METHODS FOR TREATING EYE ANGIOGENESIS, RETINAL Edema, RETINAL ISCHEMIA AND DIABETIC RETINOPATHY USING RTK SELECTIVE INHIBITORS

摘要

1. A method of inhibiting neovascularization of the eye, inhibiting retinal edema or providing regression of neovascularization, wherein said method comprises administering to a patient in need thereof a composition comprising a therapeutically effective amount of a receptor tyrosine kinase inhibitor that blocks tyrosine autophosphorylation of VEGF receptor 2 with an IC50 of ≤ 10 nM and one or more receptors selected from the group consisting of VEGF receptor 1, VEGF receptor 3, Tie-2, PDGFR, c-KIT, Flt-3 and CSF-IR, where the receptor tyrosine kinase inhibitor has an IC50 of 0.1 nM to 200 nM for each of these additional receptors for which tyrosine autophosphorylation is blocked. ! 2. The method according to claim 1, wherein the tyrosine receptor tyrosine inhibitor blocks VEGF receptor 2, VEGF receptor 1, PDGFR and Tie-2 tyrosine autophosphorylation, and where the tyrosine kinase inhibitor has an IC50 of 0.1 nM to 100 nM for VEGF receptor 1 and PDGFR 1 and an IC50 of 0.1 nM to 200 nM for Tie-2. ! 3. The method according to claim 1, wherein the tyrosine receptor tyrosine inhibitor blocks tyrosine autophosphorylation of VEGF receptor 2, VEGF receptor 1 and Tie-2, and where the tyrosine kinase inhibitor has an IC50 of 0.1 nM to 200 nM for Tie-2 and IC50 ≤ 10 nM for VEGF receptor 1. ! 4. The method according to claim 1, wherein the tyrosine receptor tyrosine inhibitor inhibits VEGF receptor 2, VEGF receptor 1 and PDGFR tyrosine autophosphorylation, and wherein the receptor tyrosine kinase inhibitor has an IC50 of 0.1 nM to 100 nM for VEGF receptor 1 and PDGFR. ! 5. The method according to claim 1, wherein the tyrosine kinase inhibitor inhibits tyrosine autophosphorylation of VEGF and Tie-2 receptor 2, and wherein the tyrosine kinase receptor inhibitor has an IC50 of 0.1 nM to 200 nM for Tie-2. ! 6. The method according to claim 1, where the inhibitor is receptor