Pharmacokinetic properties of intravitreal I-124-aflibercept in a rabbit model using PET/CT

Curr Eye Res. 2012 Dec;37(12):1171-4. doi: 10.3109/02713683.2012.727521. Epub 2012 Sep 19.

Abstract

Purpose: To determine the anatomic characteristics and pharmacokinetic properties of intravitreally-placed aflibercept in a rabbit model.

Materials and methods: Four Dutch-belted rabbits underwent intravitreal injection with I-124-aflibercept. Serial imaging with PET/CT imaging was performed on days 0, 2, 5, 7, 14, 21, 28 and 35. Measured radioactivity emission in becquerels/mL was used to calculate the half-lives for aflibercept.

Results: I-124 aflibercept was confined within the vitreous cavity for the duration of the study. I-124 aflibercept could be detected in the vitreous cavity until day 28 and the average retention time with standard error after correction for radioactive decay was 4.58 ± 0.07 days.

Conclusions: I-124 aflibercept was only visible in the vitreous cavity by PET/CT imaging following intravitreal injection. The retention properties were found to be comparable to those measured by other reported methods.

MeSH terms

  • Animals
  • Half-Life
  • Intravitreal Injections
  • Iodine Radioisotopes
  • Models, Animal
  • Multimodal Imaging
  • Positron-Emission Tomography
  • Rabbits
  • Receptors, Vascular Endothelial Growth Factor / pharmacokinetics*
  • Recombinant Fusion Proteins / pharmacokinetics*
  • Thyroid Gland / diagnostic imaging
  • Thyroid Gland / metabolism
  • Tomography, X-Ray Computed
  • Vascular Endothelial Growth Factor A / antagonists & inhibitors
  • Vitreous Body / diagnostic imaging
  • Vitreous Body / metabolism*

Substances

  • Iodine Radioisotopes
  • Recombinant Fusion Proteins
  • Vascular Endothelial Growth Factor A
  • aflibercept
  • Receptors, Vascular Endothelial Growth Factor