Euroscreen Announces Positive Completion of Phase I Trial of ESN364

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ESN364 is safe and well-tolerated with high oral bioavailability and a linear pharmacokinetic profile. The drug candidate demonstrated clear pharmacodynamics and efficacy based upon reduction of relevant hormone biomarkers.

Euroscreen SA announced today the final results from a Phase I clinical trial evaluating the safety and confirming the activity of ESN364, its proprietary, oral, small-molecule antagonist of the NK3 receptor.

"Phase I results are fully-consistent with our expectations based on the safety, pharmacokinetic and efficacy data that we had obtained with ESN364 in preclinical studies. These convincing results, together with the strong recommendation from our Clinical Advisory Board, support our decision to initiate Phase II proof-of-concept studies. We will start two Phase II trials (3-month dosing, 72 patients) for Uterine Fibroids (UF) and Poly Cystic Ovarian Syndrome (PCOS) in January 2015" stated Steven Ramael, M.D., Medical Director. "ESN364 modulates LH, estradiol and progesterone in healthy volunteers without affecting FSH. These data give us a strong competitive advantage compared to GnRH ligand products to provide a superior product with regard to both safety and efficacy for a large scope of indications such as UF, PCOS and Endometriosis in the treatment of Women’s Health.” said Jean Combalbert, Ph.D. Chief Executive Officer.

Study Design
The Phase I clinical trial of ESN364 was a randomized, double blind, placebo-controlled, single and multiple ascending dose study designed to evaluate the safety, pharmacokinetics and preliminary pharmacodynamics of ESN364 after single and repeated daily dose administration. A single ascending dose study phase was conducted in male volunteers whereas multiple-dose studies with sequential dose escalation were conducted in both male and female volunteers.

Study Results
The Phase I clinical trial enrolled 64 healthy subjects (40 male and 24 female). Safety was evaluated by means of intensive ECG and vital signs monitoring as well as via the necessary clinical laboratory assessments throughout the entire study (up to 21 days of daily dosing and up to 84 days of follow-up in female volunteers). No clinically relevant changes were observed in the clinical lab parameters, ECG and/or vital signs. The reported adverse events were mild-to-moderate in intensity, reversible and of limited duration and non-significant in relation to ESN364 treatment based upon comparison to the placebo group.

ESN364 is a proprietary, oral, small-molecule, discovered and optimized by Euroscreen. Our drug candidate is the first NK3 antagonist optimized for the purpose of the treatment of Women’s Health Disorders. Whereas competing GnRH ligand products block GnRH signaling entirely, NK3 antagonism merely decreases GnRH pulse frequency and thereby decreases LH pulse frequency but, importantly, without effecting FSH. The pharmacology of ESN364 to decrease LH pulse frequency uniquely positions this drug for the treatment of PCOS. In addition, the selective decrease in LH, but not FSH, reduces levels of the ovarian hormones estrogen and progesterone in a non-castrating manner as required for the safe, effective treatment of UF and Endometriosis.

About Euroscreen
Euroscreen S.A. is a Belgium-based, private, Drug Discovery and Development company providing first-in-class small molecule drug candidates for therapeutic areas including hormonal disorders, inflammation and neurodegenerative diseases.

Euroscreen has a drug discovery track-record with multiple innovative and proprietary small-molecules targeting GPCRs. Euroscreen has advanced its orally-available and highly specific lead program ESN364 into clinical development for the treatment of Women’s Health disorders. In addition, Euroscreen advances other small molecules (preclinical stage) targeting GPCRs of interest for unmet medical needs. Euroscreen is backed by leading investors, including Vesalius Biocapital, SRIW and Fortis Private Equity. Further information about Euroscreen and its drug discovery and development programs can be found online at or by contacting info(at)euroscreen(dot)com.

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