Relugolix Risks and Safety Profile

Primary Hypoestrogenic Risks

The American College of Radiology recommends that relugolix as monotherapy causes significant hypoestrogenic effects, including hot flashes, headaches, hypertension, and bone mineral density loss, but when combined with low-dose estrogen and progestin (add-back therapy), these risks are substantially mitigated while maintaining therapeutic efficacy, in patients with fibroid-related heavy menstrual bleeding 1, 2
Combination treatment with low-dose estrogen and progestin (add-back therapy) minimizes bone mineral density loss over time and is FDA-approved for fibroid-related heavy menstrual bleeding, with a mean BMD decrease of 4.9% over 24 weeks, in patients receiving relugolix monotherapy 1, 2, 3

Headaches are a common hypoestrogenic effect, and hypertension can develop during treatment, with relugolix monotherapy, in patients with fibroid-related heavy menstrual bleeding 1, 2

Fertility is actively suppressed during relugolix treatment, though the medication is often chosen by patients interested in uterus-preserving therapy or future fertility preservation, according to Praxis Medical Insights 4

Cessation of therapy leads to rapid recurrence of symptoms, making relugolix unsuitable as a definitive long-term solution without add-back therapy, in patients with fibroid-related heavy menstrual bleeding 1, 2
Transition to definitive therapy (surgical options or UAE) should be considered if symptoms recur rapidly after discontinuation, in patients receiving relugolix treatment 4
Relugolix is commonly used for short courses to decrease fibroid size in preparation for surgery rather than indefinite management, in patients with fibroid-related heavy menstrual bleeding 1, 2
Add-back regimens increase the overall cost of therapy but are essential for long-term management to mitigate hypoestrogenic effects, according to Praxis Medical Insights 3