Attached files
| file | filename |
|---|---|
| 8-K - REPROS THERAPEUTICS INC. | v206703_8k.htm |
| EX-99.2 - REPROS THERAPEUTICS INC. | v206703_ex99-2.htm |
Exhibit
99.1
|
Contact:
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Repros
Therapeutics Inc.
|
Joseph
Podolski (281) 719-3447
President
and Chief Executive Officer
VAGINAL
DELIVERY OF REPROS’®
PROELLEX® BYPASSES
FIRST PASS LIVER EFFECTS AND ACHIEVES GREATER SIGNALS OF EFFICACY AT
SIGNIFICANTLY LOWER EXPOSURE
Company
plans to submit new IND to FDA pending vaginal irritation study
THE
WOODLANDS, Texas – December 27, 2010 – Repros Therapeutics Inc.®
(NasdaqCM:RPRX) today announced it has completed two animal model studies
of the use of Proellex® in a
vaginally administered formulation that demonstrated effects on progesterone
sensitive tissues equivalent to the highest oral dose formerly in development by
the Company. Most importantly, extrapolating the data from the
exposure seen in animals to that seen in humans, administration of Proellex via
the vaginal route may achieve maximum circulating concentrations that are
approximately 2% of that exhibited in humans at the 50 mg dose and only 6.5% of
the lowest oral dose, 12.5 mg, previously tested in humans.
The
Company believes the high concentrations of the active ingredient and its
primary metabolite attained in first pass absorption and processing by the liver
resulted in the delayed toxicity exhibited in roughly 3-4% of the women
administered the 50 mg dose of the drug in Phase III studies. At 12.5
mg there were no adverse liver toxicity signals different than
placebo. The maximum concentrations of parent and metabolite for the
12.5 mg dose were 25% of the 50 mg dose.
The
Company’s first animal study was conducted in dogs comparing a vaginal
formulation to the oral formulation used in the Repros
studies. Maximum circulating concentrations of the active ingredient
and the metabolite in the vaginal formulation were roughly 6.5% of the values
obtained via the oral route for the same dose of the drug.
To
determine whether these low circulating levels could have any impact predictive
of efficacy, the Company conducted a study in rabbits. The rabbit
study, known as the “anti-Clauberg” assay is used as a model to determine the
efficacy potential of drugs such as Proellex. The model was
originally used by the National Institute of Health in selecting the active
ingredient of Proellex as the lead compound from the family of molecules they
discovered and exclusively licensed to Repros. The data from the
study showed that vaginal delivery of Proellex exhibits four times the activity
of the same oral dose. Coupling the findings of the dog study with
this outcome suggests a highly efficacious and safe formulation of Proellex may
be developed. The Company is completing one more dose optimization
study in the rabbit and pending that outcome will conduct a vaginal irritation
study before requesting a pre-IND meeting with the FDA. The Company
plans to submit its findings for publication. A patent application is
pending that covers this technology. The formulation uses standard
pharmaceutical excipients that have previously shown to be devoid of properties
that would irritate the vagina.
Joseph S.
Podolski, President and CEO of Repros, commented, “The animal data is
impressive. If we can obtain agreement from the FDA to conduct a study of
vaginally administered Proellex in the second quarter of 2011, we can be in a
position to compare low dose oral administration to vaginal administration by
year end.” He further noted, “Though our Phase III studies of high
oral doses were stopped due to liver toxicity, the insight we gained from
conducting those studies is invaluable. We believe we will be able to
move to Phase III after we complete these studies pending favorable
outcomes.”
About
Repros Therapeutics Inc.
Repros
Therapeutics focuses on the development of oral small molecule drugs for major
unmet medical needs that treat male and female reproductive
disorders.
Any statements that are not
historical facts contained in this release are forward-looking statements that
involve risks and uncertainties, including Repros' ability to have the partial
hold on Proellex® lifted and to determine a safe and
effective dose for Proellex, raise needed additional capital on a
timely basis in order for it to continue to fund its operations and pursue its
development activities, and such other risks which are identified in the
Company's most recent Annual Report on Form 10-K and in any subsequent quarterly
reports on Form 10-Q. These documents are available on
request from Repros Therapeutics or at www.sec.gov. Repros disclaims any intention or
obligation to update or revise any forward-looking statements, whether as a
result of new information, future events or otherwise.
For more
information, please visit the Company's website at http://www.reprosrx.com.