TherapeuticsMD, Inc. (NYSE MKT: TXMD), a women’s healthcare company ("TherapeuticsMD" or the "Company"), announced today the final PK results from two studies of TX 12-004-HR, a rapidly acting vaginal preparation capsule versus Novo Nordisk’s Vagifem ® (estradiol vaginal tablet). ESTR-1K-499 was an open label, single dose crossover, relative bioavailability study comparing 10µg of TX 12-004-HR to 10µg of Vagifem. ESTR-1K-500 was the study with the same design, but compared 25µg of TX 12-004-HR to 25µg of Vagifem. Study results showed substantially lower systemic estradiol exposure of TX 12-004-HR when compared to Vagifem. In conjunction with the previously reported efficacy of TX 12-004-HR, this PK data suggests that TX 12-004-HR may provide therapeutic advantages over Vagifem.
Side effects associated with vaginal hormone therapy may be related to peak concentrations or overall exposure to the hormones. The maximal concentration of TX 12-004-HR estradiol was about half that observed with Vagifem and the overall exposure to estradiol was approximately one-third that observed with Vagifem. The 24-hour exposure to estradiol in the case of 25µg dose of TX 12-004-HR was 3.3 fold lower than the same dose of Vagifem, and in the case of 10µg dose of TX 12-004-HR was 2.6 fold lower than the same dose of Vagifem. These results would indicate substantially less overall estradiol exposure with TX 12-004-HR, yet the biological effects shown in the pilot phase 1 study reported in October 2013 showed statistically significant results of quantitative endpoints, namely reduction of vaginal pH (p=0.0002) and reduction of vaginal parabasal cells (p<0.0001) and increase in vaginal superficial cells (p=0.0002).
Robert G. Finizio, Chief Executive Officer and Co-founder of TherapeuticsMD, said, “We are pleased that our drug candidate appears to have a lower systemic estradiol exposure while achieving statistically significant clinical efficacy. Our goal is to create a faster-acting, rapidly dissolving VagiCap with less systemic estradiol exposure in a more elegant form. These results will be used to design a development plan and a clinical program to be submitted to Food and Drug Administration ("FDA") for treatment of VVA in postmenopausal women. The VVA market is growing substantially due to increasing demands by maturing women who are remaining sexually active longer and finding dissatisfaction with current treatment options. We are committed to developing this drug candidate to offer women a significant advancement in treatment options and to meet their unmet needs,” concluded Finizio.