Repros Updates Proellex Program

Repros Therapeutics Inc.®

today announced that it believes that topline results from all three of its ongoing Proellex® studies can be reported by the end of third quarter of 2016. Each of the three placebo controlled, double-blind studies has enrolled or will enroll approximately 45 subjects. Each study has a placebo arm and two drug arms, 6 and 12 mg Proellex®. The first reported component of the three studies will be after four months of continuous treatment followed by an off drug interval to allow for return of menses. An effective dose of Proellex® results in cessation of menses (amenorrhea) without any negative effects on bone mineral density. This criterion is based on data obtained from several earlier studies in both endometriosis and uterine fibroids. To date, both low dose oral and vaginal Proellex® have been generally well tolerated. Uterine Fibroids In previous low dose oral and vaginally administered Proellex® studies in the treatment of uterine fibroids, statistically significant outcomes for reduction in menstrual bleeding, general symptoms associated with uterine fibroids have been observed, as has clinically meaningful reduction in fibroid volume. The two ongoing studies for uterine fibroids include an assessment of blood loss via an alkaline hematin extraction from used sanitary products. Women effectively treated with Proellex® do not menstruate and hence have no sanitary products to analyze. Women on placebo will continue to menstruate. The two fibroid studies are designed to achieve statistical significance for key endpoints with a relatively small subject count. Endometriosis Previous studies with Proellex® at doses of 25 and 50 mg in women with severe endometriosis showed substantial reductions in both the associated pain and resulting analgesic usage. To date, the Company has enrolled 41 subjects in a low dose trial of both 6 and 12 mg Proellex® in women with severe endometriosis (Biberoglu Berman Symptom Survey Score > 7) and who require analgesics to control the associated pelvic abdominal pain. Based on results from an interim analysis of the data, women treated with placebo exhibited pain scores at the end of treatment that were 83% of baseline but showed no reduction in analgesic usage (100% of baseline). Women in the two active treatment groups exhibited clinically relevant reductions in both pain scores and analgesic usage. In this group, pain scores were 39% of baseline and analgesic usage was reduced to 23% of baseline. Both of these assessments achieved statistically significant reduction compared to baseline and achieved or approached significance compared to placebo. Based on this assessment the Company has decided to end enrollment of the endometriosis study, as it believes the study will provide sufficient data to design a Phase 3 study based on the 40-45 subjects expected to be randomized. Topline results from this study should be available by the end of the 3rd quarter of 2016. The Company plans to request meetings with the FDA at the appropriate time to determine the Phase 3 programs that will be required for NDAs for these two indications.