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METABASIS ANNOUNCES INITIATION OF A MULTI-CENTER PHASE 2 CLINICAL
TRIAL OF REMOFOVIR FOR THE TREATMENT OF HEPATITIS B
SAN DIEGO, CA - August 3, 2004 - Metabasis Therapeutics,
Inc. (NASDAQ: MBRX) announced today the initiation of a multi-center,
multi-national Phase 2 study to evaluate the orally administered
antiviral compound remofovir mesylate in chronic hepatitis B (HBV)
infected patients. Metabasis discovered remofovir using its HepDirect
prodrug technology. In October 2001, Metabasis entered into an exclusive
worldwide development and license agreement with Valeant Pharmaceuticals
International, under which Valeant is primarily responsible for
the clinical development and registration of remofovir.
This Phase 2 study of remofovir is an open-label, randomized, multiple
oral dose study that will enroll 220 patients with compensated hepatitis
B infection at approximately 20 sites in the U.S., Taiwan, Singapore
and Korea. The study consists of five treatment groups: remofovir
- 5, 10, 20 and 30 mg/day, and Hepsera (adefovir dipivoxil) - 10
mg/day. Treatment duration will be 48 weeks and an interim analysis
will be conducted following 24 weeks of dosing to evaluate drug
safety and efficacy and, if warranted, will be used for selection
of a dose for Phase 3 studies.
Remofovir was developed using Metabasis' proprietary HepDirect
technology, a broadly applicable, liver-targeting prodrug technology
that was recently described in a Journal of the American Chemical
Society article entitled "Design, Synthesis, and Characterization
of a Series of Cytochrome P(450) 3A-Activated Prodrugs (HepDirect
Prodrugs) Useful for Targeting Phosph(on)ate-Based Drugs to the
Liver," (J. Am. Chem. Soc. 126, 5154-5163 (2004)). A prodrug
is a drug to which a chemical modification has been made that renders
the target drug inactive until enzymes in the body convert it to
its active form. In the case of a HepDirect prodrug, the enzyme
that converts it to an active form is found predominantly in the
liver. Remofovir is a HepDirect prodrug of a compound called adefovir.
Adefovir is the active component of the approved hepatitis B drug
Hepsera (adefovir dipivoxil). Hepsera is also a prodrug, however,
it is converted to the active form predominantly in the plasma.
Remofovir is designed to generate an active form of adefovir primarily
in the liver, where the virus resides, while limiting exposure outside
the liver. While the safety and efficacy of this approach remains
to be definitively proven in the clinic, this is potentially important
because while adefovir is associated with significant decreases
in HBV DNA levels, it also appears to be associated with treatment
limiting renal toxicity.
"We expect this new clinical trial to build on the pre-clinical
and clinical results we have seen to date with remofovir,"
commented Dr. Paul Laikind, Metabasis' Chairman, President and CEO.
"Valeant submitted an abstract to the American Association
for the Study of Liver Diseases (AASLD) describing the safety, tolerance,
pharmacokinetic and pharmacodynamic results from a recently completed
clinical trial of remofovir in patients infected with hepatitis
B virus. If the abstract is accepted, the results of this trial
would be presented at the 55th Annual Meeting of the AASLD in Boston
in October/November 2004. The findings from that trial led to the
decision to proceed with the Phase 2 study announced today. This
new study is designed to assess the maximally effective dose of
remofovir and assist in dose selection for the pivotal Phase 3 studies
that are expected to begin next year should the results warrant
it."
Hepatitis B remains a significant medical problem that affects
an estimated 300 million people worldwide and can cause severe liver
damage leading to liver cirrhosis and primary liver cancer. The
World Health Organization estimates that hepatitis B infection results
in more than one million deaths each year worldwide.
Dr. Mark Erion, Executive Vice President of Research and Development
at Metabasis stated, "In addition to representing an important
milestone in the development of remofovir, the initiation of this
study also gives us further confidence in the potential of our HepDirect
technology. In addition to remofovir, the HepDirect technology was
used to develop MB07133, a HepDirect prodrug of an oncolytic agent.
MB07133 is currently being studied in patients with primary liver
cancer, a deadly disease with few treatment options. The HepDirect
technology is also being used in our collaboration with Merck &
Co., Inc. to discover novel products for the treatment of hepatitis
C. Finally, we continue to evaluate the technology and its use in
certain other programs."
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-targeting prodrug
technology, was used to develop remofovir and MB07133 and is also
being used in a partnership with Merck 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'
drug candidate remofovir and its apparent activities, efficacy and
clinical development, the HepDirect technology and its applications
and capabilities and the market potential for drugs developed using
the HepDirect technology 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; the fact that positive
results from pre-clinical studies and early clinical trials does
not necessarily mean later clinical trials will succeed; 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 its licensee
Valeant, which is primarily responsible for the clinical development
and registration of remofovir; 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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