Anti-angiogenic effects of the receptor tyrosine kinase inhibitor, pazopanib, on choroidal neovascularization in rats

Assessing a Novel Depot Delivery Strategy for Noninvasive Administration of VEGF/PDGF RTK Inhibitors for Ocular Neovascular Disease

“…Topical pazopanib did not suppress CNV at any of the concentrations tested, but topical GW771806 at 5 mg/mL significantly suppressed and, in fact, regressed CNV. The effect of 5 mg/mL topical pazopanib is in contrast to previous studies showing an effect in limiting lesion progression, 31 but in those studies topical pazopanib was dosed immediately after FA analysis (day 7), whereas in our studies the drug was not dosed until day 10. The efficacy differences between pazopanib and GW771806 cannot entirely be explained by the higher depot levels, since GW771806 and pazopanib topically administered at 2 mg/mL were found at similar levels in the RPE/choroid, yet only GW771806 significantly suppressed CNV.…”

Clinical Application of Drug Delivery Systems for Treating AMD

“…Yafai et al have demonstrated that eye-drop formulation of pazopanib complexed with cyclodextrin significantly inhibited CNV in laser-induced CNV rat model (Yafai et al, 2011). Since this effect was obtained by overdose of eye-drops (30 µL/eye), it is doubtful whether this effective inhibition of CNV resulted from a topical absorption of pazopanib.…”

Clinical Evaluation of Pazopanib Eye Drops in Healthy Subjects and in Subjects With Neovascular Age-Related Macular Degeneration

“…12 Distribution studies have indicated a conjunctival/scleral route of topical ocular pazopanib to the choroid and retina, and twice-daily oral/periocular or topical dosing prevented the progression of laser-induced CNV in mice and rats, respectively. 13,14 A topical ocular formulation of pazopanib, which has the potential to provide a more convenient therapy that can be self-administered by the patient, is under investigation for the treatment of neovascular AMD. This article describes the results of 2 clinical studies conducted with topical ocular pazopanib.…”