relugolix/estradiol/norethindrone (Pending FDA Approval)

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Dosing & Uses

AdultPediatric

Uterine Fibroids

Pending FDA approval for symptoms (eg, heavy menstrual bleeding) associated with uterine fibroids

Endometriosis

Pending FDA approval for symptoms (eg, pain) associated with endometriosis

Safety and efficacy not established

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Pharmacology

Mechanism of Action

Relugolix

  • Gonadotropin-releasing hormone (GnRH) receptor antagonist; binds to and blocks GnRH receptors in the anterior pituitary gland
  • Blocking GnRH receptors decreases the release of gonadotropins (ie, luteinizing hormone, follicle-stimulating hormone), thereby decreasing the downstream production of estrogen and progesterone by the ovaries in women

Estradiol and norethindrone

  • Maintains estrogen and progesterone in the low normal range to balance relugolix, while also maintaining bone health and mitigating side effects that can result from a low-estrogen state
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Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.