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Epigenesis Pharmaceuticals is a privately held biopharmaceutical company
developing inhaled respiratory medicines for the treatment of asthma and
chronic obstructive pulmonary disease (COPD). Epigenesis is focused on inhaled
delivery to leverage the enhanced safety profile of topical therapy over
systemic therapy. The Company’s lead compound, EPI-12323, is a once
daily, small molecule, inhaled non-glucocorticoid steroid that targets the
inflammatory and airway obstruction cascade in the irritated lung.
EPI-12323 has broad anti-inflammatory and bronchodilator activities, and
does not exhibit any of the classical side effects of glucocorticoid
steroids, that comprise 30% of all current asthma sales.
Respiratory disease represents one of the most attractive pharmaceutical
sectors, with sales expected to grow from the current $35 billion in 2009
to an estimated $65 billion in 2014. Asthma and chronic obstructive
pulmonary disease (COPD) represent 40% and 16% of the respiratory market,
respectively, and are the initial indications in development by Epigenesis.
Allergic rhinitis represents 25% of the respiratory market, and Epigenesis
is planning to target this indication in the near future.
Our initial target disease, asthma, has been called a national epidemic and
COPD is the fourth leading cause of death worldwide and is expected to be
the third leading cause by 2020. It is estimated that 16 million Americans
have COPD and an equal number are undiagnosed. Allergic rhinitis is also
growing at alarming rates, especially in children. The need for a new
generation of respiratory therapeutics is both great and growing.
 In spite of the
escalating medical need, only two new therapeutic classes of medicines have
been introduced into the marketplace over the past 25 years. We are
committed to improving this situation for all patients with common
respiratory disease. Epigenesis is creating a series of medicines for the
treatment of respiratory diseases through small molecule discovery methods.
Our business model is to streamline early clinical development through
Phase II studies and then partner our compounds with global pharmaceutical
companies. Part of the Company's strategy is to use sophisticated preclinical
models to select only those compounds that have the best chance of clinical
and commercial success. We create value for our shareholders by maximizing
the opportunity for each drug and by reducing risk in clinical development.
With our expertise in respiratory medicine and respiratory pharmaceutics,
we are able to streamline early clinical development. Our current lead
compound, EPI-12323, emerged from a small molecule discovery method that
targets asthmatic pathways.
The Company is committed to developing a series of inhaled respiratory
medicines through Phase II studies using small molecule discovery methods.
Initial clinical results indicate that EPI-12323 has pronounced
anti-inflammatory and bronchodilator activity and does not exhibit any of
the classical side effects of glucocorticoid steroids. EPI-12323 does not
bind to the glucocorticoid receptor and no adverse effects have been
observed on cortisol, bone or androgenic metabolism. In addition, EPI-12323
is effective in reducing airway inflammation and improving airways
resistance and compliance and reducing hyperresponsiveness in three
preclinical models.
EPI-12323 was identified as a candidate for development in asthma since it
is a non-glucocorticoid steroid and due to its ability to delete adenosine
pools believed to be important in asthma. EPI-12323 has demonstrated
anti-asthma effects in three separate preclinical models of human asthma.
Such an extensive evaluation is a part of the Company's strategy to use
sophisticated preclinical models to select only those compounds that have
the best chance of clinical and commercial success.
The pharmacology profile for EPI-12323 compares favorably to glucocorticoid
steroids, and in some cases exceeds the market leading corticosteroid
class. Specifically, EPI-12323 exhibits a long duration of action (perhaps
once per day treatment) and a pronounced effect on neutrophils. Neutrophils
are believed to play an important role in severe asthma cases that result
in death, and are also a key effector cell in COPD.
EPI-12323
administered once daily has been studied in hundreds of patients having
mild to severe asthma and COPD and has shown an excellent safety profile in
all clinical studies, with no adverse effects observed
on cortisol, bone or androgenic metabolism. EPI-12323 has shown efficacy in an
allergen challenge study and clinical improvement in FEV1 over 4-weeks in
mild to moderate asthma.
EPI-12323 produced a clinical improvement in FEV1 over 9-weeks in moderate
to severe COPD.
In
a recent Phase 2 clinical study in 271 symptomatic moderate to severe asthmatics using a
high efficiency nebulizer device, EPI-12323 administered once daily showed
statistically and clinically meaningful improvement in a validated asthma control questionnaire (ACQ)
versus placebo at 6-weeks, and in the average change in ACQ score. Further, significantly more
responders were in the EPI-12323 group than in the placebo group. Improvement trends were also noted
in rescue beta-agonist use and in the overall asthma symptom score. In this study, patients were being treated with high dose ICS
and long-acting beta-agonist (LABA), and during a five-week run-in period,
the patient’s high dose ICS was reduced in two steps by 80% while continuing
a constant LABA dose. Patients
were randomized to either EPI-12323 or the vehicle control for 6-weeks,
while continuing on a low dose of ICS and LABA. EPI-12323 showed
statistically and clinically meaningful improvement in patient’s ACQ
score while on low dose ICS and LABA.
As a result of EPI-12323's ability to decrease both eosinophilic and
neutrophilic inflammation in the lungs, it is also being developed for
COPD. By specifically targeting the neutrophilic inflammation, EPI-12323 is
expected to reduce the ongoing tissue destruction and improve small airway
obstruction in COPD.
The successful development of EPI-12323 as a single agent
opens the opportunity to combine it with other known effective agents in
asthma, COPD and other respiratory disorders to maximize the
compound’s value. Therefore, EPI-12323 is currently being developed
in combination with other drug classes for both asthma and COPD. Using one
device to deliver two medications permits customization of the drug
combination for individual patient symptoms and offers convenience. For
COPD patients, the ability to customize therapy represents a novel approach
to a very heterogeneous disease. Epigenesis has completed preclinical
pharmacology studies combining EPI-12323 with a long acting beta agonist as
well as other drug classes, and has filed patent applications for these combinations.
Our expertise in respiratory medicine and respiratory pharmaceutics enables
us to streamline early clinical development thereby saving valuable time
and resources.
The Company has a strong portfolio of patents, trademarks and trade secrets
that provides strong protection for its therapeutic approach. Epigenesis
has strong intellectual property barriers protecting its advanced
proprietary preclinical models of human respiratory disease, its compounds
(i.e. EPI-12323), and specific product formulations for the treatment of
respiratory diseases.
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