9.2-14.1) in the serum.

Conclusions: : Intravitreal injection of bevacizumab decreased the VEGF concentration in the treated eyes for at least 4 weeks and had no or a minimal effect on the untreated fellow eyes.

Keywords: vascular endothelial growth factor • drug toxicity/drug effects 
×
×

This PDF is available to Subscribers Only

Sign in or purchase a subscription to access this content. ×

You must be signed into an individual account to use this feature.

×