Use of Carboxyamidotriazole (CAI) orotate in macular degeneration
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Publication Number
US-8420658-B2
Publication Date
2013-04-16
Expiration Date
Abstract
Method and composition of Carboxyamidotriazole orotate for treating age-related macular degeneration and other angiogenesis-dependent diseases.
Core Innovation
Carboxyamidotriazole (CAI) or 5-amino-1,2,3-triazole orotate (CAI orotate) is described as an angiogenesis inhibitor. The disclosure relates to treating age-related macular degeneration, including neovascular disease, using CAI orotate-containing compositions. The invention is positioned as providing anti-angiogenic activity by inhibiting angiogenesis-related pathological processes.
The background describes ocular pathology mediated by angiogenesis and the associated need for inhibiting neovascular disease. It presents age-related macular degeneration and other angiogenesis-dependent conditions as settings where angiogenesis inhibition is desirable. CAI orotate is presented as addressing this problem by targeting angiogenesis related conditions.
The summary reports in vitro inhibition of endothelial cell proliferation (human umbilical vein endothelial cells, HUVEC) in a dose-related manner. This endothelial proliferation inhibition is provided as supporting evidence for anti-angiogenic activity. The document also situates the therapeutic use within angiogenesis dependent diseases beyond the ocular setting, as listed in the claim.
Claims Coverage
The document provides one independent claim, which contains multiple inventive features centered on oral administration of 5-amino-1,2,3-carboxyamidotriazole orotate to treat a defined set of angiogenesis related conditions.
Oral administration of 5-amino-1,2,3-carboxyamidotriazole orotate for angiogenesis inhibition
Administering orally an amount of 5 amino 1, 2, 3-carboxyamidotriazole orotate effective to inhibit an angiogenesis related condition in an individual in need thereof.
Treatment restricted to a defined list of angiogenesis related conditions
Wherein the angiogenesis related condition consists of diabetic retinopathy, retinopathy of prematurity, corneal graft rejection, neovascular glaucoma, retrolental fibroplasias, rubeosis, myocardial angiogenesis, plaque neovascularization, telangiectasia, angiofibroma, and wound granulation.
The independent claim is directed to a method of treating an individual with an angiogenesis related condition by orally administering an effective amount of 5-amino-1,2,3-carboxyamidotriazole orotate, with the target condition limited to the listed set that includes multiple ophthalmic neovascular conditions and additional angiogenesis conditions.
Stated Advantages
Inhibits angiogenesis related conditions.
Provides anti-angiogenic activity supported by dose-related inhibition of endothelial cell proliferation (HUVEC).
Documented Applications
Treating age-related macular degeneration, including neovascular disease.
Treating angiogenesis related conditions including diabetic retinopathy.
Treating angiogenesis related conditions including retinopathy of prematurity.
Treating angiogenesis related conditions including corneal graft rejection.
Treating angiogenesis related conditions including neovascular glaucoma.
Treating angiogenesis related conditions including retrolental fibroplasias.
Treating angiogenesis related conditions including rubeosis.
Treating angiogenesis related conditions including myocardial angiogenesis.
Treating angiogenesis related conditions including plaque neovascularization.
Treating angiogenesis related conditions including telangiectasia.
Treating angiogenesis related conditions including angiofibroma.
Treating angiogenesis related conditions including wound granulation.
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