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Roche Pharmaceuticals

Ground-Breaking Combination of All-Oral Agents Demonstrates Potential as Hepatitis C Treatment Regimen

BASEL, Switzerland, BRISBANE, California and PRINCETON, New Jersey,
April 25 (ots/PRNewswire)

-

- Combination of R7227, Protease Inhibitor, and R7128, Nucleoside
Polymerase Inhibitor, Shows Significant Potency in Reducing Viral
Load in  Patients With Hepatitis C
Roche (SWX: RO, ROG; OTCQX: RHHBY), InterMune, Inc. (Nasdaq:
ITMN) and Pharmasset (Nasdaq: VRUS) today announced the first results
from their innovative, interferon-free regimen of direct-acting
antiviral (DAA) combination therapy for the treatment of patients
chronically infected with the hepatitis C virus (HCV). The study
combined two oral DAAs, R7227 (also known as ITMN-191) and R7128, for
the first time in patients. There were no serious adverse events
reported during the 14 days of dosing, the reductions in levels of
HCV RNA were significant.
Results of the INFORM-1 study were presented during the
late-breaker session today at the 44th Annual Meeting of the European
Association for the Study of the Liver (EASL) in Copenhagen.
The trial, conducted in centres in New Zealand and Australia, is
the first to investigate the combination of two oral antiviral
medicines in the absence of weekly injections of interferon, or
ribavirin. The results demonstrate for the first time that an oral
protease inhibitor and an oral nucleoside polymerase inhibitor can be
safely and effectively combined, and thus have the potential to be
developed into a new treatment regimen for hepatitis C patients.
Roche is developing R7227, a protease inhibitor, with InterMune, and
R7128, a nucleoside polymerase inhibitor, with Pharmasset.
Further studies will test the activity and safety of the
combination of R7227 and R7128 with and without interferon and/or
ribavirin. The current standard of care for HCV is a combination of
pegylated interferon plus ribavirin, which delivers overall cure
rates of 50-60%.
"These are exciting times in our fight against hepatitis C, and
the investigation of the innovative oral treatment regimen in
INFORM-1, if validated in further study, may radically change future
treatment strategies in our patients with chronic HCV infection,"
said Edward Gane, M.D., Associate Professor, University of Auckland
and Director, Auckland Clinical Studies Limited. "The initial results
from this study of the R7227/R7128 combination raise hopes of the
possibility for an interferon-free treatment regimen, as well as the
potential for a shorter, more potent interferon-based regimen."
INFORM-1 Results in Brief
INFORM-1 is a randomized, double-blind, ascending dose Phase I
trial which has enrolled a total of 57 patients.
Patients receiving the combination of R7227 and R7128 for 14 days
- without pegylated interferon or ribavirin - experienced a median
reduction in viral levels of -4.8 to -5.2 log10IU/mL in the highest
doses tested. The addition of R7128 to R7227 resulted in sustained
viral load reductions over the dosing period, with ~63% of patients
experiencing a decrease in viral levels below the quantification
limit of the diagnostic assay (less than 40 IU/mL). Furthermore, 25%
of patients in the highest dosage groups were below the limit of
detection of virus in their blood (less than 15 IU/mL) after 14 days.
In the early low-dose groups, after only three days of dosing,
the mean reduction in viral load levels was 0.6 log10 greater with
combination treatment (-2.9), compared to the performance of the
individual compounds when administered as a single agent (-0.46 and
-1.84 for R7128 and R7227, respectively). This suggests an additive
effect for the combination.
The combination was well tolerated over 14 days, with no
treatment-related serious adverse events (SAEs), no dose reductions
and no discontinuations. Pharmacokinetic analysis confirmed that
there were no drug-drug interactions between the compounds.
Next Steps in the Development Program
The companies are now exploring twice-daily dosing of R7227 and
higher total daily doses (600 mg twice-daily and 900 mg twice-daily)
than those explored in the first patient cohorts of INFORM-1. The
companies also plan to explore the innovative DAA combination therapy
in "treatment-experienced" patients with HCV, or those who did not
achieve a cure with a previous interferon-based treatment.
Other Clinical Studies with R7227 and R7128
In addition to clinical studies of interferon-free combination
DAA regimens such as those studied in INFORM-1, R7227 and R7128 each
are proceeding rapidly in development in combination with Roche's
PEGASYS(R) (peginterferon alfa-2a) and COPEGUS(R) (ribavirin). A
Phase IIb study with R7128 has now begun, while a Phase IIb study
with R7227 is slated to begin in the summer.
The Foundation and Future of HCV Treatment
Combination therapy of pegylated interferon and ribavirin is the
current standard of care for HCV. PEGASYS is the leading treatment
for HCV, and also is the pegylated interferon therapy of choice for
most HCV antiviral agents in development - including those developed
through collaborations with Roche, as well as those developed by
other companies. The collaborations with InterMune and Pharmasset
position Roche as a leader in developing innovative treatments for
HCV.
Dial-In and Webcast Details
InterMune and Pharmasset will host a live webcast of a discussion
of the INFORM-1 results from the EASL conference today, Saturday,
April 25, 2009, at 7:00 p m. CEST (1:00 p.m. EDT). Participating in
the discussion will be Dr. Ed Gane, principal investigator in the
INFORM-1 trial. Members of management from Roche, InterMune and
Pharmasset will also be available to answer questions. A live webcast
and slide presentation will be available through the Investor
Relations pages of both InterMune and Pharmasset at
http://www.intermune.com or http://www.pharmasset.com, respectively.
Alternatively, interested parties may access the discussion and ask
questions by dialing 888-799-0528 (U.S. & Canada) or 973-200-3372
(International), conference ID # 95452531. A webcast replay will be
available approximately three hours after the call and will be
archived at http://www.intermune.com and at
http://www.pharmasset.com.
The teleconference replay will be available for 10 business days
following the call and can be accessed by dialing 800-642-1687 (U.S.
and Canada) or 706-645-9291 (international), and entering conference
ID # 95452531.
The companies recommend logging on at least 15 minutes prior to
the start of the webcast to ensure adequate time for any software
downloads that may be required.
About R7227 (ITMN-191)
R7227 is a potent, macrocyclic inhibitor of HCV NS3/4A protease
activity,  and has produced multi-log10 reductions in levels of HCV
levels in chronic  HCV patients, when administered for 14 days as
monotherapy and when combined  with PEGASYS and COPEGUS. R7227 was
safe and well tolerated in these studies.
About InterMune
InterMune is a biotechnology company focused on the research,
development  and commercialization of innovative therapies in
pulmonology and hepatology. InterMune has a pipeline portfolio
addressing idiopathic pulmonary fibrosis (IPF) and hepatitis C virus
(HCV) infections. The pulmonology portfolio includes the Phase 3
program, CAPACITY, which is evaluating pirfenidone as a possible
therapeutic candidate for the treatment of patients with IPF and a
research program focused on pirfenidone analog ITMN-520. The
hepatology portfolio includes the HCV protease inhibitor compound
R7227 (ITMN-191), a second-generation HCV protease inhibitor research
program, and a research program evaluating a new target in
hepatology. For additional information about InterMune and its R&D
pipeline, please visit http://www.intermune.com.
About R7128 R7128, a cytidine nucleoside analog inhibitor of HCV
RNA polymerase, is being developed for the treatment of chronic HCV
infection. R7128 has shown potent in vivo activity against all of the
most common HCV genotypes (1, 2 and 3). R7128 was safe and well
tolerated when given with PEGASYS and COPEGUS for up to 28 days.
About Pharmasset
Pharmasset is a clinical-stage pharmaceutical company committed
to discovering, developing and commercializing novel drugs to treat
viral infections. Pharmasset's primary focus is on the development of
oral therapeutics for the treatment of hepatitis B virus (HBV),
hepatitis C virus (HCV) and human immunodeficiency virus (HIV).
Pharmasset is currently developing three product candidates. R7128,
an oral treatment for chronic HCV infection, has completed a 4-week
clinical trial in combination with PEGASYS plus COPEGUS through a
strategic collaboration with Roche, and is initiating a Phase 2b
trial. Racivir, which is being developed for the treatment of HIV in
combination with other approved HIV drugs, has completed a Phase 2
clinical trial. PSI-7851, an unpartnered second generation HCV
nucleotide analogue recently entered phase 1 studies. Additional
information is available on the Internet at http://www.pharmasset.com
About Roche
Headquartered in Basel, Switzerland, Roche is a leader in
research-focused healthcare with combined strengths in
pharmaceuticals and diagnostics. Roche is the world's largest biotech
company with truly differentiated medicines in oncology, virology,
inflammation, metabolism and CNS. Roche is also the world leader in
in-vitro diagnostics, tissue-based cancer diagnostics and a pioneer
in diabetes management. Roche's personalised healthcare strategy aims
at providing medicines and diagnostic tools that enable tangible
improvements in the health, quality of life and survival of patients.
In 2008, Roche had over 80,000 employees worldwide and invested
almost 9 billion Swiss francs in R&D. The Group posted sales of 45.6
billion Swiss francs. Genentech, United States, is a wholly owned
member of the Roche Group. Roche has a majority stake in Chugai
Pharmaceutical, Japan. For more information: http://www.roche.com.
Forward-Looking Statements
This news release contains forward-looking statements within the
meaning of section 21E of the Securities Exchange Act of 1934, as
amended, that reflect the companies' judgments and involve risks and
uncertainties as of the date of this release, including without
limitation the statements related to anticipated product development
timelines. All forward-looking statements and other information
included in this press release are based on information available to
the companies as of the date hereof, and the companies assume no
obligation to update any such forward-looking statements or
information. Actual results could differ materially from those
described in the forward-looking statements.
Factors that could cause or contribute to such differences
include, but are not limited to, those discussed in detail under the
heading "Risk Factors" in the companies' most recent annual reports
on Form 10-K filed with the SEC and in other periodic reports filed
with the SEC. The risks and other factors discussed above should be
considered only in connection with the fully discussed risks and
other factors discussed in detail in the respective Forms 10-K and in
the companies' other periodic reports filed with the SEC, all of
which are available via their respective web sites at
http://www.intermune.com and http://www.pharmasset.com.
All trademarks used or mentioned in this release are protected by
law.
Additional information
-About Hepatitis, Roche Health Kiosk:
http://www.health-kiosk.ch/start_hepa.htm
-About Pegasys and Hepatitis:
http://www.roche.com/products/product-details.htm?type=product&id=86
- About INFORM-1: http://www.clinicaltrials.gov

Contact:

For further information, please contact: Roche: Mike Nelson,
International Communications Manager, Roche, +41-79-572-5165,
mike.nelson@roche.com. InterMune: Jim Goff, Sr. Director, Corp. Comm.
& IR, InterMune, Inc. +1-415-466-2228, jgoff@intermune.com.
Pharmasset: Richard E. T. Smith, Ph.D., VP, Investor Relations and
Corporate Communications, Pharmasset, +1-609-613-4181,
richard.smith@pharmasset.com.

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