Repros Completes Enrollment in Three Androxal Studies

Repros Therapeutics Inc. RPRX today announced it believes that enough patients have enrolled in each of its three ongoing Androxal studies to provide statistically meaningful results for each trial. The Company expects to report top-line data for the three trials at the end of 2011. The three Androxal clinical studies are ZA-202, ZA-203 and ZA-204. ZA-202: a 3-month, 3-arm double blind placebo controlled Phase 2b study designed to assess the ability of Androxal to improve glycemic control in type 2 diabetic men currently on oral hypoglycemic agents as a result of the normalization of testicular function. To date, 115 subjects have been enrolled and randomized in the trial. Repros previously reported that Androxal achieved highly statistically significant improvement (p<0.00001) in testosterone levels compared to placebo in an interim analysis (n=61) of study ZA-202. In addition, a statistically significant (p=0.039) and clinically relevant reduction in HbA1c was observed for men taking Androxal vs. placebo in the subgroup of men that achieved morning testosterone levels > 450ng/dl. HbA1c is a common marker used to follow improvements in glycemic control in diabetic men across various therapies. Several studies conducted by others have failed to show signals for improved HbA1c when testosterone was administered to type 2 diabetic men in a hormone replacement therapy setting. ZA-203: a 3-month, 4-arm, Phase 2b study comparing two doses of Androxal to blinded placebo and open label Testim® in secondary hypogonadal men naive to testosterone treatment and who have been confirmed to exhibit a morning testosterone of <250 ng/dl. This study is being conducted per FDA recommendations, and should be useful for the Company to obtain a Special Protocol Assessment (SPA) for the design of subsequent Phase 3 registration studies of Androxal. The primary efficacy endpoint is the change in morning testosterone from baseline levels in the Androxal arms compared to placebo. Impacts on sperm counts are being evaluated for safety purposes. To date, 126 men have been enrolled and randomized into the study. At this time, 40 subjects have completed the three-month dosing period. Twenty-four subjects have also had their end of dosing sperm counts reported. Unaudited clinical labs and sperm counts have been assessed in this group. As a reminder, the Testim arm is open label, therefore, we can report those results. In the Testim arm, the average morning testosterone level after three months of treatment is 443 ng/dl. Of the 8 men that have had their end of dosing sperm counts assessed, 4 that previously exhibited normal levels dropped below the World Health Organization's (WHO) normal reference concentration of 20 million sperm per milliliter. One subject that was below baseline improved and the other three remained normal. One of the men that maintained a normal sperm concentration did not achieve a morning testosterone level > 300 ng/dl (the generally accepted lower limit of normal). Six of 8 of the men in the blinded group exhibited elevations in Luteinizing hormone (LH) after dosing had normal sperm counts at the start of the study. That number was improved to 7 of 8 after the three month dosing period. In the group of men that did not exhibit an increase in LH, 6 of 8 were normal at baseline (one subject who was at the 20 million level at baseline decreased to below the cutoff) and 5 of 8 were normal at the end of blinded dosing.