GUANIDINIUM DERIVATIVES FOR THE TREATMENT OF OCULAR PAIN

PROJECT SUMMARY The absence of safe and effective strategies for the management of ocular pain is motivating the development of a novel topical drug suitable for patient self administrationConventional local anestheticssuch as proparacaineinhibit voltage gated Naion channelsNaVand are highly effective for the management of ocular pain in acutein office settingsHoweverthese agents are short acting and toxic to the corneal surfacewhich prevents their use beyond a few administrationsSiteOne Therapeutics has discovered a chemical series of novelexquisitely selective inhibitors of human NaVa subtype implicated in the transmission of pain signals by human geneticsThese compounds exhibit excellent analgesic effects when administered systemicallyTopical ocular administration is well tolerated and leads to good intraocular exposureThe goal of this phase II grant is to fund preclinical studies including candidate selectionformulation developmentand early IND enabling studies PROJECT NARRATIVE Ocular pain is the single most common reason for a visit to an ophthalmologistDespite the high prevalence of this conditioncurrently no drug is available to effectively manage itExisting local anestheticssuch as proparacaineare toxic to the corneal surface and suitable only for in office administrationWe aim to develop a safeeffectivelong acting topical therapy for ocular pain and discomfortwhich is suitable for patient selfadministration