Methods, compositions, and formulations for the treatment of thyroid eye disease

Abstract

Compositions, formulations, methods, and systems for treating thyroid eye disease and related conditions (e.g., Grave's Ophthalmopathy). The methods described herein include administering, to a patient in need, systemic or local beta adrenergic agonists (e.g., as an extended release crystalline microparticle suspension). The methods can further include administering a compound for reducing beta adrenergic receptor desensitization (e.g., a corticosteroid) prior to administering or coadministered with the beta adrenergic agonist. The methods can also include locally administering to the eye an immunosuppressant agent (e.g., rapamycin) prior to administering a beta adrenergic agonist. The compositions described herein include ophthalmic pharmaceutical formulations of beta adrenergic agonists in the form of extended release crystalline microparticle suspensions or mixtures of the crystalline microparticle suspensions with beta adrenergic agonist solutions. The compositions also include ophthalmic formulations of a compound for reducing beta adrenergic receptor desensitization in the form of extended release crystalline microparticle suspensions.

Description

[0001] cross reference [0001] This application claims the benefit of U.S. Provisional Patent Application Serial Nos. 60 / 852,221, filed October 17, 2006, 60 / 898,009, filed January 29, 2007, and 60 / 919,011, filed April 13, 2007, which Incorporated herein by reference in its entirety. Background of the invention [0002] Graves' disease is a common disease with an incidence rate of 1 / 1000 women per year. In addition to hyperthyroidism, 25-50% of individuals with Graves' disease progress to clinically involving the eye, ie, thyroid eye disease. Graves' Ophthalmopathy (GO) is a typical form of thyroid eye disease. While some GO patients suffer only mild ocular discomfort, 3-5% suffer from severe pain and inflammation with diplopia and even vision loss. [0003] The clinical symptoms and signs of GO can be explained mechanistically as a marked increase in tissue volume within the bony orbit. Enlargement of the orbital tissue causes the globe to move forward, and outflow from t...

AI Technical Summary

Problems solved by technology

While some GO patients suffer only mild eye discomfort, 3-5% suffer from severe pain and inflammation with diplopia and even vision loss

Images