Special attention should be paid to embryo fetal toxicity during the use of Masinotecan. Women of childbearing age should rule out pregnancy before treatment and take effective contraceptive measures during treatment and at least one month after discontinuation.

1、 Drug name

1. Common name: Macitentan;

2. Product Name: Opsumit ®。

2、 Indications

Masitentan is an endothelin receptor antagonist (ERA) used to treat pulmonary arterial hypertension (PAH, WHOI class) and delay disease progression.

3、 Specifications and characteristics

1. Specification: 10mg

2. Appearance: Tablets

4、 Main components

Active ingredient: Masitentan (chemical name: N - [5- (4-bromophenyl) -6- [2- [(5-bromo-2-pyrimidinyl) oxy] ethoxy] -4-pyrimidinyl] - N '- propylsulfonamide).

5、 Usage and dosage

1. Recommended dosage: 10mg orally, once daily.

2. Medication method: Take the whole tablet orally, before or after meals.

3. Omission treatment: If remembered on the same day, take the medication as scheduled the next day.

6、 Dose adjustment

1. Abnormal liver function: pause when ALT/AST is greater than 3 times the upper limit, and consider reducing dosage after recovery.

2. Hemoglobin reduction: Use with caution in patients with severe anemia (Hb<10g/dL).

7、 Medication precautions

1. Pregnancy risk: Women need to undergo pregnancy testing before treatment, monthly during treatment, and one month after discontinuing medication, and take two contraceptive measures.

2. Monitoring requirements: Baseline and regular check ups for liver function and hemoglobin.

3. Vomiting treatment: Vomiting after taking medication does not require supplementation.

8、 Medication for special populations

1. Pregnant women: Prohibited, may cause fetal malformation.

2. Breastfeeding period: Stop taking medication or breastfeeding.

3. Children and the elderly: safety and effectiveness are not clearly defined; Elderly patients do not need to adjust their dosage.

9、 Adverse reactions

1. Common (≥ 3%): anemia (13%), nasopharyngitis (20%), bronchitis (12%), headache (14%), influenza (6%), urinary tract infection (9%).

2. Serious reactions: hepatotoxicity, pulmonary edema (PVOD), reduced sperm count.

10、 Contraindications

Pregnant women are prohibited from using it.

11、 Drug interactions

1. Strong CYP3A4 inducers (such as rifampicin): significantly reduce the exposure of Masinoten and avoid combination therapy.

2. Strong CYP3A4 inhibitors (such as ketoconazole and ritonavir): Increase exposure to Masinotenib and avoid combination therapy.

12、 Storage method

1. Storage temperature: 20-25 ° C (68-77 ° F), short-term 15-30 ° C (59-86 ° F) allowed.

2. Keep the original packaging and avoid moisture and light exposure.

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