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发表于 2004-9-29 10:14
2期临床开始（内容同上）
Multicenter Phase 2 Trial of Remofovir in Hepatitis B Initiated
Date: Tue, 3 Aug 2004 09:03:10 -0400
From: [email protected]
Subject: Multicenter Phase 2 Trial of Remofovir in Hepatitis B Initiated
Multicenter Phase 2 Trial of Remofovir in Hepatitis B Initiated
SAN DIEGO, Aug. 3 /PRNewswire-FirstCall/ -- 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(TM) 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."
Source: Metabasis Therapeutics, Inc.
[此贴子已经被作者于2004-9-28 21:15:06编辑过]
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