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US 2006/0233859 A1 Whitcup Et Al US 20060233859A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2006/0233859 A1 Whitcup et al. (43) Pub. Date: Oct. 19, 2006 (54) METHODS FOR TREATING RETINOPATHY Related U.S. Application Data WITH EXTENDED THERAPEUTIC EFFECT (63) Continuation-in-part of application No. 10/837,357, (75) Inventors: Scott M. Whitcup, Laguna Hills, CA filed on Apr. 30, 2004. (US); David A. Weber, Danville, CA (US) Publication Classification Correspondence Address: (51) Int. Cl. ALLERGAN, INC., LEGAL DEPARTMENT A 6LX 3/573 (2006.01) 2525 DUPONT DRIVE, T2-7H A6F 2/00 (2006.01) IRVINE, CA 92.612-1599 (US) (52) U.S. Cl. ............................................ 424/427: 514/179 (73) Assignee: Allergan, Inc., Irvine, CA (57) ABSTRACT (21) Appl. No.: 11/292,544 Methods for treating and preventing retinopathic conditions by administering a glucocorticoid to the vitreous chamber of (22) Filed: Dec. 2, 2005 a patient at risk of, or Suffering from, the retinopathy. Patent Application Publication Oct. 19, 2006 Sheet 1 of 3 US 2006/0233859 A1 FIGURE 1 Vitreous Humor Concentrations of Dexamethasone in Treated Eye: Comparison of all Dose Levels and Dosage Forms 10000 an(0am-350T OOO - an a 700T 5 100 XC - - - Quantification Limit 0.35OE 10 - a 700E Hours FIGURE 2 Percent of Dexamethasone Released from DEXPS DDS over Time for all Dose Levels and Dosage Forms 60 50 40 - : 30 4 S. 20 10 O Hours Patent Application Publication Oct. 19, 2006 Sheet 2 of 3 US 2006/0233859 A1 FIGURE 3 Vitreous Humor Concentrations of Dexamethasone in Treated Eye: Comparison of all Dose Levels and Dosage Forms - - - Quantification Limit sm 700E Days FIGURE 4 Percent of Dexamethasone Released from DEX PS DDS Over Time for all Dose Levels and Dosage Forms Days Patent Application Publication Oct. 19, 2006 Sheet 3 of 3 US 2006/0233859 A1 10 N 20 28 34 t 38 / \)W T 42 44 FIG. 5 US 2006/0233859 A1 Oct. 19, 2006 METHODS FOR TREATING RETINOPATHY WITH 0005. An anterior ocular condition can include a disease, EXTENDED THERAPEUTIC EFFECT ailment or condition, Such as for example, aphakia; pseudophakia; astigmatism; blepharospasm; cataract; con CROSS REFERENCE junctival diseases; conjunctivitis; corneal diseases; corneal 0001. The present application is a continuation in part of ulcer, dry eye syndromes; eyelid diseases; lacrimal appara U.S. patent application Ser. No. 10/837,357, filed Apr. 30, tus diseases; lacrimal duct obstruction; myopia; presbyopia; 2004, the entire content of which is expressly incorporated hyperopia; pupil disorders; refractive disorders and Strabis by reference herein. mus. Glaucoma can also be considered to be an anterior ocular condition because a clinical goal of glaucoma treat BACKGROUND ment can be to reduce a hypertension of aqueous fluid in the 0002 This invention relates to methods for extended anterior chamber of the eye (i.e. reduce intraocular pres treatment of an ocular condition. In particular the present Sure). invention releases to methods for extended treatment of an 0006 The present invention is directed to a method for ocular condition with an intraocular implant. providing an extended treatment of an ocular condition, Such 0003. An ocular condition can include an inflammatory, as an anterior ocular condition or a posterior ocular condi neoplastic, infectious, vascular, neovascular and/or degen tion or to an ocular condition which can be characterized as erative disease, aliment or condition which affects or both an anterior ocular condition and a posterior ocular involves the eye or one of the parts or regions of the eye. condition. Broadly speaking the eye includes the eyeball and the tissues 0007. Therapeutic compounds useful for the treatment of and fluids which constitute the eyeball, the periocular an ocular condition can include cytokines and active agents muscles (such as the oblique and rectus muscles) and the with, for example, an anti-neoplastic (i.e. anti-cancer), anti portion of the optic nerve which is within or adjacent to the angiogenesis, kinase inhibition, anticholinergic, anti-adren eyeball. An anterior ocular condition is a disease, ailment or ergic and/or anti-inflammatory activity. condition which affects or which involves an anterior (i.e. front of the eye) ocular region, location or site (hereafter an 0008 Macular degeneration, such as age related macular ocular site). Such as a periocular muscle, an eyelid or an eye degeneration (AMD) is a leading cause of irreversible ball tissue or fluid which is located anterior to the posterior vision loss in elderly populations. It is estimated that thirteen wall of the lens capsule or ciliary muscles. Thus, an anterior million Americans have evidence of macular degeneration. ocular condition primarily affects or involves, the conjunc Macular degeneration results in a break down or injury to the tiva, the cornea, the anterior chamber, the iris, the posterior macula, the central part of the retina responsible for the chamber (behind the iris but in front of the posterior wall of sharp, direct vision needed to read or drive. Central vision is the lens capsule), the lens or the lens capsule and blood especially or selectively affected. Macular degeneration is vessels and nerve which vascularize or innervate an anterior diagnosed as either dry or wet (exudative). The dry form of ocular region or site. A posterior ocular condition is a macular degeneration is more common than the wet form of disease, ailment or condition which primarily affects or macular degeneration, with about 90% of AMD patients involves a posterior ocular site such as choroid or Sclera (in being diagnosed with dry AMD. The wet form of the disease a position posterior to a plane through the posterior wall of usually leads to more rapid and more serious vision loss. the lens capsule), vitreous, vitreous chamber, retina, optic Macular degeneration can produce a slow or Sudden painless nerve (including the optic disc), and blood vessels and loss of vision. The cause of macular degeneration is not nerves which vascularize or innervate a posterior ocular site. clear. The dry form of AMD may result in thinning of macular tissues, depositing of pigment in the macula, or a 0004 Thus, a posterior ocular condition can include a combination of the two processes. With wet AMD, new disease, ailment or condition, such as for example, macular blood vessels grow within and beneath the retina and leak degeneration (such as non-exudative age related macular blood and fluid. This leakage causes injury to retinal cells degeneration and exudative age related macular degenera and creates blind spots in central vision. tion); macular hole; light, radiation or thermal damage to a posterior ocular tissue; choroidal neovascularization; acute 0009 Macular edema (ME) can result in a swelling or macular neuroretinopathy; macular edema (such as cystoid thickening of the macular and appears to be a nonspecific macular edema and diabetic macular edema); Behcet’s dis response of the retina to a variety of insults. Thus, ME is ease, retinal disorders, diabetic retinopathy (including pro associated with a number of diseases, including anterior or liferative diabetic retinopathy); retinal arterial occlusive posterior uveitis, retinal vascular abnormalities (diabetic disease; central retinal vein occlusion: uveitic retinal dis retinopathy and retinal venous occlusive disease), as a ease; retinal detachment; ocular trauma which affects a sequela of cataract Surgery (Irvine-Gass Syndrome), macu posterior ocular site; a posterior ocular condition caused by lar degeneration, vitreo-macular traction syndrome, inher or influenced by an ocular laser treatment; posterior ocular ited or acquired retinal degeneration, eye inflammation, conditions caused by or influenced by a photodynamic idiopathic central serous chorioretinopathy, pars planitis, therapy; photocoagulation; radiation retinopathy, epiretinal retinitis pigmentosa, radiation retinopathy, posterior vitreous membrane disorders; branch retinal vein occlusion; anterior detachment, epiretinal membrane formation, idiopathic jux ischemic optic neuropathy; non-retinopathy diabetic retinal tafoveal retinal telangiectasia, following Nd:YAG capsulo dysfunction, retinitis pigmentosa and glaucoma. Glaucoma tomy or iridotomy. Some patients with ME may have a can be considered a posterior ocular condition because the history of use of topical epinephrine or prostaglandin ana therapeutic goal is to prevent the loss of or reduce the logs for glaucoma. Macular edema involves the develop occurrence of loss of vision due to damage to or loss of ment of microangiopathy, characterized by abnormal retinal retinal cells or retinal ganglion cells (i.e. neuroprotection). vessel permeability and capillary leakage into the adjacent US 2006/0233859 A1 Oct. 19, 2006 retinal tissues. The macula becomes thickened due to accu oids including dexamethasone have also been shown to have mulation of fluid which leaks out of weak blood vessel walls potent anti-permeability activity by inhibiting the synthesis due to a breakdown of the inner blood-retinal barrier at the of VEGF. Despite known anti-inflammatory and anti-per level of the capillary endothelium, often resulting in signifi meability properties, use of corticosteroid in the treatment of cant disturbances in visual acuity. The blood and fluid leaks macular edema has been limited because of the inability to out of the weak vessel walls into a very small area of the deliver and to maintain adequate quantities of the drugs at macula which is rich in cones,
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