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Title: Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration
Authors: Meredith, Erik L.
Mainolfi, Nello
Poor, Stephen
Qiu, Yubin
Miranda, Karl
Powers, James
Liu, Donglei
Ma, Fupeng
Solovay, Catherine
Rao, Chang
Johnson, Leland
Ji, Nan
Artman, Gerald
Hardegger, Leo
Hanks, Shawn
Shen, Siyuan
Woolfenden, Amber
Fassbender, Elizabeth
Sivak, Jeremy M.
Zhang, Yiqin
Long, Debby
Cepeda, Rosemarie
Liu, Fang
Hosagrahara, Vinayak P.
Lee, Wendy
Tarsa, Peter
Anderson, Karen
Elliott, Jason
Jaffee, Bruce
Keywords: pyrimidine derivative
capsule endoscope
Issue Date: 2015
Source: Meredith, E. L., Mainolfi, N., Poor, S., Qiu, Y., Miranda, K., Powers, J., et al. (2015). Discovery of Oral VEGFR-2 Inhibitors with Prolonged Ocular Retention That Are Efficacious in Models of Wet Age-Related Macular Degeneration. Journal of Medicinal Chemistry, 58(23), 9273-9286.
Series/Report no.: Journal of Medicinal Chemistry
Abstract: The benefit of intravitreal anti-VEGF therapy in treating wet age-related macular degeneration (AMD) is well established. Identification of VEGFR-2 inhibitors with optimal ADME properties for an ocular indication provides opportunities for dosing routes beyond intravitreal injection. We employed a high–throughput in vivo screening strategy with rodent models of choroidal neovascularization and iterative compound design to identify VEGFR-2 inhibitors with potential to benefit wet AMD patients. These compounds demonstrate preferential ocular tissue distribution and efficacy after oral administration while minimizing systemic exposure.
ISSN: 0022-2623
DOI: 10.1021/acs.jmedchem.5b01227
Schools: School of Biological Sciences 
Rights: © 2015 American Chemical Society. This paper was published in Journal of Medicinal Chemistry and is made available as an electronic reprint (preprint) with permission of American Chemical Society. The published version is available at: []. One print or electronic copy may be made for personal use only. Systematic or multiple reproduction, distribution to multiple locations via electronic or other means, duplication of any material in this paper for a fee or for commercial purposes, or modification of the content of the paper is prohibited and is subject to penalties under law.
Fulltext Permission: open
Fulltext Availability: With Fulltext
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