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METABOLEX REPORTS POSITIVE
PHASE 1 CLINICAL TRIAL FOR TREATMENT OF TYPE 2 DIABETES
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| Company Continues to Advance
Its Insulin Sensitizer Clinical Program |
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HAYWARD, Calif.,
(March 3, 2005): Metabolex, Inc. today announced
positive early clinical trial results for MBX-2044, a novel
investigational, oral insulin sensitizer for type 2 diabetes.
MBX-2044 is designed to eliminate the dose-limiting side effects
of the currently marketed sensitizers. Data from the Phase
1 dose-escalating study showed that the drug was well tolerated
in healthy volunteers.
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| “The insulin sensitizers
currently on the market can effectively control blood glucose
levels. However, they do have significant side effects in terms
of edema and weight gain,” said Kenneth S. Polonsky, M.D.,
Professor of Medicine, Washington University School of Medicine.
“Metabolex is applying its expertise in the biology of
diabetes to develop improved insulin sensitizers that can lower
glucose levels without causing these side effects.” |
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Insulin sensitizers,
with worldwide sales of nearly $4 billion, represent
an attractive treatment option for type 2 diabetes
because they target insulin resistance, the underlying
cause of the disease. Both MBX-2044 and Metabolex's
lead compound, metaglidasen (formerly MBX-102), are
insulin sensitizers that have chemical structures
and methods-of-action that are different than current
insulin sensitizers on the market.
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“MBX-2044 is an excellent
complement to our portfolio of second-generation product candidates,
and the results of this trial enable us to move it forward
to proof-of-efficacy studies,” said David B. Karpf,
M.D., Chief Medical Officer of Metabolex and Clinical Associate
Professor of Medicine at Stanford. “The marketed insulin
sensitizers cause weight gain which can lead many patients
to stop taking them. Moreover, many patients should not even
start therapy with these drugs because they can induce edema,
or fluid retention, which can lead to the serious side-effect
of congestive heart failure.” |
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“By developing optimized
insulin sensitizers, we hope to improve the care of patients
with type 2 diabetes, and also to potentially study these
compounds for the prevention of type 2 diabetes in patients
at increased risk of developing this debilitating disease,”
added Dr. Karpf. |
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The lead candidate in Metabolex's
clinical development program, metaglidasen is now completing
Phase 2 trials. Results will be presented at the 3rd International
Symposium on PPARS Efficacy and Safety in Monte Carlo on March
22, 2005. An interim safety analysis of the Phase 2 trial
indicated that the incidence of edema and weight gain was
no greater than placebo.
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| MBX-2044 Study
Design |
| In the Phase 1 clinical trial for MBX-2044,
healthy volunteers were given a single dose ranging from 1.5
mg to 120 mg. There were seven dosing cohorts and each cohort
consisted of six non-diabetic men and women who were either
overweight or normal weight. MBX-2044 was well tolerated at
all doses and showed a reduction in uric acid levels, a property
also shared by metaglidasen, after a single dose. |
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| Novel Method-of-Action |
| PPARs (peroxisome proliferator-activated receptors)
control the expression of genes involved in glucose metabolism,
lipid metabolism and inflammation. Metaglidasen and MBX-2044
are Selective PPAR Modulators (SPPARMs) that modulate the genes
needed for insulin sensitization, but not those responsible
for edema and weight gain. |
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| About Diabetes |
| Type 2 diabetes is a disease characterized
by insulin resistance, in which the body does not properly use
insulin, the hormone that converts glucose into energy. According
to the American Diabetes Association, it is the 6th leading
cause of death in the United States and affects about 18.2 million
people, while about 41 million people in the U.S. are prediabetic.
Most diabetics have type 2, or adult-onset, diabetes and the
incidence is expected to rise to 10 percent of the population
by the year 2010. |
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| The cause of diabetes is unknown, although
genetics and environmental factors such as lack of exercise
and obesity appear to play a role. Treatment includes dietary
changes, insulin injections, and oral therapies. |
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| About Metabolex |
Metabolex is a privately
held biotechnology company dedicated to the discovery and
development of novel therapeutics to transform the treatment
of diabetes and related metabolic disorders. Metabolex has
drawn on its deep understanding of diabetes to create the
largest database of genes involved in diabetes and to build
a rich pipeline of product candidates and drug discovery targets.
The company's clinical program is focused on developing next-generation
insulin sensitizers that lower blood glucose without the serious
safety and tolerability issues associated with currently marketed
products. |
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| For additional information about
Metabolex and its development pipeline, visit www.metabolex.com. |
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