COMPOSITIONS, FORMULATIONS AND METHODS FOR TREATING OCULAR DISEASES
Disclosed herein are compounds effective for activation of Tie-2 and inhibition of HPTP-beta. The compounds can provide effective therapy for conditions associated with angiogenesis, for example, ocular conditions. Formulations for increased solubility are disclosed. Combination therapy with antibodies and PK/PD data are also disclosed.
1 - 54 . (canceled)
55 . A method of treating an ocular edema in an eye of a subject in need thereof, the method comprising intravitreally administering to the subject a pharmaceutical formulation, wherein the pharmaceutical formulation comprises a therapeutically-effective amount of a Tie-2 activator,
wherein the Tie-2 activator activates Tie-2 in the eye of the subject,
wherein the therapeutically-effective amount of the Tie-2 activator is from about 1 mg to about 10 mg;
wherein after administration of the pharmaceutical formulation to the subject, a visual acuity of the subject increases;
wherein the pharmaceutical formulation further comprises a solubilizing agent; and
wherein the method further comprises inhibiting VEGF in the eye of the subject.
56 . The method of claim 55 , wherein the therapeutically-effective amount of the Tie-2 activator is about 1.5 mg.
57 . The method of claim 55 , wherein the therapeutically-effective amount of the Tie-2 activator is about 6 mg.
58 . The method of claim 55 , wherein the solubilizing agent is a polysorbate.
59 . The method of claim 55 , wherein the ocular edema is diabetic macular edema.
60 . The method of claim 55 , wherein a plasma concentration of the Tie-2 activator is not less than about 1 ng/mL about 2 hours after the administration of the pharmaceutical formulation.
61 . A method of activating Tie-2 in an eye of a subject in need thereof, the method comprising intravitreally administering to the subject a pharmaceutical formulation, wherein the pharmaceutical formulation comprises a therapeutically-effective amount of a Tie-2 activator,
wherein the subject has an ocular edema;
wherein the therapeutically-effective amount of the Tie-2 activator is from about 1 mg to about 10 mg;
wherein after administration of the pharmaceutical formulation to the subject, a visual acuity of the subject increases;
wherein the pharmaceutical formulation further comprises a solubilizing agent; and
wherein the method further comprises inhibiting VEGF in the eye of the subject.
62 . The method of claim 61 , wherein the therapeutically-effective amount of the Tie-2 activator is about 1.5 mg.
63 . The method of claim 61 , wherein the therapeutically-effective amount of the Tie-2 activator is about 6 mg.
64 . The method of claim 61 , wherein the solubilizing agent is a polysorbate.
65 . The method of claim 61 , wherein the ocular edema is diabetic macular edema.
66 . The method of claim 61 , wherein a plasma concentration of the Tie-2 activator is not less than about 1 ng/mL about 2 hours after the administration of the pharmaceutical formulation.