Method for treating eye disease or conditions affecting the posterior segment of the eye

Abstract

This invention relates to the use of prodrug for the manufacture of a medicament useful for treating an ocular disease affecting the posterior segment of the eye, in a subject in need thereof, wherein the prodrug is a composition injected into the vitreous body, and the frequency of injections does not exceed one injection per month.

1 . A method for treating an ocular disease affecting the posterior segment of the eye, in a subject in need thereof, comprising administering to said subject an effective amount of prodrug wherein the prodrug is a composition injected into the vitreous body, and the frequency of injections does not exceed one injection per month. 
     
     
         2 . The method according to  claim 1 , wherein two months after one injection of said prodrug; the drug cannot be detected in the vitreous or the molar ratio of the prodrug to the drug, in the vitreous, is more than 60. 
     
     
         3 . The method according to  claim 1 , wherein the molar ratio of the prodrug to the drug, in the retina, two months after one injection of said prodrug, is less than 60. 
     
     
         4 . The method according to  claim 1 , wherein the molar ratio of the prodrug to the drug, in the choroid, two months after one injection of said prodrug, is less than 60. 
     
     
         5 . The method according to  claim 1 , wherein the prodrug is injected in the vitreous in an amount enabling the sustained release of a therapeutically amount of said drug for a duration of at least one month, preferably at least 2 months, more preferably at least 6 months. 
     
     
         6 . The method according to  claim 1 , wherein the prodrug is injected at most once every two months, more preferably at most once every six months. 
     
     
         7 . The method according to  claim 1 , wherein the half-life of the prodrug is of at least 15 days. 
     
     
         8 . The method according to  claim 1 , wherein the prodrug is dexamethasone palmitate. 
     
     
         9 . The method according to  claim 1 , wherein the prodrug is in combination with any suitable excipient or carrier suitable for ophthalmic use. 
     
     
         10 . The method according to  claim 1  wherein the prodrug is within an oily carrier. 
     
     
         11 . The method according to  claim 1  wherein the prodrug is within an emulsion. 
     
     
         12 . The method according to  claim 1 , wherein the prodrug releases at least one drug selected in the group comprising antivirals, chosen from the group comprising idoxuridine, trifluorothymidine, trifluorouridine, acyclovir, ganciclovir, cidofovir, interferon, DDI, AZT, foscamet, vidarabine, irbavirin; non-steroidal anti-inflammatories chosen from the group comprising amfenac, ketorolac, indomethacin, ibuprofen, diclofenac, flurbiprofen, piroxicam and other COX2 inhibitors; cytokines, interleukines and growth factors epidermal growth factor, fibroblast growth factor, pigment epithelium growth factor, platelet derived growth factor, transforming growth factor beta, ciliary neurotrophic growth factor, glial derived neurotrophic factor, NGF, EPO, PLGF, brain nerve growth factor (BNGF), vascular endothelial growth factor (VEGF) and monoclonal antibodies or proteins inhibiting the activity of such cytokines and growth factors; anti-inflammatories chosen from the group comprising alclometasone dipropionate, amcinonide, amcinafel, amcinafide, beclamethasone, betamethasone, betamethasone dipropionate, betamethasone valerate, clobetasone propionate, chloroprednisone, clocortelone, Cortisol, cortisone, cortodoxone, difluorosone diacetate, descinolone, desonide, defluprednate, dihydroxycortisone, desoximetasone, dexamethasone, deflazacort, diflorasone, diflorasone diacetate, dichlorisone, esters of betamethasone, fluazacort, flucetonide, flucloronide, fludrotisone, fluorocortisone, flumethasone, flunisolide, fluocinonide, fluocinolone, fluocinolone acetonide, flucortolone, fluperolone, fluprednisolone, fluroandrenolone acetonide, fluocinolone acetonide, flurandrenolide, fluorametholone, fluticasone propionate, hydrocortisone, hydrocortisone butyrate, hydrocortisone valerate, hydrocortamate, loteprendol, medrysone, meprednisone, methylprednisone, methylprednisolone, mometasone furoate, paramethasone, paramethasone acetate, prednisone, prednisolone, prednidone, triamcinolone acetonide, triamcinolone hexacatonide, and triamcinolone, salts, derivatives, and a mixture thereof; antiangiogenic compounds such as anecortave, combretastatin, vascular endothelial growth factor (VEGF) inhibitors, squalamine, AdPEDF, VEGF-traps; immunological response modifiers chosen from the group comprising muramyl dipeptide, cyclosporins, interferons, interleukin-2, cytokines, tacrolimus, tumor necrosis factor, pentostatin, thymopentin, transforming factor beta.sub.2, erythropoetin; antineogenesis proteins; antibodies (monoclonal or polyclonal) or antibodies fragments, oligoaptamers, aptamers and gene fragments such as oligonucleotides, plasmids, ribozymes, small interference RNA, (nucleic acid fragments, peptides. 
     
     
         13 . The method according to  claim 1 , wherein the treatment or prevention of a disorder affecting the posterior segment of the eye,comprises the treatment of any disease, ailment or condition which primarily affects or involves a posterior ocular site such as choroid or sclera, vitreous, vitreous chamber, retina, optic nerve, and blood vessels and nerves which vascularize or innervate a posterior ocular site. 
     
     
         14 . The method according to any one of  claim 1 , wherein the disorder is one or more of the following: Macular Disorders such as myopia, Non-Exudative Age Related Macular Degeneration, Exudative Age Related Macular Degeneration, Choroidal Neovascular Membranes and Cystoid Macular Edema; Inflammatory Disorders such as Uveitic Retinal Disease, Endophthalmitis, Toxoplasmic Retinochoroiditis, Systemic General Disorders Associated with Retinal Uveitis or Retinochoroidal Syndromes (Syphilis, Tuberculosis, Lyme Diseases, Chung Strauss Disease, LED, etc), Neuroretinitis, Optic Neuritis; Vascular Disorders such as Diabetic Retinopathy, Diabetic Macular Edema, Arterial Occlusion, Venous Occlusion; Heredo Retinal Dystrophies such as Stargardt's Disease, Fundus Flavimaculatus, other Heredomacular Dysropy; Trauma caused by Laser, photodynamic therapy, Photocoagulation, Hypoperfusion During Surgery; Macular Hole; Retinal Disease Associated with Tumors, Posterior Uveal Melanoma, Retinoblastoma and Choroidal Metastasis. 
     
     
         15 . A method to extend the duration of a treatment of a disease or a condition of the posterior segment of an eye, in a subject in need thereof, comprising administering to said subject an effective amount of a prodrug wherein said prodrug is injected into the vitreous body at most one a month.