Relugolix combination therapy for treating endometriosis-associated pain

Relugolix in combination with estradiol and norethindrone is currently in clinical development for the treatment of endometriosis-associated pain. Endometriosis is a common, long-term gynaecological disorder where the tissue that normally lines the womb (endometrium) grows in other places. When this tissue breaks down as part of the normal menstrual cycle it becomes trapped in a woman’s pelvis. This can negatively impact the quality of life for women with the disease, as it results in painful periods (dysmenorrhea) and other endometriosis-associated pain. Currently there are no medicinal products approved specifically to cure endometriosis with most treatments directed at reducing the pain and reducing the severity of other associated symptoms.
Relugolix is co-administered with estradiol and norethindrone in the form of an oral tablet. Relugolix works by selectively binding to the gonadotrophin-releasing hormone (GnRH) receptor to block luteinizing hormone (LH) and follicle stimulating hormone (FSH) from binding to this receptor. This results in less production and release of oestrogen and progesterone by the ovaries so that menstruation is reduced. If licenced, relugolix combination therapy would be the first GnRH antagonist approved for the treatment of endometriosis-associated pain.