Amakem NV, a kinase platform company focusing on ophthalmology, presented key preclinical data on its potent, locally active Rho Kinase (ROCK) inhibitor AMA0076 at the 2012 Association for Research in Vision and Ophthalmology (ARVO) Annual Meeting being held at Fort Lauderdale, US from 6 - 10 May. The ARVO meeting is the world's largest gathering of international eye and vision researchers.
Amakem presented two posters which highlight the significant potential of AMA0076 as a novel potential treatment for glaucoma. Based on Amakem's 'Localized Drug Action' platform, AMA0076 is a highly potent ROCK inhibitor that has been designed to allow for high localized dosing in the eye combined with low systemic exposure. AMA0076 is aimed at providing better patient outcomes than other ROCK inhibitor based treatments currently in development because its improved side effect profile enables higher dosing, leading to better efficacy.
Van de Velde et al showed that topical administration of AMA0076 lowers intraocular pressure (IOP) in an efficient manner in normotensive NZW and DB rabbits, with a potency exceeding that of the development stage ROCK inhibitor Y-39983 and the leading current glaucoma treatment Latanoprost (Poster Number D821). In contrast with Y-39983, following administration of AMA0076, no hyperemia was observed at the concentrations tested and no lowering of IOP was seen in the untreated eye. These data highlight AMA0076's potential therapeutic value while the absence of hyperemia and the lack of effect in the untreated eye offer an improved side effect profile compared to other ROCK inhibitors that have been in development or that are currently in development.
Hollanders et al used a glaucoma model to show that benzalkonium chloride (BAK) increases the effectiveness of AMA0076 in reducing IOP versus AMA0076 alone (Poster Number D818). AMA0076 has already been shown to be more effective in reducing IOP than existing treatments and other ROCK inhibitors in several preclinical models. This study suggests this effect could be further enhanced by using BAK to increase the permeability of AMA0076.
Jack Elands, CEO of Amakem, said: "Existing treatments for glaucoma are not effective for all patients and there is a real need for new approaches to a condition which affects many millions of people and remains a significant cause of blindness. The data presented at ARVO supports our belief that in AMA0076 we have a highly promising candidate for treatment of one of the most important eye diseases. What is most remarkable about AMA0076 is that it is effective in reducing IOP, without causing hyperemia, a problem that has hampered the development of other ROCK inhibitors. Thus, AMA0076 may offer a significant improvement in the treatment of glaucoma."
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