Amakem Initiates Phase 2a Proof of Concept Study with the Rho Kinase (ROCK) Inhibitor AMA0076 in Patients with Glaucoma and Ocular Hypertension under a US IND
DIEPENBEEK, Belgium, September 27, 2012 /PRNewswire/ –
Amakem NV, a kinase platform company focusing on ophthalmology, today announces that
it has initiated a Phase 2a proof of concept study of its novel Rho Kinase (ROCK)
inhibitor, AMA0076, in patients with glaucoma and ocular hypertension. The start of the
study follows Amakem’s receipt of Investigational New Drug Application (IND) approval from
the United States Food and Drug Administration (FDA). AMA0076 is a highly potent ROCK
inhibitor and is based on Amakem’s ‘Localized Drug Action’ platform, which generates novel
kinase inhibitors that minimize the risk of systemic as well as local side effects such as
The study is a multicenter, randomized, double-masked, placebo-controlled
dose-escalation study with AMA0076 applied topically, as eye drops. First patients have
initiated treatment in this 80 patient clinical trial with six participating centers in
the United States (ClinicalTrials.gov identifier NCT01693315).
The primary efficacy endpoint will be reduction in intraocular pressure (IOP), which
is a major factor in the pathology of glaucoma, after two and four weeks of dosing. A
number of secondary efficacy endpoints will be used to further analyze the impact of
AMA0076 on IOP. The Company expects to report top line results in 2013.
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. Pre-clinical studies have shown that AMA0076
highly effectively lowers IOP in relevant models, with a magnitude of IOP reduction
exceeding that of the current leading glaucoma treatment latanoprost. Importantly, AMA0076
has been shown to avoid hyperemia, also known as ‘red eye’, which is seen as a major dose
limiting side effect for other ROCK inhibitors in development.
Dr Jack Elands, CEO of Amakem, said: “Today’s announcement is a major milestone for
Amakem. With our first product entering the clinic we expect to validate our Localized
Drug Action platform. Conceived and developed by the company’s founder and CSO, Dr Dirk
Leysen, this platform allows the development of novel drugs in ophthalmology and other
indications, by harnessing the power of kinase inhibition while managing potential side
effects. It is very satisfying to have progressed AMA0076 within 20 months from discovery
into its first clinical trial and to the point where we believe we will further
demonstrate the potential of our platform to create valuable new therapeutics.”
Dr Steve Pakola, Chief Medical Officer of Amakem, said: “Glaucoma affects many
millions of people and remains a significant cause of vision loss and blindness. Existing
treatments are not effective for all patients and while the potential of ROCK inhibitors
to reduce IOP has been recognized, their development has been held back by their side
effect profile, particularly hyperemia which is distressing for patients and reduces
compliance. We look forward to confirming in the clinic the highly promising results we
have seen so far with AMA0076 and to advancing what we believe has the potential to be a
valuable new treatment option for glaucoma patients.”
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. AMA0076 is currently undergoing Phase 2a proof
of concept trials.
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 email@example.com +32(0)474-828-580 Citigate Dewe Rogerson Chris Gardner/Nina Enegren firstname.lastname@example.org email@example.com +44(0)20-7638-9571
SOURCE Amakem NV