Repros' IND for Proellex-V Accepted By the FDA

Repros Therapeutics Inc.®

today announced its Investigational New Drug Application for Proellex-V, or vaginally delivered Proellex, has been accepted by the FDA. The indication identified in the new IND is for the use of Proellex-V for the purpose of significant fibroid size reduction and symptom elimination with the goal of avoiding surgery. Approximately twenty percent of women of reproductive age in the U.S. have symptomatic fibroids with roughly 300,000 hysterectomies performed annually as a consequence. There is no approved chronic drug therapy for treatment of this debilitating condition. Within the IND, the Company submitted animal model data that suggest vaginally administered doses of Proellex-V will exhibit profoundly greater anti-proliferative effects on tissues that respond to progesterone stimulation than oral Proellex administration. In addition, vaginal administration reduces systemic exposure to a small fraction of that seen with oral administration, and thereby avoids the first pass liver effects that were an issue with the highest dose, 50 mg, of the oral formulation. In animal studies, vaginal administration resulted in maximum exposure levels roughly 1/6th of that achieved with the same oral dose. At the same time, anti-proliferative effects were more than 4 times that of the equivalent oral dose. As part of the IND, the Company submitted data from a completed rabbit vaginal irritation study using the highest dose anticipated in human studies and in the final dosage format in which no irritation was observed.