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Plexxikon Inc. today announced data from preclinical studies
of Polycystic Kidney Disease (PKD) demonstrating
significantly reduced kidney disease following treatment
with Plexxikon’s novel drug candidate. Plexxikon’s novel
small molecule kinase inhibitor is a highly selective and
potent inhibitor of Raf kinase, a critical mediator of PKD
pathology. These data were recently presented at the ISN
Forefronts Symposium on Polycystic Kidney Disease in
Montreal, Canada by Stefan Somlo, M.D., CNH Long Professor
of Internal Medicine and Genetics and Chief of Nephrology at
the Yale University School of Medicine.
“The
degree to which this compound slowed progression of the
kidney disease in preclinical models with early onset
aggressive polycystic kidney disease was very dramatic,
demonstrating the promise of this agent as a candidate
therapy for patients with this disease,” stated Dr. Somlo.
“There are currently no treatments for PKD, which is an
inherited disease of the kidneys and other organs that often
becomes manifest between the ages of 30 and 40 and
eventually leads to kidney failure in a significant
proportion of affected individuals.”
“Plexxikon’s PKD drug candidate is another example of the
highly selective kinase inhibitors we are developing at
Plexxikon, a prerequisite for a compound to be useful in
treating a chronic disease such as PKD, and we are pleased
to see such strong preclinical data in polycystic kidney
disease and safety in GLP toxicology studies,” stated K.
Peter Hirth, Ph.D., chief executive officer of Plexxikon.
“We look forward to initiating a Phase 1 clinical trial for
this novel drug candidate in 2008.”
In the
preclinical study of Plexxikon’s PKD drug candidate, doses
of the drug candidate were administered orally daily for 14
days. A marked reduction in kidney cyst burden was observed
in the treatment group compared to vehicle treated mice.
Levels of blood urea nitrogen (BUN), an indicator of kidney
function, were also significantly improved in the
drug-treated groups compared with the vehicle-treated group,
suggesting that improved renal function accompanied reduced
cyst growth in treated animals.
Using its
proprietary Scaffold-Based Drug Discovery™ platform,
Plexxikon has identified a portfolio of unique compounds
that selectively block Raf-dependent cells, leaving healthy
cells unharmed since Raf activity is differentially
regulated in those cells. The co-crystallography platform
enabled scientists at Plexxikon to determine the exact
location where such inhibitors selectively bind to the
kinase active site.
Plexxikon’s family of Raf
kinase inhibitors selectively target a unique binding site
of the protein, minimizing the common side effects seen from
other less selective kinase inhibitors. In several different
systems, Plexxikon’s Raf inhibitor blocks proliferation of
dysfunctional cells, without detectable affects on healthy
cells. Interestingly, our drug candidate is highly selective
for the PKD indication, with no detectable inhibition of
cancer cell line growth – including no activity in cancers
bearing the important B-RafV600E oncogene.
PKD is a genetic disease characterized by the development of
many fluid filled cysts in the kidneys. The cysts can
profoundly increase the size of the kidneys while damaging
much of the normal tissue resulting in impaired function of
the kidneys and ultimately kidney failure. Approximately
600,000 people in the U.S. and 12.5 million people worldwide
suffer from PKD, which is the fourth leading cause of kidney
failure. Patients whose kidneys fail require either dialysis
or kidney transplantation to survive. There are currently no
treatments available to alter the progression of PKD.
In other news,
Plexxikon today announced the appointment of Edward T.
Mathers to its board of directors. Mr. Mathers currently
serves as executive vice president, corporate development
and venture at MedImmune, where he has been since 2002. He
is responsible for the company’s licensing and business
development activities and is also a key leader of the
company’s MedImmune Ventures, Inc. team evaluating
investment opportunities.
“We are pleased to
welcome Ed to our board of directors. His depth of
experience in corporate development will be invaluable as we
further develop and execute on our business strategies and
position our product candidates for partnering. While
Plexxikon has been very successful to date in securing
industry leading partnerships, our discovery platform has
continued to prove prolific in producing a broad portfolio
of unpartnered assets. We are pleased to bring in Ed’s
expertise as our business grows and additional strategic
opportunities are explored,” stated Dr. Hirth.
Prior to joining MedImmune, Mr. Mathers was vice president
of marketing and corporate licensing and acquisitions at
Inhale Therapeutic Systems. He was with Glaxo Wellcome, Inc.
(GlaxoSmithKline) for 15 years prior to that holding a
number of increasingly responsible positions in sales and
marketing. Mr. Mathers started his career at Ortho
Pharmaceuticals Corporation (a division of Johnson &
Johnson) as a researcher. In addition to Plexxikon, he
currently serves on the boards of directors of both
Metastatix, Inc. and Kémia, Inc. He holds a bachelor’s
degree in chemistry from North Carolina State University.
Plexxikon Profile
Plexxikon Profile Plexxikon is a leader in structure-guided
discovery and development of novel small molecule
pharmaceuticals to treat human disease. The company’s
clinical stage programs include PLX204 for the treatment of
diabetes, and PLX4032 for the treatment of melanoma and
colorectal cancer. Preclinical development programs include
a kinase inhibitor for the treatment of pain, and a
portfolio of kinase inhibitors for the treatment of kidney
disease, rheumatoid arthritis and metastatic breast cancer.
Plexxikon’s proprietary Scaffold-Based Drug Discovery™
platform is being applied to build a pipeline of diverse
product opportunities for the treatment of metabolic and
cardiovascular disease, inflammation, oncology and CNS
disorders. This discovery process integrates a number of
state-of-the-art technologies, including structural
screening as one key component that provides a significant
competitive advantage over other drug discovery approaches.
To date, the company has discovered a portfolio of clinical
and preclinical stage compounds in multiple disease areas
addressing significant unmet needs in each therapeutic
category.
Plexxikon is seeking pharmaceutical
and biotechnology partners for select collaboration
opportunities. For more information, please visit
www.plexxikon.com.
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