Locteron dosed once every two weeks demonstrated a comparable reduction in viral
load compared to once-weekly standard of care with 57% less flu-like adverse events
PITTSBORO, NORTH CAROLINA, April 16, 2010 - Biolex Therapeutics, Inc. announced
that interim results from EMPOWER, a prospectively designed analysis of results from two
Phase 2b trials of Locteron®, were presented yesterday in a late-breaker session at the 45th
Annual Meeting of the European Association for the Study of the Liver (EASL) in Vienna,
Austria. Locteron, controlled-release interferon alpha 2b, is designed to improve patient care
by providing a more convenient once-every-two week dosing schedule and by reducing the
flu-like symptoms associated with pegylated interferons, the current standard of care. In the
EMPOWER study, the 480 μg dose of Locteron demonstrated viral kinetics and response
rates that were comparable to the PEG-Intron® control while also achieving a 57% reduction
in flu-like adverse events.
The objective of the EMPOWER study was to test the hypothesis that the 480 ug dose of
Locteron dosed once every two weeks reduces flu-like symptoms but retains equivalent
efficacy compared to PEG-Intron (1.5 μg/kg, administered every week). The 133 patients in
the EMPOWER study were enrolled in two contributing Phase 2b trials:
• SELECT-2, a Phase 2b dose-finding trial evaluating the 320, 480 or 640 μg doses of
Locteron versus PEG-Intron. Interim results from SELECT-2 were also presented at
EASL yesterday. SELECT-2 contributed a total of 59 Locteron 480 μg and PEGIntron
patients to EMPOWER.
• The 480 STUDY, a Phase 2b trial evaluating the 480 μg dose of Locteron versus PEGIntron.
Interim results from the 480 STUDY will be presented in an oral presentation
at EASL later today. The 480 STUDY contributed 74 patients to EMPOWER.
All patients were treatment-naïve-genotype-1 subjects with chronic hepatitis C, and all
patients were also treated with weight-based ribavirin. A total of 30 sites participated in the
two trials (14 sites in the US, 11 in Europe, and five in Israel). All patients in EMPOWER
have completed at least six weeks of study, and over 80% of the patients have completed 12
weeks of study.
Through six weeks of treatment, Locteron 480 μg administered once every two weeks
demonstrated reductions in viral loads (mean changes in HCV RNA from baseline) that were
somewhat more rapid than that achieved with PEG-Intron administered once per week. Rates
of undetectable HCV RNA achieved after six weeks of treatment were 31% for Locteron 480μg and 19% for PEG-Intron. The currently available results after 12 weeks of treatment (a
number of patients have not yet reached the 12-week time point) suggest comparable
reductions in mean HCV RNA and rates of undetectable HCV RNA for Locteron 480 μg and
PEG-Intron.
In EMPOWER, flu-like adverse events were predefined to include arthralgia, chills, fever,
headache, and myalgia. A substantial reduction in flu-like adverse events for patients treated
with Locteron was evident even in the first week of the trial and continued through the 12-
week time point available for evaluation. After six weeks of treatment, total flu-like adverse
events reported for Locteron 480 μg were 52% less than the total events reported for PEGIntron.
Available results after 12 weeks of treatment suggest total flu-like adverse events
reported for Locteron 480 μg were 57% less than the total reported for PEG-Intron.
The EMPOWER results were presented by the lead author, Walker Long, MD, Chief Medical
Officer and Vice President, Drug Development, Biolex Therapeutics, in the form of a poster
titled “Q2Week Controlled-Release Interferon Alpha2b + Ribavirin Reduces Flu-like
Symptoms >50% and Provides Equivalent Efficacy in Comparison to Weekly Pegylated
Interferon Alpha2b + Ribavirin in Treatment-Naïve Genotype 1 Chronic Hepatitis C: Results
from EMPOWER, a Randomized Open-Label 12-week Comparison in 133 Patients.”
“The EMPOWER study allows us to focus on the activity associated with one specific dose of
Locteron and test our hypothesis that equivalent efficacy can be achieved while greatly
reducing flu-like adverse events,” said Dr. Long. “These results exceed our expectations. We
believe that the importance of reducing flu-like adverse events will grow with the advent of
direct-acting virals and the shortening of therapy, due to the prevalence of these side effects
during the first three months of treatment.”
Three serious adverse events were reported for Locteron 480 μg and three were reported for
PEG–Intron. All events were expected labeled events for interferon alpha. Higher rates of
mild or moderate (Grade 2 and Grade 3) reductions in measurements of white blood cell
counts, platelets and neutrophils were observed for Locteron 480 μg compared to PEG-Intron,
while higher rates of mild or moderate reductions in measurements of hemoglobin were
observed for PEG-Intron. There were no Grade 4 reductions in hematological measurements
for either Locteron 480 μg or for PEG-Intron. There were no novel toxicities identified in
either cohort of the trial.
Locteron is an investigational therapeutic candidate and has not been approved for sale by the
United States Food and Drug Administration or by any international regulatory agency.
Locteron Overview
Locteron is a controlled-release interferon alpha designed to improve patient care in the
treatment of hepatitis C through a more favorable side-effect profile and dosing convenience
compared to existing pegylated interferon products. In contrast to Locteron’s controlledrelease
mechanism, the currently approved products, Pegasys® and PEG-Intron, and the investigational product Zalbin™, are immediate-release products that lack a controlled-release
mechanism. Interferon alpha serves as the foundation of current combination therapy for
hepatitis C patients. It is estimated that worldwide sales of interferon products for the
treatment of hepatitis C will approach $6 billion by 2016.
Locteron incorporates an advanced controlled-release drug delivery technology that allows
dosing once every two weeks, more convenient than Pegasys and PEG-Intron, each of which
require dosing every week. More importantly, Locteron’s controlled-release mechanism
results in the gradual release of interferon alpha 2b to patients over the duration of two weeks
and avoids the early peak plasma levels of the active interferon that characterize the pegylated
interferons and Zalbin. This controlled-release mechanism is designed to reduce the
frequency, duration and severity of flu-like symptoms commonly experienced by patients
treated with pegylated interferons and with Zalbin.