What are the serious side effects of myfembree and how to deal with them?

myfembree

Also called relugolix/estradiol/norethindrone acetate, it is a combination of relugolix, estradiol (E2) and norethindrone acetate (NETA). Relugolix is a non-skin GnRH receptor antagonist that competitively binds Binds to pituitary GnRH receptors, thereby reducing the release of luteinizing hormone (LH) and follicle-stimulating hormone (FSH), resulting in lower serum concentrations of the ovarian sex hormones estradiol and progesterone, and reducing bleeding associated with uterine fibroids and pain associated with endometriosis.

myfembree is indicated for the treatment of heavy menstrual bleeding associated with uterine leiomyomas and moderate to severe pain associated with endometriosis.

Serious side effects of myfembree and how to deal with them

1. Thromboembolic diseases and vascular events: myfembree increases the risk of thrombosis or thromboembolic diseases, including pulmonary embolism, deep vein thrombosis, stroke and myocardial infarction, and is therefore contraindicated in women with current or past thromboembolic or thromboembolic diseases and women who are at increased risk of these events.

Discontinue immediately if arterial or venous thrombosis, cardiovascular or cerebrovascular events occur or are suspected. If feasible, discontinue myfembree at least 4-6 weeks before surgery where the risk of thromboembolism is increased, or during prolonged immobilization.

2. Bone loss: Myfembree is contraindicated in women with known osteoporosis. Consider the benefits and risks of myfembree treatment in patients with a history of low-traumatic fractures or risk factors for osteoporosis or bone loss, including taking drugs that may reduce bone mineral density (BMD).

It is recommended to assess BMD by dual-energy X-ray absorptiometry (DXA) at baseline. For women with heavy menstrual bleeding related to uterine fibroids, regular DXA is recommended during treatment with myfembree. For women with moderate to severe pain associated with endometriosis, an annual DXA is recommended while taking myfembree. If the risks associated with bone loss outweigh the potential benefits of treatment, consider discontinuing myfembree.

3. Hormone-sensitive malignant tumors: Myfembree is contraindicated in women who currently have or have a history of hormone-sensitive malignant tumors (such as breast cancer) and women who are at higher risk of hormone-sensitive malignant tumors. If a hormone-sensitive malignancy is diagnosed, discontinue use of myfembree.

4. Suicidal ideation and mood disorders: including depression, assess patients with a history of suicidal ideation, depression, and mood disorders before initiating treatment. Monitor patients for changes in mood and symptoms of depression, including soon after starting treatment, to determine whether the risks of continuing treatment with myfembree outweigh the benefits. Advise patients who develop suicidal thoughts and behaviors to seek immediate medical attention.

5. Liver function damage and elevated transaminases: If symptoms or signs of liver damage, such as jaundice or right upper quadrant pain, occur during medication, you should seek medical attention promptly. Acute liver function abnormalities may require discontinuation of myfenbre until liver tests return to normal. Myfembree is contraindicated in patients with known liver damage or disease.

6. Gallbladder disease or cholestatic jaundice: If signs or symptoms of gallbladder disease or jaundice occur, discontinue use of myfembree.

7. Increased blood pressure: A study showed adverse reactions of new onset or worsening hypertension. Therefore, myfembree is contraindicated in women with uncontrolled hypertension. For women with well-controlled hypertension, continue to monitor blood pressure. If blood pressure rises significantly, stop taking the medication.

myfembree

Relugolix is a gonadotropin-releasing hormone (GnRH) receptor antagonist that reduces serum estradiol and progesterone concentrations to postmenopausal levels. Adding estradiol/norethindrone acetate to relugolix improves relugolix-induced bone loss and hot flashes.

In two Phase 3 LIBERTY trials, relugolix + estradiol/norethindrone significantly reduced menstrual bleeding and improved a range of other uterine fibroid symptoms in women with uterine fibroid-related heavy menstrual bleeding. The combination is generally well tolerated, with vasomotor symptoms being the most common.

Treatment with this combination for more than 2 years did not result in clinically meaningful bone loss in most women. Relugolix/estradiol/norethindrone acetate is convenient for once-daily administration and is a useful addition to current drug treatments for premenopausal women with uterine fibroids.

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