SOURCE: Biolex Therapeutics
November 06, 2007 01:45 ET
Biolex Therapeutics Researchers Present Locteron™ Phase 2a Hepatitis C Trial Results at AASLD Conference
Phase 2a Trial Demonstrates Statistically Significant Dose Response
PITTSBORO, NC--(Marketwire - November 6, 2007) - Biolex Therapeutics, Inc. today announced
that the results from its SELECT-1 Phase 2a clinical trial of Locteron™
will be presented today at the 58th Annual Meeting of the American
Association for the Study of Liver Diseases (AASLD). SELECT-1 was a
twelve-week trial designed to evaluate four doses of Locteron administered
once every two weeks in combination with the antiviral drug ribavirin.
Viral kinetic modeling of the SELECT-1 results by Eva Herrmann, Ph.D. and
Stefan Zeuzem, M.D. of Saarland University Hospital, Homburg/Saar, Germany,
demonstrated a statistically significant dose response. The study results
also suggested that patients receiving Locteron experienced side effects
that were less frequent and less severe than those previously reported in
clinical trials for the currently marketed pegylated interferons and for
Albuferon®, a product candidate currently under development. Biolex is
co-developing Locteron with its partner OctoPlus N.V.
As a controlled-release interferon alfa, Locteron is designed to improve
patient care through a more favorable side-effect profile and more
convenient patient dosing compared to existing pegylated interferon
products and Albuferon (albumin-fused interferon), each of which lack a
controlled-release mechanism. SELECT-1 (Safety and Efficacy of Locteron:
European Clinical Trial-1) was designed to evaluate four different doses of
Locteron, 160, 320, 480 and 640 micrograms (µg), administered once every
two weeks in combination with ribavirin administered orally twice per day
in 32 treatment-naïve hepatitis C patients with the genotype-1 variant of
Anti-viral results for SELECT-1 were as follows:
-- A clear dose response was observed in the study, and viral kinetic
modeling by Drs. Herrmann and Zeuzem demonstrated a statistically
significant HCV RNA reduction during the entire 12-week treatment period.
Specifically the dose effect was associated with mean and maximal anti-
viral efficiency of Locteron (p=0.003 and p=0.006, respectively; Jonckheere-
-- Average viral reduction after 12 weeks of treatment was greater than
four logs for each of the 640, 480 and 320 µg doses, compared to 1.8 logs
for the lowest dose of 160 µg.
-- The percentage of patients who achieved early virologic response
(EVR), defined as at least a two-log reduction in hepatitis C virus, was
100% in the 640 and 480 µg dose cohorts and 88% in the 320 µg dose cohort,
compared to 37.5% in the 160 µg dose cohort. The results compare favorably
with results previously reported in clinical trials for the currently
marketed pegylated interferon alfa products and for Albuferon for which EVR
rates ranging from approximately 74% to 90% in clinical trials have been
Locteron side effect and patient tolerability results in SELECT-1 were as
-- Locteron was well tolerated at all doses.
-- There were no serious adverse events in the 160 µg, 320 µg, and 480 µg
cohorts. There was one serious adverse event in the 640 µg cohort, a case
of otitis, or inflammation of the ear, which completely resolved.
-- The vast majority (over 90%) of the adverse events that were
experienced were rated as mild.
The majority of the side effects experienced by patients treated with
Locteron in the SELECT-1 study appear to be less frequent and less severe
than the side effects reported in previous clinical trials for pegylated
interferons and Albuferon. For example, only one patient (3%) in the
SELECT-1 study receiving Locteron experienced a clinical adverse event
rated as severe, indicating an improvement over previously reported
incidences of 14% and 18% in clinical trials for Pegasys® and Albuferon,
respectively. In addition, serious adverse events in SELECT-1 were limited
to the one aforementioned event occurring in the highest, 640 µg, Locteron
Injection site reactions were reported in 41% of the patients in SELECT-1.
All injection site reactions were mild with the exception of one patient in
the 640 µg cohort who had a reaction rated as moderate. The SELECT-1
results are within the range of the incidence of injection site reactions
reported in clinical trials of Intron®-A, PEG-Intron® and Pegasys of
49%, 75% and 22%, respectively.
Locteron combines BLX-883, a recombinant interferon alfa produced by Biolex
in its patented LEX System(SM), with PolyActive™, an advanced
controlled-release drug delivery technology developed by OctoPlus.
Locteron is the only controlled-release interferon alfa known to be in
Phase 2 clinical development for the treatment of hepatitis C and is
designed to improve patient care through a more favorable side-effect
profile and more convenient patient dosing. Locteron is configured to
allow dosing once every two weeks, an improvement in patient convenience
compared to currently marketed pegylated interferon alfa products that
require dosing every week. More importantly, Locteron's controlled-release
mechanism results in the gradual release of interferon alfa to patients
over the duration of two weeks. This controlled-release mechanism is
designed to cover inter-dose troughs while reducing the frequency, duration
and severity of side effects, including flu-like symptoms, commonly
experienced by patients treated with currently marketed pegylated
interferons and with Albuferon.
Biolex and OctoPlus plan to commence SELECT-2, a Phase 2b trial of Locteron
in 2008. The 12-week results of the Phase 2b trial will be used as the
basis for dose selection for the commencement of the Phase 3 development
program. 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.
About Biolex Therapeutics
Biolex is a clinical-stage biopharmaceutical company that uses its patented
LEX System(SM) to develop hard-to-make therapeutic proteins and to optimize
monoclonal antibodies. The LEX System is a novel technology that
genetically transforms the aquatic plant Lemna to enable the production of
biologic product candidates. The company's product candidates are designed
to provide superior efficacy/tolerability profiles and to address large,
proven pharmaceutical markets. Biolex's lead product candidate,
Locteron™, under joint development with OctoPlus N.V., is in Phase 2
clinical trials and is the only controlled-release interferon alfa known to
be currently in clinical development for the treatment of chronic hepatitis
C. Biolex has also developed two other product candidates that capitalize
on the benefits of the LEX System, which it is advancing toward clinical
trials: BLX-155, a direct-acting thrombolytic designed to dissolve blood
clots in patients; and BLX-301, an anti-CD20 antibody it is optimizing for
the treatment of non-Hodgkin's B-cell lymphoma and other diseases.