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Discovery of Oral VEGFR-2 Inhibitors That Provide Sustained Ocular Retention and Efficacy in Models of Wet-AMD

Meredith, Erik and Mainolfi, Nello and Poor, Stephen and Qiu, Yubin and Miranda, Karl and Powers, James and Liu, Donglei and Ma, Fupeng and Solovay, Catherine and Rao, Chang and Johnson, Leland and Ji, Nan and Artman Iii, Gerald and Hardegger, Leo and Elliott, Jason and Hanks, Shawn and Shen, Siyuan and Woolfenden, Amber and Zhang, Yiqin and Sivak, Jeremy and Long, Debby and Cepeda, Rosemarie and Hosagrahara, Vinayak and Lee, Wendy and Tarsa, Peter and Liu, Fang and Anderson, Karen and Jaffee, Bruce (2015) Discovery of Oral VEGFR-2 Inhibitors That Provide Sustained Ocular Retention and Efficacy in Models of Wet-AMD. Journal of Medicinal Chemistry.

Abstract

The benefit of intravitreal anti-VEGF therapy in treating wet age-related macular degeneration (AMD) has been well established. Identification of suitable VEGFR-2 inhibitors would provide alternative dosing opportunities beyond intravitreal injection. To identify such inhibitors, we employed a high–throughput in vivo screening strategy with a model of choroidal neovascularization and iterative compound design to provide VEGFR-2 inhibitors with potential to benefit wet AMD patients. These compounds, when dosed orally, provided good efficacy and preferential ocular tissue distribution while minimizing systemic exposure.

Item Type: Article
Date Deposited: 28 Apr 2016 23:45
Last Modified: 28 Apr 2016 23:45
URI: https://oak.novartis.com/id/eprint/21148

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