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The drug is the first NK3 antagonist which has been optimized for use in women’s health, and is being developed for sex-hormone related disorders such as endometriosis, polycystic ovarian syndrome and uterine fibroids.

  • ESN-364 is an oral available small molecule which, due to its unique mechanism of action, allows modulation of the hypothalamic-pituitary gonadal axis with a selective action on hormones relevant to disease. As such, the agent is expected to have greater tolerability than competing products which target GnRH.
  • In preclinical studies, superior potency and safety were seen when compared with competitors.
  • The European phase I trial was initiated in 64 healthy male and female volunteers in December 2013, and will assess safety, tolerability,
  • pharmacokinetics and hormone levels to evaluate on-target activity. Proof-of-concept phase II trials in patients with sex-hormone related disorders are planned for the fourth quarter of 2014.
  • Euroscreen estimates the combined endometriosis, uterine fibroid and polycystic ovarian syndrome therapeutic market will be valued at $3.6 billion by 2018.

Adapted from - Thomson Reuters Cortellis Competitive Intelligence

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