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An orally administered gonadotropin-releasing hormone antagonist1


See how ORILISSA works


ORILISSA is a GnRH receptor antagonist available in 2 oral dosages

ORILISSA competes with endogenous gonadotropin-releasing hormone (GnRH) for GnRH receptor occupancy and blocks receptors upon binding1,2

  • ORILISSA is a GnRH receptor antagonist available in 2 oral dosages
  • ORILISSA competitively binds to GnRH receptors
  • As a GnRH antagonist, ORILISSA binds without stimulating the receptors
ORILISSA is a GnRH-receptor antagonist

GnRH-receptor antagonism1,2

  • When ORILISSA enters the pituitary, it acts like a player in a game of musical chairs, competing with GnRH to sit in the receptor
  • Like a molecular game of musical chairs, GnRH is left with fewer receptors to activate
dose-dependent suppression of LH and FSH

Suppression of Luteinizing Hormone (LH) and Follicle-Stimulating Hormone (FSH) in a dose-dependent manner1-5

  • GnRH receptor antagonism leads to a dose-dependent suppression of LH and FSH
  • Starting at 4-6 hours after administration of a single dose of ORILISSA, a decline in LH and FSH can be seen*

*Does not imply onset of efficacy during this time.

dose-dependent suppression of estradiol

Decreased levels of estradiol and progesterone1,3,5

  • After approximately 24 hours, subsequent suppression of estradiol levels occurs*
  • The degree of suppression is dependent on the dose of ORILISSA


*Does not imply onset of efficacy during this time.


Watch the role of estrogen in endometriosis and the mechanism of action of ORILISSA.