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 the virus.

SELECT-1 Results

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-
    Terpstra-test).
    
--  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
    reported.
    

Locteron side effect and patient tolerability results in SELECT-1 were as follows:

--  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 dose cohort.

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 Overview

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.

Contact Information

  • Contacts:
    Dale Sander
    Chief Financial Officer
    858-663-6993
    Email Contact

    158 Credle Street
    Pittsboro, NC 27312
    www.biolex.com
    tel 919.542.9901
    fax 919.542.9910