MONTREAL--(Marketwire - December 22, 2008) - TOPIGEN Pharmaceuticals Inc., a clinical-stage
biopharmaceutical company focused in respiratory disorders, today announced
that it has received a clinical trial approval (CTA) letter to move TPI
1100, a drug candidate for the treatment of chronic obstructive pulmonary
disease (COPD), into clinical development in 2009. TPI 1100 is a novel,
inhaled inhibitor against phosphodiesterases (PDEs), PDE 4 and PDE 7. PDEs
are a group of enzymes that are validated targets for COPD.
In related news, TOPIGEN announced that it has reprioritized its pipeline
candidates for COPD and will fund further development of TPI 1100 after
determining that it is a more promising candidate for COPD than TPI 1020.
This follows the results of a Phase II study that was recently completed
for TPI 1020 in patients with COPD, which showed good safety and
tolerability, but did not demonstrate the desired activity profile. TPI
1020 is a novel, anti-inflammatory respiratory drug licensed from NicOx
S.A. for respiratory indications. Potential opportunities for TPI 1020 in
other indications are currently being explored by NicOx and TOPIGEN under
the ongoing collaboration agreement.
Mark Parry-Billings, Chief Executive Officer of TOPIGEN, commented, "PDE
inhibition is a very exciting area with great potential in fighting
inflammatory respiratory diseases. With regulatory approval to evaluate
TPI 1100 in the clinic, we look forward to moving this product candidate
through development. Our decision to not invest further in TPI 1020 for
COPD reflects the systematic approach TOPIGEN will continue to take in
focusing resources on the development programs with the greatest chance of
achieving clear differentiation and value in the respiratory market. The
Company remains committed to the treatment of COPD, which is estimated to
affect 30 million people in the United States, Europe and Asia."
About TPI 1100
TPI 1100 is a novel, potent, selective and dual-acting RNA-silencing
oligonucleotide against phosphodiesterase isoforms PDE4 and PDE7. The drug
is designed to inhibit multiple gene expression pathways known to be linked
to progressive airway inflammation and remodeling in COPD. Delivered
topically via aerosol to the lungs and without the need for specialized
formulation technologies, TPI 1100 represents a novel RNA-silencing therapy
with a highly selective mechanism for reducing lung inflammation and is
expected to be without the dose-limiting systemic side effects widely
associated with known small molecule inhibitors. The drug utilizes
TOPIGEN's proprietary FANA™ Technology, a new generation of
oligonucleotide chemistry with potential for broad gene-targeting drug
In May 2008, TOPIGEN representative Marylène Fortin, Ph.D., presented an
abstract on TPI 1100 at the American Thoracic Society's 2008 International
Conference, in Toronto, Canada, titled "TPI 1100: an inhaled antisense
oligonucleotide (AON) against Phosphodiesterase (PDE) 4 and 7 with
significant anti-inflammatory effects in a mouse model for COPD." In this
presentation, TPI 1100 was compared with roflumilast, an orally active PDE
4 inhibitor. TPI 1100 was shown to reduce PDE 4B, 4D and 7A mRNA
expression in cells from lung lavage and inhibited neutrophil recruitment.
Moreover, TPI 1100 blocked the induction of the pro-inflammatory chemokines
KC, MIP-2 and MIP-1alpha. In contrast, the effect of roflumilast on
neutrophil recruitment was minimal, and no inhibition of chemokines was
observed. For more information or for a copy of the abstract, please visit
COPD is a disease characterized by persistent airflow limitation in the
lungs. Today, it is the fourth leading cause of death in the U.S., after
heart disease, cancer and cerebrovascular diseases, accounting for more
than 120,000 deaths annually. The cellular mechanisms that are responsible
for COPD pathology are not yet completely understood.
Chronic airflow limitation is believed to be a consequence of an abnormal
recruitment of inflammatory cells such as neutrophils (cells releasing
enzymes that destroy lung tissue) in response to cigarette smoke exposure.
Smoking is the most important risk factor associated with the development
of COPD. Acute exacerbations are the most common complication and a
contributor to associated morbidity and mortality. Although current
treatments improve quality of life and provide symptomatic relief in most
patients, there is a need for better drugs to slow the progressive decline
in lung function.
About NicOx S.A.
NicOx is a product-driven biopharmaceutical company dedicated to the
development of nitric oxide-donating drugs for unmet medical needs. NicOx
is targeting the therapeutic areas of inflammation and cardio-metabolic
disease. Headquartered in Sophia-Antipolis, France, NicOx is a public
company listed on the Eurolist of Euronext, Paris. For more detailed
information on NicOx, visit www.nicox.com.
TOPIGEN Pharmaceuticals is developing a clinical pipeline of innovative
therapeutics for respiratory diseases, including asthma and COPD. The
Company's unique, multi-targeted oligonucleotide product candidates have
compelling therapeutic profiles that address major unmet medical needs.
Topigen's business strategy is to advance products through clinical proof
of concept and out-license to partners for commercialization.