The label for products containing Relugolix, specifically those used as combination oral contraceptives (COCs), received a boxed warning regarding serious cardiovascular events, effective January 29, 2026. This warning explicitly states that cigarette smoking increases the risk of serious cardiovascular events from COC use. The risk is further heightened with age, particularly in women over 35 years of age.
Background
Relugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist. It is a component in certain combination products, such as relugolix, estradiol hemihydrate, and norethindrone acetate, which are formulated as combination oral contraceptives (COCs). COCs are widely prescribed for various indications, including contraception and management of gynecological conditions. Given the broad use of COCs, safety information regarding their use, especially in specific patient populations, is crucial for prescribing clinicians and patients.
What this means
This new boxed warning represents a significant update for healthcare providers prescribing combination oral contraceptives, including those that may contain Relugolix. The warning explicitly states that cigarette smoking substantially increases the risk of serious cardiovascular events when using COCs. Furthermore, this risk is particularly pronounced in women over 35 years of age. This necessitates a thorough assessment of a patient's smoking status and age by clinicians. Comprehensive counseling on the associated cardiovascular risks is crucial before initiating or continuing COC therapy. The presence of a boxed warning, the FDA's strongest warning, highlights the critical importance of these risk factors and the need for careful patient selection and ongoing monitoring to mitigate potential adverse outcomes related to serious cardiovascular events.
Source
The information regarding this label revision was obtained from the U.S. Food and Drug Administration (FDA), as published on DailyMed, a service of the National Library of Medicine. The boxed warning became effective on January 29, 2026, and the full details are accessible via dailymed.nlm.nih.gov.