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METABASIS ANNOUNCES PUBLICATION OF A NEW MOLECULAR MODELING TECHNOLOGY
FOR IMPROVING DRUG DISCOVERY AND OPTIMIZATION
SAN DIEGO, CA - July 13, 2004 - Metabasis Therapeutics,
Inc. (NASDAQ: MBRX) announced today the publication of an article
entitled "Development of a Quantum Mechanics-Based Free-Energy
Perturbation Method: Use in the Calculation of Relative Solvation
Free Energies" in the Journal of the American Chemical Society
(126, 6224-6225 (2004)). The publication by M. Rami Reddy et al.,
describes Metabasis' work on a new molecular modeling technology.
Efforts by pharmaceutical companies to design drugs using a combination
of structural information on drug targets and computation methods
has been hampered by limitations in calculation accuracy, throughput
or both. As described in the article published in the Journal of
the American Chemical Society, Metabasis, in collaboration with
U. Chandra Singh, has developed a method that has the potential
to address both limitations. The method, which entails for the first
time the integration of quantum mechanics (QM) with a method known
as free energy perturbation, was used to predict the relative differences
in the solvation free energies of small molecules.
"Metabasis is developing proprietary methods that make use
of the findings reported in the publication. If successful, Metabasis
expects to use the technology on its discovery programs in an effort
to more efficiently find novel leads and convert these leads to
drug candidates, " commented Dr. Paul Laikind, Chairman, President
and CEO of Metabasis.
Metabasis Executive Vice President of Research and Development,
and an author of the publication, Dr. Mark Erion, stated "Success
in these calculations suggests that the method may soon be useful
for predicting relative binding affinities for small molecules against
a drug target as well as certain drug properties such as the partition
coefficient, solubility and ionization potential. Moreover, the
use of QM may enable future automation of calculations using free
energy perturbation and therefore provide an accurate method for
computationally screening compound libraries for new leads and for
more efficient lead optimization."
Metabasis made extensive use of computer assisted drug design strategies
during the development of its proprietary NuMimetic technology,
which was subsequently used to discover CS-917. CS-917 is a first-in-class
gluconeogenesis inhibitor for the treatment of type 2 diabetes.
In a recent Phase II trial, CS-917 appeared to significantly lower
blood glucose levels in patients over a 28 day period. The NuMimetic
technology was also used to discover MB07803, a 2nd generation gluconeogenesis
inhibitor for type 2 diabetes that is expected to enter the clinic
next year, as well as a lead compound for an advanced research program
focused on the discovery of another first-in-class drug that may
be useful for treating hyperlipidemia and diabetes.
About Metabasis (www.mbasis.com):
Metabasis Therapeutics, Inc. is a biopharmaceutical company focused
on the discovery, development and commercialization of novel small
molecule drugs principally to treat metabolic diseases linked to
pathways in the liver and to treat liver diseases. The company has
established a broad product pipeline targeting large markets with
significant unmet medical needs. Metabasis has three internally
discovered, novel product candidates in clinical development: CS-917,
remofovir and MB07133, indicated for the treatment of type 2 diabetes,
hepatitis B and primary liver cancer, respectively. All three products
are being studied in patients and preliminary evidence of efficacy
has been demonstrated with CS-917 and remofovir. Metabasis has developed
several proprietary technologies for use in discovering and optimizing
drugs, including the NuMimetic technology and the HepDirect
technology. The NuMimetic Technology was used to discover CS-917,
a first-in-class gluconeogenesis inhibitor, and was also used to
identify MB07803, a 2nd generation gluconeogenesis inhibitor that
is expected to enter the clinic in 2005 for the treatment of type
2 diabetes. The HepDirect technology, a liver-targeted prodrug technology,
was used to develop remofovir and MB07133 and is also being used
in a partnership with Merck & Co., Inc. to discover new treatments
for hepatitis C. Metabasis is continuing to identify and develop
new product candidates using its proprietary technologies and know-how.
Forward-Looking Statements:
Statements in this press release that are not strictly historical
in nature constitute "forward-looking statements." Such
statements include, but are not limited to, references to Metabasis'
new molecular modeling technology, its applications and capabilities,
as well as statements about Metabasis' other proprietary technologies
as well as its product candidates and research programs. Such forward-looking
statements involve known and unknown risks, uncertainties and other
factors which may cause Metabasis' actual results to be materially
different from historical results or from any results expressed
or implied by such forward-looking statements. These factors include,
but are not limited to, risks and uncertainties related to the progress
and timing of clinical trials for Metabasis' product candidates;
difficulties or delays in development, testing, obtaining regulatory
approval, producing and marketing Metabasis' product candidates;
adverse side effects or inadequate efficacy of Metabasis' product
candidates or proprietary technologies; Metabasis' dependence on
collaborative partners; the scope and validity of intellectual property
protection for Metabasis' product candidates, proprietary technologies
and their uses; competition from other pharmaceutical or biotechnology
companies; Metabasis' ability to obtain additional financing to
support its operations; and other factors discussed in the "Risk
Factors" section of Metabasis' prospectus filed with the Securities
and Exchange Commission pursuant to Rule 424(b)(4) of the Securities
Act on June 16, 2004. All forward-looking statements are qualified
in their entirety by this cautionary statement. Metabasis is providing
this information as of this date of this release and does not undertake
any obligation to update any forward-looking statements contained
in this release as a result of new information, future events or
otherwise.
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