# US 11,078,262 B2 · High viscosity macromolecular compositions for treating ocular conditions > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,078,262 B2 - Document ID: US11078262B2 - Status: Granted - Kind: B2 - Application number: 11/742,350 - Filed: 2007-04-30 - Published: 2008-10-30 - Granted: 2021-08-03 - Earliest claimed: 2007-04-30 - Assignees: Allergan, Inc. - Applicants: Patrick M. Hughes; Gerald W. DeVries; Robert T. Lyons; John T. Trogden; Scott M. Whitcup - Inventors: Patrick M. Hughes; Gerald W. DeVries; Robert T. Lyons; John T. Trogden; Scott M. Whitcup - Web page: https://patentgrep.com/patent/US11078262B2 ## CPC - C07K 16/22: against growth factors {; against growth regulators} - A61K 9/0048: {Eye, e.g. artificial tears} - A61K 9/08: Solutions {(composition of solutions A61K47/00)} - A61K 38/39: Connective tissue peptides, e.g. collagen, elastin, laminin, fibronectin, vitronectin, cold insoluble globulin [CIG] - A61K 47/34: Macromolecular compounds obtained otherwise than by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyesters, polyamino acids, polysiloxanes, polyphosphazines, copolymers of polyalkylene glycol or poloxamers (A61K47/10 takes precedence) - A61P 9/00: Drugs for disorders of the cardiovascular system - A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis - A61P 27/02: Ophthalmic agents - A61P 35/00: Antineoplastic agents - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - C12N 15/1138: {against receptors or cell surface proteins} - A61K 2039/505: {comprising antibodies} - C07K 2317/24: containing regions, domains or residues from different species, e.g. chimeric, humanized or veneered - C12N 2310/14: interfering nucleic acids [NA] - C12N 2310/315: Phosphorothioates - C12N 2310/317: with an inverted bond, e.g. a cap structure - C12N 2310/332: Abasic residue - C12N 2320/32: Special delivery means, e.g. tissue-specific - C07K: PEPTIDES (peptides in foodstuffs A23; obtaining protein compositions for foodstuffs, working-up proteins for foodstuffs A23J; preparations for medicinal purposes A61K; peptides containing beta-lactam rings C07D; cyclic dipeptides not having in their molecule any other peptide link than those which form their ring, e.g. piperazine-2,5-diones, C07D; ergot alkaloids of the cyclic peptide type C07D519/02; macromolecular compounds having statistically distributed amino acid units in their molecules, i.e. when the preparation does not provide for a specific; but for a random sequence of the amino acid units, homopolyamides and block copolyamides derived from amino acids C08G69/00; macromolecular products derived from proteins C08H1/00; preparation of glue or gelatine C09H; single cell proteins, enzymes C12N; genetic engineering processes for obtaining peptides C12N15/00; compositions for measuring or testing processes involving enzymes C12Q; investigation or analysis of biological material G01N33/00) - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C12N: MICROORGANISMS OR ENZYMES; COMPOSITIONS THEREOF; PROPAGATING, PRESERVING, OR MAINTAINING MICROORGANISMS; MUTATION OR GENETIC ENGINEERING; CULTURE MEDIA (microbiological testing media C12Q1/00) ## Abstract Anti-angiogenesis compositions, and methods of using such compositions, useful for injection into the vitreous of human eyes are provided. Such compositions include MAAC solutions or particles present in a therapeutically effective amount, a viscosity-inducing component, and an aqueous carrier component. The compositions have viscosities at about 25° C. of at least about 10 cps or about 100 cps at a shear rate of 0.1/second. In a preferred embodiment, the viscosity at 25° C. is in the range of from about 80,000 cps to about 300,000 cps. ## Claims ### Claim 1 A method for treating a posterior ocular condition, the method comprising: administering into the vitreous of an eye of a mammal suffering from an ocular condition a composition consisting of; a therapeutically effective amount of a macromolecular anti-angiogenic component (MAAC), wherein the MAAC is selected from a VEGF antibody comprising bevacizumab, a VEGF antibody fragment comprising ranibizumab, a VEGF antibody mimic comprising CT-322, C7S100, or C7C100, and combinations thereof; a viscosity inducing component in an amount effective to increase the viscosity of the composition to a viscosity at about 25° C. of at least 10 cps at a shear rate of about 0.1/second, wherein said viscosity inducing component is injectable into the vitreous of a mammalian eye without permanently diminishing visual acuity, sodium chloride, dibasic sodium phosphate heptahydrate, monobasic sodium phosphate monohydrate, and water; wherein the posterior ocular condition is selected from macular edema, macular degeneration, diabetic retinopathy, and combinations thereof; and wherein the administering is by subconjunctival, suprachoroidal, intravitreal or combination thereof. ### Claim 2 (depends on 1) The method of claim 1 wherein said viscosity inducing component comprises a compound having a molecular weight in the range from about 10,000 Daltons to about 2 million Daltons. ### Claim 3 (depends on 1) The method of claim 1 wherein said viscosity inducing component comprises a compound having a molecular weight in the range of about 100,000 Daltons to about 1.5 million Daltons. ### Claim 4 (depends on 1) The method of claim 1 wherein said viscosity inducing component comprises a compound having a molecular weight in the range of about 200,000 Daltons to about 1 million Daltons. ### Claim 5 (depends on 1) The method of claim 1 wherein said viscosity inducing component has a viscosity of at least 100 cps at a shear rate of 0.1/second at 25° C. ### Claim 6 (depends on 1) The method of claim 1 wherein said viscosity inducing component has a viscosity of at least 1000 cps at a shear rate of 0.1/second at 25° C. ### Claim 7 (depends on 1) The method of claim 1 wherein said viscosity inducing component has a viscosity of at least 10,000 cps at a shear rate of 0.1/second at 25° C. ### Claim 8 (depends on 1) The method of claim 1 wherein said viscosity inducing component has a viscosity of at least 70,000 cps at a shear rate of 0.1/second at 25° C. ### Claim 9 (depends on 1) The method of claim 1 wherein said viscosity inducing component has a viscosity of at least 200,000 cps at a shear rate of 0.1/second at 25° C. ### Claim 10 (depends on 1) The method of claim 1 wherein said viscosity inducing component has a viscosity of at least 250,000 cps at a shear rate of 0.1/second at 25° C. ### Claim 11 (depends on 1) The method of claim 1 wherein said viscosity inducing component has a viscosity of at least 300,000 cps at a shear rate of 0.1/second at 25° C. ### Claim 12 (depends on 1) The method of claim 1 wherein said composition is administered to the vitreous of said eye by placement into the vitreous of the eye through a 27-gauge needle. ### Claim 13 (depends on 1) The method of claim 1 wherein said composition is administered to the vitreous of said eye by placement into the vitreous of the eye through a 30-gauge needle. ### Claim 14 A method for treating a posterior ocular condition, the method comprising: administering into the vitreous of an eye of a mammal suffering from an ocular condition a composition consisting of; a therapeutically effective amount of a MAAC selected from one or more of: a VEGF TRAP; icrucumab, ramucirumab, endostatin, angiostatin, tumstatin, and pigment epithelium derived factor, a viscosity inducing component in an amount effective to increase the viscosity of the composition to a viscosity at about 25° C. of at least 10 cps at a shear rate of about 0.1/second, wherein said viscosity inducing component is injectable into the vitreous of a mammalian eye without permanently diminishing visual acuity, sodium chloride, dibasic sodium phosphate heptahydrate, monobasic sodium phosphate monohydrate, and water; wherein the posterior ocular condition is selected from macular edema, macular degeneration, diabetic retinopathy, and combinations thereof; and wherein the administering is by subconjunctival, suprachoroidal, intravitreal or combination thereof.