DIEPENBEEK, Belgium, May 8, 2012 /PRNewswire/ --
Local ROCK Inhibition Highly Effective in Lowering IOP in Glaucoma Model While Avoiding Hyperemia
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 Veldeet 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."
Amakem is an ophthalmology company developing new treatments for serious eye conditions. Amakem's product pipeline is based on its unique Localized Drug Action platform which is designed to generate safe and effective novel kinase inhibitors that minimize systemic exposure with the aim of reducing side effects. Amakem's lead candidate, AMA0076, is for glaucoma and the Company is working to apply the Localized Drug Action approach to a range of other eye diseases.
Founded in 2010, Amakem has raised more than 21m in funding and is backed by leading life sciences investors including Forbion, Crédit Agricole, Vesalius BioCapital, LRM, PMV/Vinnof and Life Science Research Partners.
Amakem is based in Belgium and located in the life sciences incubator "BioVille" at the University of Hasselt. The Company has a long-standing collaboration with the Ophthalmology Research Center of the University Leuven Hospital.
About Localized Drug Action
Amakem's 'Localized Drug Action' platform is designed to generate novel kinase inhibitor drugs which are contained locally and thus reduce or eliminate side effects. Kinases are crucial mediators of important disease pathways representing more than 22% of the drugable genome. However, kinases are present throughout the body and so there is a significant risk of toxicity due to on target effects in non-target organs and tissues if there is systemic exposure. This risk is acceptable in oncology indications, but not in others thus substantially reducing the potential of drugs targeting this class.
Amakem's kinase inhibitors are designed to be rapidly inactivated outside the target organ. In indications that can be treated by topical administration, it is therefore possible to contain the drug locally as it becomes inactive before it can reach other organs or tissues if it leaks out of the target organ.
Localized Drug Action is based on the inactivation of kinase inhibitors outside the target organ, e.g. in the bloodstream by specifically targeted enzymes. Each of Amakem's kinase inhibitors brings together kinase specificity and enzymatic conversion specificity. When the drug candidate leaves the target organ it is converted to a functionally inactive metabolite. This inactive metabolite is then eliminated from the body.
For more information, please contact
Jack Elands, CEO
Citigate Dewe Rogerson
Chris Gardner/Nina Enegren