Last updated on April 18, 2014 at 0:14 EDT

Amakem Announces Further Proof-of-Concept Results for its ‘Localized Drug Action’ Platform

November 2, 2011

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.

About Amakem

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 EUR21m in funding and is
backed by leading life sciences investors including Forbion, Credit
Agricole, Vesalius BioCapital, LRM, PMV/Vinnof and Life Science Research

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
        Amakem NV
        Jack Elands, CEO

        Citigate Dewe Rogerson
        Chris Gardner/Nina Enegren


Source: PR Newswire