Rulugoli reduces the secretion of luteinizing hormone (LH) and follicle stimulating hormone (FSH) by blocking the GnRH receptor in the anterior pituitary gland, thereby lowering estrogen levels in the body. This mechanism is highly effective in treating uterine fibroids and endometriosis, as the occurrence and development of these diseases are closely related to high levels of estrogen.

1、 Drug name and main ingredients

1. Common name: Relugolix

2. Product Name: MYFEMBREE ® (Compound preparation, containing rilugole, estradiol, and norethinyl acetate)

3. Dosage form: Oral film coated tablets

4. Main ingredients: Each tablet contains 40mg of rilugole, 1mg of estradiol (E2), and 0.5mg of norethinyl acetate (NETA)

2、 Indications

Applicable to premenopausal women in the following two situations:

1. Severe bleeding related to uterine fibroids: for patients with fibroids causing menstrual flow>80ml/cycle or anemia (Hb<110g/L);

2. Endometriosis related pain: suitable for pelvic pain with VAS score ≥ 4, with or without deep infiltrating nodules.

3. Usage restrictions: The treatment time should not exceed 24 months (as it may lead to irreversible bone density decline).

3、 Specifications and characteristics

1. Specification: Each tablet contains 40mg/E21mg/NETA0.5mg of Relugol, light yellow to yellow circular film coated tablets, with "MVT" engraved on one side and "415" on the other side.

2. Packaging: 28 tablets/bottle (including desiccant), equipped with a child safety bottle cap.

4、 Usage and dosage

1. Regular dosage: 1 tablet once a day, swallowed whole, can be taken with food or on an empty stomach.

2. Omission treatment: If missed, it should be taken as soon as possible on the same day and taken according to the original plan the next day; No need to take additional medication after vomiting.

3. Special medication: When using P-gp inhibitors (such as erythromycin) in combination, a minimum interval of 6 hours is required (taking MYFEMBREE first).

5、 Medication precautions

1. Monitoring requirements:

Regularly monitor bone density (DXA scan), liver function, blood pressure, blood lipids, and blood glucose before and during treatment.

Seek medical attention immediately if jaundice, chest pain, sudden visual changes, or severe headaches occur.

2. Contraceptive measures: Non hormonal contraception (such as condoms) should be used during treatment and within one week after discontinuation.

3. Diet: Avoid grapefruit juice (which may interfere with metabolism).

6、 Medication for special populations

1. Pregnant women: Absolute contraindication (can cause early miscarriage).

2. Breastfeeding period: Breastfeeding is prohibited during the treatment period and within one week of discontinuation of medication.

3. Liver injury: Moderate to severe liver injury (Child Pugh B/C) is contraindicated.

4. Elderly: No need to adjust dosage, but need to strengthen monitoring.

7、 Adverse reactions

1. Common (≥ 3%): hot flashes (10.6%), abnormal uterine bleeding (6.3%), hair loss (3.5%), decreased libido (3.1%).

2. Serious reactions: Thrombotic events (DVT/PE), hepatotoxicity, depression or suicidal tendencies, uterine fibroid prolapse.

8、 Contraindications

1. History of thrombotic disease or high risk (such as smoking and age>35 years, uncontrolled hypertension).

2. Pregnancy, breast cancer or other hormone sensitive tumors.

3. Osteoporosis or severe liver disease.

4. People who are allergic to ingredients.

9、 Drug interactions

1. P-gp inhibitor: Increase exposure to rilugole with an interval of 6 hours;

2. Strong CYP3A inducers (such as rifampicin): reduce efficacy and avoid combination therapy;

3. Hormonal contraceptives: may reduce efficacy and increase adverse reactions.

10、 Storage method

Store at room temperature (15-30 ° C), keep the original bottle away from light and moisture, and do not remove the desiccant.

Relugolixinformation