DIEPENBEEK, Belgium, November 2, 2011 /PRNewswire/ --
Kinase inhibitor reduces inflammation in the lungs in COPD model with no cardiovascular side effects
Amakem NV, a kinase platform company focusing on ophthalmology, today presented further data demonstrating the effectiveness of its 'Localized Drug Action' approach at the Discovery on Target conference in Boston, MA. The Localized Drug Action platform underpins Amakem's lead product, AMA0076 for the treatment of glaucoma, and has applications to a wide range of kinase inhibitors in indications where local administration is viable: eye, lungs, skin, GI tract, ears and via local injections. The principle is to treat a specific organ with a locally administered drug which is then deactivated before it can reach other organs or tissues. By limiting or avoiding systemic exposure, any potential side effects in non-target organs can be reduced.
The latest research was in an important model of Chronic Obstructive Pulmonary Disease (COPD), the smoking mouse model. Studies, showed that AMA0247, a highly selective Rho Kinase (ROCK) inhibitor, was very effective in inhibiting the inflammatory reaction in the lungs, as measured by neutrophil infiltration, but had no effect on blood pressure or heart rate.
The lack of effects of AMA0247 outside the target organ, and specifically on the cardiovascular system, supports previous data on AMA0076, Amakem's novel, highly potent ROCK inhibitor for the treatment of glaucoma, a condition which damages the optic nerve resulting in vision loss and ultimately blindness. AMA0076 has been proven in preclinical models to be highly effective in reducing intraocular pressure (IOP), a major factor in glaucoma, while avoiding important side effects such as hyperemia. Hyperemia, also known as 'red eye', results from dilatation of blood vessels in the white of the eye and is a distressing and dose limiting side effect for patients.
Jack Elands, CEO of Amakem, said: "This latest study provides further evidence for the effectiveness of our Localized Drug Action platform in harnessing the strengths of kinase inhibitors as new drugs while avoiding the side effects that can limit their use. As well as their potential in our core area of ophthalmology, kinase inhibitors hold great promise for inflammatory diseases such as COPD. However, side effects caused by their activity outside the target organ, for example lowering blood pressure through vasodilation, have severely reduced their potential. We have now shown in one of the most challenging and widely used COPD models that our modified kinase inhibitor can reduce inflammation in the lung without causing cardiovascular problems."
Amakem's primary focus is on eye diseases. As well as developing AMA0076 for glaucoma, the Company is exploring the development of additional compounds targeting other eye diseases and has initiated several collaborations, including the Ophthalmology Research Center of the University Leuven Hospital on several other ophthalmic indications.
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