Amakem Presents AMA0076 Data at the 2012 ARVO Annual Meeting
DIEPENBEEK, Belgium, May 8, 2012 /PRNewswire/ –
Local ROCK Inhibition Highly Effective in Lowering IOP in Glaucoma Model While
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
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
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 EUR21m in funding and is backed by
leading life sciences investors including Forbion, Credit 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
Amakem NV Jack Elands, CEO firstname.lastname@example.org +32(0)474-828-580
Citigate Dewe Rogerson Chris Gardner/Nina Enegren email@example.com firstname.lastname@example.org +44(0)20-7638-9571