Repros Therapeutics Inc. Provides Additional Information on Proellex Clinical Program

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Tue Jul 7, 2009 6:00am EDT

THE WOODLANDS, Texas--(Business Wire)--
Repros Therapeutics (NasdaqGM:RPRX) provides a further update on the clinical
development of Proellex 25 and 12.5 mg doses. 

Repros` recent decision to discontinue the use of the Proellex 50 mg dose in its
ongoing clinical studies was based on observations of a dose-related increase in
liver enzymes in a low percentage of women. The company believes that the 25 mg
and 12.5 mg doses will offer comparable efficacy benefits while providing an
improved safety profile. 

The overall clinical development program for Proellex includes numerous
pharmacokinetic, pharmacodynamic, Phase I, Phase II, and ongoing Phase III
clinical trials. These studies used doses of Proellex ranging from 3 mg up to
200 mg daily. From completed studies as well as from an ongoing large open label
trial, it has been determined that the drug appears to be well tolerated. 

Most drugs are predominantly metabolized in the liver, as is Proellex. Repros
has paid particular attention in all ongoing and completed trials to detect any
change in liver enzymes in women taking Proellex. Frequent monitoring of liver
enzymes has allowed the early detection of increases at or above a level where
the treatment with Proellex would have to be discontinued. This level was set in
the clinical trials at an increase in liver aminotransferases (ALT; AST) greater
than, or equal to three times the Upper Level of Normal (≥ 3 x ULN). 

The following data were observed in 470 women treated with Proellex through June
2009 (n values may vary slightly due to randomization):

 Proellex     Subjects Exposed At Various Doses     Number of Subjects Discontinuing Treatment due to Aminotransferases     Percent of Women Discontinuing Treatment due to Aminotransferases   
 
Dose        
> 1 Month                            
≥ 3 x ULN                                                              
≥ 3 x ULN                                                          
 
(mg)                                                                                                                                                                                          
 12.5         N = 55                                0                                                                       0 %                                                                 
 25           N = 225                               1                                                                       0.4 %                                                               
 50           N = 190                               9                                                                       4.7 %                                                               


The above listed elevations all occurred in the first four months of treatment
and resolved without intervention upon discontinuation of product. No elevations
have been observed in studies with subjects treated for multiple four month
treatment periods. Additionally, the one subject in the chart above on the 25 mg
dose, which case was noted and reported 2 years ago, also showed a positive ANA
titer, which may have been a pre-existing condition. The ANA (antinuclear
antibody) test helps diagnose autoimmune diseases, such as rheumatoid arthritis
and lupus, but can also be positive in people with other diseases, as well as
linked to use of certain medications. 

Completed studies at 25 and 12.5 mg doses have demonstrated statistically and
clinically significant control of excessive menstrual bleeding and improvement
in quality of life parameters. In a completed Phase II study, which included 127
women with uterine fibroids, doses of 25 and 12.5 mg were compared to placebo
for a period of three months. Both the 25 and 12.5 mg doses showed statistically
significant (p < 0.0001) improvements in three clinically relevant endpoints:
hemoglobin level, menstrual bleeding scores and quality of life parameters. 

Repros believes that the decision to move forward with the 25 and 12.5 mg doses
will improve the benefit/risk profile of Proellex. Additionally, Repros believes
that any new studies required for the approval of the 12.5 mg dose will not
adversely impact anticipated timing of NDAs for Proellex. 

"Drug development is a dynamic process, the aim of which is to try and bring to
market a product with an optimal balance between benefits and risks that will
address an unmet medical need in patients. Our decision to stop the 50 mg dose
supports this concept, as well as demonstrates our commitment to safeguarding
the well-being of the women participating in our clinical trials," stated Dr.
Paul Lammers, President of Repros Therapeutics. 

About Repros Therapeutics

Repros Therapeutics focuses on the development of oral small molecule drugs for
major unmet medical needs that treat male and female reproductive disorders. 

Our lead drug, Proellex, is a selective blocker of the progesterone receptor and
is being developed for the treatment of symptoms associated with uterine
fibroids and endometriosis. We are also developing Proellex as a short course
pre-surgical treatment for anemia associated with excessive menstrual bleeding
related to uterine fibroids. There is no currently approved effective long-term
orally administered drug treatment for uterine fibroids or endometriosis. In the
United States alone, 300,000 women per year undergo a hysterectomy as a result
of severe uterine fibroids. 

Our second product candidate, Androxal, is a single isomer of clomiphene citrate
and is an orally active proprietary small molecule compound. We are developing
Androxal for men of reproductive age with low testosterone levels who want to
improve or maintain their fertility and/or sperm function while being treated
for low testosterone. In November 2008, we received guidance from the FDA
suggesting submission of a new IND to the Division of Metabolic and Endocrine
Products, or DMEP, for the investigation of Androxal as a potential treatment
for type 2 diabetes. We plan to submit a new IND for this indication to the DMEP
as soon as practicable. 

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 success in the clinical development of its technologies,
the timing of enrollment and release of data in such clinical studies and the
accuracy of such studies, the timing of submission of NDAs, limited patient
populations of clinical studies to date and the possibility that final data may
not be consistent with interim data, Repros' ability to raise additional capital
in a timely manner and on acceptable terms or at all 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. 



Repros Therapeutics
Dr. Paul Lammers, President, 713-294-2380 

Copyright Business Wire 2009

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