FORMULATIONS FOR TREATING OCULAR DISEASES AND CONDITIONS
First Claim
1. A method of treating macular edema in a human subject by repeated administration of rapamycin, the method comprising:
- administering two or more doses of a rapamycin formulation to an eye of the human subject, wherein the period between consecutive doses is at least 8 weeks, and the cumulative amount of rapamycin in the two or more doses is effective to treat macular edema in the human subject for an extended period of at least 16 weeks.
2 Assignments
0 Petitions
Accused Products
Abstract
Diseases and conditions associated with tissues of the body, including but not limited to tissues in the eye, can be effectively treated, prevented, inhibited, onset delayed, or regression caused by administering therapeutic agents to those tissues. Described herein are liquid formulations which deliver a variety of therapeutic agents, including but not limited to rapamycin, to a subject for an extended period of time; liquid formulations which form a non-dispersed mass when placed in an aqueous medium of a subject; non-dispersed mass-forming liquid formulations which form a gel or gel-like substance in an aqueous medium; liquid formulations, comprising a therapeutic agent and a plurality of polymers; and methods for delivering therapeutic agents to a subject for an extended period of time using the liquid formulations. The liquid formulation may be placed in an aqueous medium of a subject, including but not limited to via intraocular or periocular administration, or placement proximate to a site of a disease or condition to be treated in a subject. A method may be used to administer rapamycin to treat or prevent angiogenesis, choroidal neovascularization, or age-related macular degeneration, or wet age-related macular degeneration in a subject. The liquid formulations may comprise rapamycin or other therapeutic agents.
172 Citations
96 Claims
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1. A method of treating macular edema in a human subject by repeated administration of rapamycin, the method comprising:
administering two or more doses of a rapamycin formulation to an eye of the human subject, wherein the period between consecutive doses is at least 8 weeks, and the cumulative amount of rapamycin in the two or more doses is effective to treat macular edema in the human subject for an extended period of at least 16 weeks. - View Dependent Claims (2, 3, 4, 5, 6, 7)
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8. A method of treating diabetic macular edema in a human subject by repeated administration of rapamycin, the method comprising:
administering two or more doses of a rapamycin formulation to an eye of the human subject, wherein the rapamycin formulation is a solution comprising rapamycin and polyethylene glycol, the rapamycin formulation is administered by placement of each dose between a sclera and a conjunctiva of the eye of the subject, the period between consecutive doses is at least 8 weeks, and wherein the cumulative amount of rapamycin in the two or more doses is effective to treat diabetic macular edema in the human subject for an extended period of at least 16 weeks. - View Dependent Claims (9, 10, 11, 12, 13, 14, 15, 16, 17, 18)
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19-54. -54. (canceled)
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55. A method of administering by a periocular route a liquid formulation to an eye of a subject without causing chemosis of the eye, comprising:
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administering less than 40 μ
l of the liquid formulation between a sclera and a conjunctiva of the eye of the subject,wherein the liquid formulation comprises a therapeutic agent and a solvent, and wherein the liquid formulation has a hygroscopicity that is 80% or greater than the hygroscopicity of a liquid formulation consisting essentially of about 2% (w/w) rapamycin, about 4% (w/w) ethanol, and about 94% (w/w) polyethylene glycol 400 (PEG
400). - View Dependent Claims (56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66)
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67-87. -87. (canceled)
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88. A method for treating wet age-related macular degeneration or diabetic macular edema in a human subject, the method comprising:
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(a) administering to the human subject a volume of a first formulation by intravitreal placement, wherein the volume of the first formulation comprises an amount of ranibizumab or bevacizumab; and (b) administering to the human subject a volume of a second formulation by subconjunctival placement, wherein the volume of the second formulation comprises an amount of rapamycin, or a pharmaceutically acceptable salt or ester thereof; wherein the amount of ranibizumab or bevacizumab and the amount of rapamycin or a pharmaceutically acceptable salt or ester thereof, together are effective to treat wet age-related macular degeneration or diabetic macular edema when administered to the human subject. - View Dependent Claims (89, 90, 91, 92, 94, 95)
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93. The method of 88, wherein the second formulation consists essentially of about 2% (w/w) rapamycin, about 4% (w/w) ethanol, and about 94% (w/w) polyethylene glycol 400 (PEG 400).
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96-125. -125. (canceled)
Specification