Relugolix, Estradiol, and Norethindrone Acetate
Class: Antigonadotropins
Chemical Name: 1-[4-[1-[(2,6-difluorophenyl)methyl]-5-[(dimethylamino)methyl]-3-(6-methoxypyridazin-3-yl)-2,4-dioxothieno[2,3-d]pyrimidin-6-yl]phenyl]-3-methoxyurea
Molecular Formula: C29H27F2N7O5SC18H24O2C22H28O3
CAS Number: 737789-87-6
Brands: Myfembree
Warning
WARNING: THROMBOEMBOLIC DISORDERS AND VASCULAR EVENTS
See full prescribing information for complete boxed warning
Estrogen and progestin combinations, including relugolix, estradiol, and norethindrone acetate, increase the risk of thrombotic or thromboembolic disorders, especially in women at increased risk for these events.
Relugolix, estradiol, and norethindrone acetate is contraindicated in women with current or a history of thrombotic or thromboembolic disorders and in women at increased risk for these events, including women over 35 years of age who smoke or women with uncontrolled hypertension.
Introduction
The combination of relugolix (a gonadotropin-releasing hormone [GnRH] receptor antagonist), estradiol (an estrogen), and norethindrone acetate (a progestin) decreases menstrual blood loss.
Uses for Relugolix, Estradiol, and Norethindrone Acetate
Relugolix, estradiol, and norethindrone acetate has the following uses:
Relugolix, estradiol, and norethindrone acetate is a combination of relugolix, a gonadotropin-releasing hormone (GnRH) receptor antagonist, estradiol, an estrogen, and norethindrone acetate, a progestin, and is indicated for the management of heavy menstrual bleeding associated with uterine leiomyomas (fibroids) in premenopausal women.
Relugolix, estradiol, and norethindrone acetate has the following limitations of use:
Use of relugolix, estradiol, and norethindrone acetate should be limited to 24 months due to the risk of continued bone loss, which may not be reversible.
Relugolix, Estradiol, and Norethindrone Acetate Dosage and Administration
General
Relugolix, estradiol, and norethindrone acetate is available in the following dosage form(s) and strength(s):
Tablets: fixed-dose combination containing relugolix 40 mg, estradiol 1 mg, and norethindrone acetate 0.5 mg
Dosage
It isessentialthat the manufacturer's labeling be consulted for more detailed information on dosage and administration of this drug. Dosage summary:
Adults
Dosage and Administration
Exclude pregnancy and discontinue hormonal contraceptives prior to relugolix, estradiol, and norethindrone acetate initiation.
Begin taking relugolix, estradiol, and norethindrone acetate as early as possible after the onset of menses, but no later than seven days after menses has started.
Take one tablet orally once daily at approximately the same time each day, with or without food.
If a dose of relugolix, estradiol, and norethindrone acetate is missed, take the missed dose as soon as possible the same day and then resume regular dosing the next day at the usual time.
Avoid concomitant use of relugolix, estradiol, and norethindrone acetate with oral P-gp inhibitors. If concomitant use of oral P-gp ...
