Valemetostat is an oral, selective EZH1 and EZH2 dual inhibitor, belonging to the histone methyltransferase inhibitor class of anti-tumor drugs.

1、 Drug name

1. Common name: Valemetostat Tosilate

2. Product Name: EZHARMIA ®) piece

2、 Indications

Used to treat the following two types of adult patients:

1. Recurrent or refractory adult T-cell leukemia/lymphoma.

2. Recurrent or refractory peripheral T-cell lymphoma.

3、 Specifications and characteristics

1. Specifications: There are two types of specifications. Ezzarmia tablets 50mg, each containing 67.6mg of varmestat tosylate (equivalent to 50mg of varmestat). Ezalemia tablets 100mg, each containing 135mg of varmestat tosylate (equivalent to 100mg of varmestat).

2. Appearance: The 50mg tablet is a white circular film coated tablet with a diameter of approximately 8.1mm and engraved with the code "220". The 100mg tablet is a red white oval shaped film coated tablet with a length diameter of about 14.1mm and a short diameter of about 6.7mm, engraved with the code "440".

4、 Main components

Active ingredient: Valametostatosylate salt.

5、 Usage and dosage

1. The recommended dosage for adults is once daily, 200mg (famotistat dose), taken orally on an empty stomach.

2. The dosage can be appropriately reduced according to the patient's tolerance.

6、 Dose adjustment

1. Dose adjustment is mainly based on the severity of adverse reactions.

2. The standard dose is 200mg. The dosage reduction is divided into four levels: 150mg for level one, 100mg for level two, and 50mg for level three. If 50mg is still intolerable, the medication needs to be discontinued.

7、 Medication precautions

1. Medication and eating: Food can significantly reduce drug absorption, and should be taken on an empty stomach 1 hour before or 2 hours after meals.

2. Missed dose: If one dose is missed, unless there is less than 12 hours before the next dose, the missed dose should be taken as soon as possible, and then the next dose should be taken according to the original plan. Do not take double the dose at once.

3. Vomiting: If vomiting occurs after taking medication, it should not be taken again, and the next dose should be taken according to the planned time.

8、 Medication for special populations

1. Patients with liver dysfunction: The medication data for patients with severe liver dysfunction is limited and caution should be exercised. Mild to moderate patients may need to adjust the dosage.

2. Pregnant women: Use only when the treatment benefits outweigh the potential risks. Animal experiments have shown embryo fetal toxicity and teratogenicity.

3. Breastfeeding women: It is recommended to stop breastfeeding as animal experiments have shown that drugs can be secreted through breast milk.

4. Individuals with fertility: Female patients and male partners must take effective contraceptive measures during treatment and within 2 weeks after the last dose. Male patients may be at risk of reduced sperm production.

5. Children: Safety and efficacy have not yet been established.

9、 Adverse reactions

1. Common serious adverse reactions include bone marrow suppression (such as thrombocytopenia, anemia, neutropenia) and infection.

2. Other common adverse reactions include taste disorders, nausea, diarrhea, rash, hair loss, fatigue, AST/ALT elevation, etc.

10、 Contraindications

Patients with a history of allergies to any of the ingredients in this product are prohibited from using it.

11、 Drug interactions

1. Prohibition or need to adjust dosage combination: When used in combination with potent CYP3A inhibitors (such as itraconazole, clarithromycin) or P-gp inhibitors (such as verapamil), it will significantly increase the blood concentration of this product. It is necessary to reduce the dosage of this product or even avoid combination use.

2. Attention should be paid to the combination use: Combining with intermediate acting CYP3A inhibitors (such as fluconazole) may increase the risk of side effects of this product. The combination with CYP3A inducers (such as rifampicin) may reduce the efficacy of this product, and switching to drugs without induction should be considered.

3. Effects on other drugs: This product is a P-gp inhibitor, and when used in combination with P-gp substrates (such as digoxin), it may increase the blood concentration and risk of side effects of the latter, requiring close monitoring.

12、 Storage method

1. Store at room temperature.

2. Moisture proof is required, and it should be removed from the aluminum-plastic packaging before use.

13、 Manufacturer

Daiichi Sankyo Company, Limited.

Valemetostatinformation