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Suppression and regression of choroidal neovascularization by the multitargeted kinase inhibitor pazopanib

Kyoichi Takahashi1, Yoshitsugu Saishin, Yumiko Saishin

  • 1Department of Ophthalmology, Johns Hopkins University School of Medicine, Baltimore, Maryland 21287-9277, USA.

Archives of Ophthalmology (Chicago, Ill. : 1960)
|April 15, 2009
PubMed
Abstract

Insights

Pazopanib effectively suppresses choroidal neovascularization (CNV) in mice, showing strong bioavailability to the retina. This kinase inhibitor demonstrates dose-dependent regression of established CNV, suggesting potential human therapeutic applications.

Area of Science:

  • Ophthalmology
  • Pharmacology
  • Biomedical Research

Background:

  • Choroidal neovascularization (CNV) is a leading cause of vision loss.
  • Current treatments for CNV have limitations.
  • Pazopanib is a multitargeted kinase inhibitor with potential anti-angiogenic properties.

Purpose of the Study:

  • To evaluate the efficacy of pazopanib hydrochloride in treating choroidal neovascularization (CNV) in a mouse model.
  • To assess the bioavailability and therapeutic effects of pazopanib on CNV.

Main Methods:

  • CNV was induced in mice using laser photocoagulation to rupture Bruch's membrane.
  • Mice were administered pazopanib via oral gavage or periocular injection.
  • The area of CNV was quantified to measure treatment efficacy.

Main Results:

  • Oral pazopanib (100 mg/kg twice daily) suppressed CNV development by 93%.
  • Established CNV showed dose-dependent regression (58%-71%) with daily oral doses (40-200 mg/kg).
  • Periocular injection also induced significant CNV regression (40%), with good retinal/choroidal bioavailability observed.

Conclusions:

  • Pazopanib demonstrates significant oral bioavailability to the retina and choroid in mice.
  • Pazopanib effectively suppresses CNV development and promotes regression of established CNV.
  • Pazopanib holds promise as a potential therapeutic agent for treating human CNV.

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