当前位置： SCI文献检索 > JOURNAL OF MEDICINAL CHEMISTRY期刊下所有文献 > The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-

The Discovery of N-(1-Methyl-5-(trifluoromethyl)-1H-pyrazol-3-yl)-5-((6- ((methylamino)methyl)pyrimidin-4-yl)oxy)-1H-indole-1-carboxamide (Acrizanib), a VEGFR-2 Inhibitor Specifically Designed for Topical Ocular Delivery, as a Therapy for Neovascular Age-

Abstract：

:A noninvasive topical ocular therapy for the treatment of neovascular or "wet" age-related macular degeneration would provide a patient administered alternative to the current standard of care, which requires physician administered intravitreal injections. This manuscript describes a novel strategy for the use of in vivo models of choroidal neovascularization (CNV) as the primary means of developing SAR related to efficacy from topical administration. Ultimately, this effort led to the discovery of acrizanib (LHA510), a small-molecule VEGFR-2 inhibitor with potency and efficacy in rodent CNV models, limited systemic exposure after topical ocular administration, multiple formulation options, and an acceptable rabbit ocular PK profile.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Adams CM,Anderson K,Artman G 3rd,Bizec JC,Cepeda R,Elliott J,Fassbender E,Ghosh M,Hanks S,Hardegger LA,Hosagrahara VP,Jaffee B,Jendza K,Ji N,Johnson L,Lee W,Liu D,Liu F,Long D,Ma F,Mainolfi N,Meredith EL,Miran

doi

10.1021/acs.jmedchem.7b01731

subject

Has Abstract

pub_date

2018-02-22 00:00:00

pages

1622-1635

issue

4

eissn

0022-2623

issn

1520-4804

journal_volume

61

pub_type

杂志文章

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