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Roche Pharmaceuticals

Roche's R1626, First-in-Class Hepatitis C Polymerase Inhibitor, Demonstrates Impressive End-of-Treatment Response in Phase IIa Study

Basel, Switzerland (ots/PRNewswire)

- R1626 Also Shows a High Barrier to the Development of
Resistance
Roche's investigational treatment for hepatitis C, R1626, has
shown an impressive end-of-treatment response rate when given in
combination with PEGASYS(R) (peginterferon alfa-2a) and COPEGUS(R)
(ribavirin).
After 4 weeks of treatment with this triple combination, followed
by 44 weeks of Pegasys and Copegus, levels of the hepatitis C virus
(HCV) were undetectable in 84% of patients infected with genotype 1
virus. This was higher than in patients treated with Pegasys and
Copegus alone for the entire 48-week treatment period (65%).(1) These
new data were presented in a late-breaker oral session at the 43rd
Annual Meeting of the European Association for the Study of the Liver
(EASL), being held in Milan, Italy.
Discovered and developed at Roche, R1626 is a potent polymerase
inhibitor which belongs to a new generation of treatments that
directly inhibit replication of HCV. It is the most advanced
polymerase inhibitor in development.
"These results demonstrate that R1626 holds significant promise
to potentially increase the number of hepatitis C patients who can be
successfully treated. It is particularly interesting that R1626, a
polymerase inhibitor, is demonstrating a higher end-of-treatment
response rate than current HCV protease inhibitors in development,
together with a high barrier to the development of resistance," said
Dr David Nelson, Director of Hepatology and Liver Transplantation at
the University of Florida, Gainesville, Florida, USA. "Since most
patients responded very early in treatment with R1626, we expect
excellent SVR rates that improve significantly on those achieved with
the current standard of care. I look forward to SVR data from this
Phase IIa study, and to results of the ongoing Phase IIb study."
Patients in this Phase IIa study will be followed for an
additional 24 weeks with no treatment to determine the rate of
sustained virological response (SVR), indicating a cure.
Rapid development of R1626 - a Large Phase IIb Study is Now Fully
Enrolled
A large Phase IIb study with R1626 was initiated in November 2007
to define the optimal dose of R1626, in combination with Pegasys and
Copegus. This Phase IIb trial, called POLI 1, is now fully enrolled
with approximately 500 patients.
More About the Phase IIa Study and End-of-Treatment Results
Presented at EASL
The Phase IIa study is a multicenter trial that enrolled 104
patients with genotype 1 HCV, who had not previously received
treatment. Its primary endpoint was to evaluate the 4-week efficacy
and safety of combining R1626 with Pegasys alone or with Pegasys plus
Copegus, in comparison to a current HCV standard of care, Pegasys
plus Copegus.
Patients were randomised into the following treatment groups:
  • Group A: R1626 1,500 mg twice a day plus Pegasys 180 mcg weekly for 4 weeks
  • Group B: R1626 3,000 mg twice a day plus Pegasys 180 mcg weekly for 4 weeks
  • Group C: R1626 1,500 mg twice a day plus Pegasys 180 mcg weekly plus Copegus 1,000/1,200 mg daily for 4 weeks
  • Group D (standard of care group): Pegasys 180 mcg weekly plus Copegus 1,000/1,200 mg daily for 4 weeks
Following the 4 weeks of treatment in this study, all patients
received Pegasys 180 mcg weekly plus Copegus 1,000/1,200 mg daily for
an additional 44 weeks to complete the 48-week trial.
The study found(1):
  • Data collected at 4 weeks showed that patients receiving the triple combination (Group C) had a mean decrease in viral load of 5.2 log10 from baseline, indicating a robust and rapid virological response
  • At week 48, HCV was undetectable in 84% of patients receiving the triple combination R1626 1,500 mg BID + Pegasys + Copegus, compared with 65% of patients treated with Pegasys and Copegus alone
  • A higher incidence of grade 4 neutropaenia was reported in the R1626 treatment arms during the 4-week treatment period; however, after stopping treatment with R1626, absolute neutrophil counts returned to the levels typically seen with patients taking standard of care alone
R1626 - a High Barrier to the Development of Resistance
In a separate oral presentation at EASL, it was reported that
R1626 continues to present a high barrier to the development of viral
resistance. Resistance is a serious concern in hepatitis C treatment,
as resistant viruses have emerged in patients early on in treatment
with protease inhibitors. Resistance to R1626 has not been yet been
identified, after either 2 weeks of R1626 monotherapy, or after 4
weeks in patients treated with R1626 in combination therapy.(2)
About Hepatitis C
Hepatitis C, the most common chronic blood-borne infection, is
transmitted primarily through blood or blood products. Hepatitis C
chronically infects 180 million people worldwide, with an additional
three to four million people newly infected each year.(3) It is a
leading cause of cirrhosis, liver cancer and liver failure, despite
being potentially curable. The future of hepatitis C therapy is
likely to involve combinations of new small-molecule antiviral drugs
and pegylated interferon-based treatment, such as Pegasys.
About Roche
Headquartered in Basel, Switzerland, Roche is one of the world's
leading research-focused healthcare groups in the fields of
pharmaceuticals and diagnostics. As the world's biggest biotech
company and an innovator of products and services for the early
detection, prevention, diagnosis and treatment of diseases, the Group
contributes on a broad range of fronts to improving people's health
and quality of life. Roche is the world leader in in-vitro
diagnostics and drugs for cancer and transplantation, a market leader
in virology and active in other major therapeutic areas such as
autoimmune diseases, inflammation, metabolic disorders and diseases
of the central nervous system. In 2007 sales by the Pharmaceuticals
Division totalled 36.8 billion Swiss francs, and the Diagnostics
Division posted sales of 9.3 billion Swiss francs. Roche has R&D
agreements and strategic alliances with numerous partners, including
majority ownership interests in Genentech and Chugai, and invested
over 8 billion Swiss francs in R&D in 2007. Worldwide, the Group
employs about 79,000 people. Additional information is available on
the Internet at http://www.roche.com.
All trademarks used or mentioned in this release are protected by
law.
References:
(1). Nelson D, Pockros P, Godofsky E, et al. 84% end-of-treatment
response (EOTR, week 48) achieved with R1626, peginterferon alfa 2a
(40KD) and ribavirin for 4 weeks followed by the standard of care:
Results of a phase 2a study in treatment-naive HCV genotype 1
patients. In: 43rd Annual Meeting of the European Association for the
Study of the Liver (EASL); 2008 April 26, 2008; Milan, Italy; 2008.
(2). Le Pogam S, Seshaadri A, Kang H, et al. Low level of
resistance, low viral fitness and absence of resistance mutations in
baseline quasispecies may contribute to high barrier to R1626
resistance in vivo. In: 43rd Annual Meeting of the European
Association for the Study of the Liver (EASL); 2008; Milan, Italy;
2008.
(3). World Health Organization. Initiative for Vaccine Research,
Viral Cancers, Hepatitis C. 2006. (Accessed July 24, 2006, at http://
www.who.int/vaccine_research/diseases/viral_cancers/en/index2.html.)

Contact:

Contact: Mike Nelson, Roche, +41-79-572-5165, Michelle Marchione,
Axon Communications, +44(0)208-439-9449

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