Endometriosis is a disease characterized by endometrial tissue, which normally lines the uterus, growing outside the uterus usually elsewhere in the abdominal cavity. These extra-uterine growths swell and shed with the menstrual cycle just like normal endometrial tissue, but because they are located outside of the uterus, they cannot be excreted. This leads to pain and infertility, among other symptoms.
Treatments for endometriosis
There is currently no cure for endometriosis, but there are treatments available that can ease the symptoms. Many patients benefit from hormonal birth control, which can ensure the endometrial tissue does not swell by controlling the amount of estrogen and progesterone present, greatly reducing pain and inflammation.
Gonadotropin-releasing hormone (GnRH) receptor antagonists are another class of hormonal treatments that can be used to treat endometriosis.
How do GnRH receptor antagonists work?
GnRH receptor antagonists are chemicals that are structurally similar to GnRH. They bind to the GnRH receptor in the hypothalamus (the area of the brain considered the hormone “master switch”) and prevent the receptor from signaling to the ovaries to release estrogen. This means that the endometrial tissue, both inside and outside the uterus becomes quiescent — they do not swell or shed. It also means that no egg is released from the ovaries.
GnRH receptor antagonists can greatly reduce the pain that endometriosis patients experience.
Examples of GnRH receptor antagonists used to treat endometriosis
Orilissa (elagolix) is the only GnRH receptor antagonist that is approved to treat pain in endometriosis.
Experimental GnRH receptor antagonists currently being studied in trials to treat pain in endometriosis include linzagolix and relugolix.
Other GnRH receptor antagonists that are used off-label to treat endometriosis include Cetrotide (cetrorelix) and Antagon (ganirelix acetate).
Other information
GnRH antagonists can cause side effects such as nausea, headache, stomach pain, bloating, and rapid weight gain.
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