CURACYTE
SCIENTISTS DISCOVER NEW ANTI-TUMOR AGENTS
Munich,
Germany, June 17th , 2003 - Curacyte AG, a Munich-based drug
development company focused on novel treatments of inflammatory diseases,
thrombotic disorders and cancer has announced today that its scientists
have discovered a series of novel small molecule inhibitors of matriptase,
a trypsin-like serine protease. Matriptase is an important mediator in the
degradation of the extracellular matrix, a process which plays a key role
during metastasis. Inhibiting this key enzyme produced by tumor cells
might provide a route to prevent tumor metastasis and invasive growth.
This compound series thus offers potential as novel anti-tumor agents for
the treatment of metastatic malignancies and Curacyte will now move this
program into pre-clinical development.
Since the discovery
of the gene in 1999, matriptase has increasingly gained attention as a
potential biological target for inhibiting tumor spread. Today, matriptase
is recognized as an innovative anti-cancer target. In in vitro assays, the
Curacyte inhibitor series exhibit excellent affinity and selectivity
towards the target and a pharmacokinetic profile that supports their use
as pharmaceutically active substances.
Dr. Helmut
Giersiefen, Chief Executive Officer of Curacyte AG, commented on the
recent scientific success:
"The discovery
of the matriptase inhibitors corroborates the validity and value of our
protease technology. Based on our proprietary inhibitor libraries and our
competence with respect to the chemistry of these substances, we have
identified a series of novel potential anti-tumor agents, enabling us to
move another important project into preclinical development. We will
continue to derive therapeutically valuable applications from our protease
technology that we can leverage with pharmaceutical partners."
Curacyte pursues the
development of its protease technology in close collaboration with the
Center of Vascular Biology and Medicine of the University of Jena
(Germany) under the leadership of Dr. Jörg Stürzebecher, a well-known
pioneer in the area of synthetic inhibitors of serine proteases.
"We are very
proud of our collaboration with Curacyte," commented Dr. Stürzebecher.
"The successful development of these matriptase inhibitors was
possible by combining our knowledge of the structure-function relationship
of protease inhibitors that we gained over decades with the competence in
drug discovery and pharmaceutical development provided by Curacyte. Our
collaboration on protease inhibitors, including matriptase has been
ongoing for over two years and establishes a benchmark for the fruitful
synergies that can be created by bringing together academic and commercial
competencies."
- End
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Notes
1. Curacyte – www.curacyte.com
Curacyte AG was founded in 1999 as a research-based biopharmaceutical
company dedicated to the discovery and development of innovative and
clinically meaningful new medicines. Last year, the company announced its
merger with VitaResc Biotech AG, a development-stage company focused on
novel treatments of inflammatory diseases, thrombotic disorders and
cancer. The Company has one product in the clinic, this lead product,
Pyridoxalated Hemoglobin Polyoxethylene (PHP), is currently in a Phase III
pivotal study as a treatment for patients suffering from distributive
shock and has several programs in pre-clinical development.
In addition to
matriptase inhibitors, the company has a number of research and
pre-clinical programs focused on other protease inhibitors:
In order to exploit
the utility of protease inhibitors in extracorporeal blood treatment
applications, in September 2002, Curacyte announced that it had entered
into a sublicensing agreement with Gambro Dialysatoren GmbH (Hechingen,
Germany). Several development projects of Curacyte have their origin in
the protease technology, including inhibitors of Factor Xa, plasma
kallikrein and urokinase. Inhibitors of Factor Xa are currently in the
lead optimization stage as oral anticoagulants and plasma kallikrein
inhibitors are being evaluated for preventing activation of blood clotting
on surfaces of hemodialysis membranes. CJ-463 represents the first highly
specific inhibitor of urokinase and has been in formal preclinical
development since Q3 2002. Curacyte anticipates initiating first clinical
studies with this anti-metastatic agent early in 2004.
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