METHODS AND COMPOSITIONS FOR PREVENTING OR TREATING OPHTHALMIC CONDITIONS

• US 20110177047A1
• Filed: 08/23/2010
• Published: 07/21/2011
• Est. Priority Date: 08/24/2009
• Status: Active Grant

• Current Assignee: Stealth BioTherapeutics, Inc. (Morningside Group Ltd.)
• Original Assignee: Stealth Peptides International Inc
• Inventors: Liang, Xiaoling, Tang, Shibo, Liu, Liping
• Granted Patent: US 8,470,784 B2
• Time in Patent Office: Days
• US Class Current: 424/94.1
• CPC Class Codes: A61K 38/06 Tripeptides
• CPC Class Codes: A61K 38/07 Tetrapeptides
• CPC Class Codes: A61K 45/06 Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/12 for cataracts
• CPC Class Codes: C07K 5/0817 the first amino acid being Arg
• CPC Class Codes: C07K 5/1016 and aromatic or cycloaliphatic

Abstract

The disclosure generally describes methods of preventing or treating ophthalmic diseases or conditions in a mammalian subject, such as diabetic retinopathy, cataracts, retinitis pigmentosa, glaucoma, macular degeneration, choroidal neovascularization, retinal degeneration, and oxygen-induced retinopathy. The methods comprise administering an effective amount of an aromatic-cationic peptide to subjects in need thereof.

Claims

1. A method for treating or preventing an ophthalmic condition in a mammlian subject in need thereof, comprising administering to the subject a therapeutically effective amount of a peptide represented by the formula D-Arg-2′

6′

-Dmt-Lys-Phe-NH₂ or Phe-D-Arg-Phe-Lys-NH₂.

2. The method of claim 1, wherein the ophthalmic condition is selected from the group consisting of:

diabetic retinopathy, cataracts, retinitis pigmentosa, glaucoma, macular degeneration, choroidal neovascularization, retinal degeneration, and oxygen-induced retinopathy.

3. The method of claim 1, wherein the peptide is D-Arg-2′

6′

-Dmt-Lys-Phe-NH₂.

4. The method of claim 1, wherein the peptide is Phe-D-Arg-Phe-Lys-NH₂.

5. The method of claim 1, wherein the subject is a human.

6. The method of claim 1, wherein the peptide is administered intraocularly, iontophoretically, orally, topically, systemically, intravenously, subcutaneously, or intramuscularly.

7. The method of claim 1 further comprising separately, sequentially, or simultaneously administering a second active agent.

8. The method of claim 7, wherein the second active agent is selected from the group consisting of:

an antioxidant, a metal complexer, an anti-inflammatory drug, an antibiotic, and an antihistamine.

9. The method of claim 8, wherein the antioxidant is vitamin A, vitamin C, vitamin E, lycopene, selenium, α

-lipoic acid, coenzyme Q, glutathione, or a carotenoid.

10. The method of claim 7, wherein the second active agent is selected from the group consisting of:

aceclidine, acetazolamide, anecortave, apraclonidine, atropine, azapentacene, azelastine, bacitracin, befunolol, betamethasone, betaxolol, bimatoprost, brimonidine, brinzolamide, carbachol, carteolol, celecoxib, chloramphenicol, chlortetracycline, ciprofloxacin, cromoglycate, cromolyn, cyclopentolate, cyclosporin, dapiprazole, demecarium, dexamethasone, diclofenac, dichlorphenamide, dipivefrin, dorzolamide, echothiophate, emedastine, epinastine, epinephrine, erythromycin, ethoxzolamide, eucatropine, fludrocortisone, fluorometholone, flurbiprofen, fomivirsen, framycetin, ganciclovir, gatifloxacin, gentamycin, homatropine, hydrocortisone, idoxuridine, indomethacin, isofluorophate, ketorolac, ketotifen, latanoprost, levobetaxolol, levobunolol, levocabastine, levofloxacin, lodoxamide, loteprednol, medrysone, methazolamide, metipranolol, moxifloxacin, naphazoline, natamycin, nedocromil, neomycin, norfloxacin, ofloxacin, olopatadine, oxymetazoline, pemirolast, pegaptanib, phenylephrine, physostigmine, pilocarpine, pindolol, pirenoxine, polymyxin B, prednisolone, proparacaine, ranibizumab, rimexolone, scopolamine, sezolamide, squalamine, sulfacetamide, suprofen, tetracaine, tetracyclin, tetrahydrozoline, tetryzoline, timolol, tobramycin, travoprost, triamcinulone, trifluoromethazolamide, trifluridine, trimethoprim, tropicamide, unoprostone, vidarbine, xylometazoline, pharmaceutically acceptable salts thereof, and combinations thereof.