Endometriosis is a painful disorder in which tissue similar to the lining inside the uterus (called “the endometrium”) grows outside of the uterus, where it induces a chronic inflammatory reaction that may result in scar tissue. The symptoms of endometriosis include significant pain that accompanies periods, ovulation, and sexual intercourse as well as heavy menstrual bleeding, chronic pelvic pain, fatigue and infertility. Endometriosis can also affect general physical, mental, and social well being.
An estimated 2.5 million women in the US have been diagnosed and are being treated for the painful and debilitating symptoms of endometriosis. However, available treatments fail to control the pain associated with the disease over the long term. The only approved class of treatments for endometriosis—gonadotropin-releasing hormone (GnRH) agonists—work by excessively suppressing estrogen/estradiol production, which may lead to bone mineral density loss or other adverse effects.
ObsEva is currently advancing OBE2109, a novel, orally administered GnRH receptor antagonist with a potentially best-in-class profile in late-stage clinical development for the treatment of endometriosis-associated pain. Linzagolix acts by binding to and blocking the GnRH receptor in the pituitary gland, ultimately dose-dependently reducing estrogen production by the ovaries. Through previously reported results from linzagolix and sophisticated pharmacological modelling, it has been established that maintaining estradiol within a specific target range provides the optimal balance between reducing symptoms while mitigating bone density loss associated with excessive estradiol suppression.
Oral GnRH receptor antagonist