An overview of the basic information in the instructions for Trametinib Tablets

1. Common names: trametinib, Trametinib, tramatinib

Product name: Mekinist,Mekinist

2. Indications:

1. Melanoma:

(1)Trametinib (Trametinib)As a single agent in patients treated with BRAF inhibitors, or in combination with dabrafenib, for the treatment of patients with unresectable or metastatic melanoma with BRAF V600E or V600K mutations;

(2)Trametinib In combination with dabrafenib for adjuvant treatmentMelanoma patients with BRAF V600E or V600K mutations, and patients with lymph node involvement after complete resection.

2. Non-small cell lung cancer (NSCLC): Trametinib is suitable for combined treatment with dabrafenib in patients with metastatic non-small cell lung cancer with BRAF V600E mutations.

3. Anaplastic thyroid cancer (ATC): Trametinib combined with dabrafenib to treat patients with locally advanced or metastatic anaplastic thyroid cancer with BRAF V600E mutation and no satisfactory local-regional treatment options.

4. Solid tumors: Trametinib in combination with dabrafenib in adult and pediatric patients 1 year of age and older with BRAF V600E-mutated unresectable or metastatic solid tumors who have progressed after prior therapy and for whom there are no satisfactory alternative treatment options.

5. Low-grade glioma (LGG): Trametinib combination treatment with dabrafenib Pediatric patients 1 year old and above with BRAF V600E mutated low-grade glioma and need systemic treatment.

6. Limitations of use: Trametinib is not suitable for the treatment of patients with colorectal cancer due to its known intrinsic resistance to BRAF inhibition.

3. Usage and dosage:

1. Before treatment: Before starting treatment with trametinib and dabrafenib, doctors will confirm the presence of BRAF V600E mutations in tumor specimens.

2. Medication management:

（1）Trametinib tablets: Do not crush or break trametinib tablets. Take it at the same time every day, about 24 hours apart. Do not take a missed dose within 12 hours of your next dose of trametinib. If vomiting occurs after administration of trametinib, do not take additional doses. Take your next dose at the scheduled time.

(2)Trametinib Oral Solution: is administered by a caregiver. Before using the oral solution, ensure that caregivers are trained on the proper dosage and administration of trametinib oral solution. To prepare the oral solution of trametinib , tap the bottle until the powder flows freely. Add 90mL of distilled or purified water to the powder in the bottle, and invert or gently shake the recapped bottle for up to 5 minutes until the powder is completely dissolved, producing a clear solution. Separate the dose adapter from the oral syringe. After the solution has reconstituted, insert the dosing adapter into the neck of the bottle. Administer trametinib oral solution via an oral dosing syringe or feeding tube.

3. Recommended dose: For adult patients, the recommended dose of trametinib tablets is 2 mg, which should be taken orally at least 1 hour before or 2 hours after a meal. The recommended dose is 1 mg once daily for pediatric patients weighing 26-37 kg, 1.5 mg once daily for pediatric patients weighing 38-50 kg, and 2 mg once daily for pediatric patients weighing 51 kg or more.

The recommended duration of treatment for patients taking trametinib is until disease progression or unacceptable toxicity, except in the adjuvant melanoma setting, where treatment is recommended for one year until disease relapse or unacceptable toxicity.

4. Dose adjustment: Patients may experience some adverse reactions during treatment with trametinib. Doctors will adjust the dose of the drug according to the severity of the condition, such as reducing, interrupting or stopping the medication. If the patient cannot tolerate up to two dose reductions, permanently discontinue trametinib tablets or oral solution. When coadministered with dabrafenib, dose adjustments of trametinib are not recommended to treat adverse reactions associated with the coadministration, such as noncutaneous malignancies and uveitis. No dose adjustment of trametinib is required for new primary cutaneous malignancies.

4. Adverse reactions:

The most common side effects of trametinib are rash, diarrhea, fatigue, peripheral edema, nausea, and acneiform dermatitis. Some patients develop a rash, redness, or acne-like rash, and the skin may become very dry. This rash can become severe, leading to skin infection and hospitalization. The most common side effects of trametinib when combined with dabrafenib are fever, fatigue, nausea, chills, headache, diarrhea, vomiting, joint pain, and rash. After trametinib was put on the market, adverse events such as drug eruption with eosinophilia and systemic symptoms (DRESS syndrome), Swyer-James syndrome (SJS), and hemophagocytic lymphohistiocytosis (HLH) also occurred.

5. Storage:

（1)Trametinib tablets: Store refrigerated at 2°C to 8°C (36°F to 46°F). Dispense the medicine in the original bottle. Do not remove the desiccant. Protect from moisture and light. Do not put medications in pill boxes.

(2)Trametinib Oral solution: Store refrigerated at 2°C to 8°C (36°F to 46°F). Store in original carton to protect from light and moisture. After reconstitution, store in original bottle below 25°C (77°F) and do not freeze. Discard any unused solution 35 days after reconstitution.

The original drug of Trametinib has been launched in China and is included in the scope of medical insurance. Only patients who meet the indications can choose to reimburse. The price of 2 mg*30 tablets is more than RMB 10,000. The original drug of Trametinib sold overseas is priced at more than RMB 7,000 (the price may fluctuate due to the exchange rate). There are also generic trametinib drugs produced in other countries overseas, and their pharmaceutical ingredients are basically the same as those of the original drugs sold domestically and abroad. For example, the price of 2mg*30 tablets produced by a Laos pharmaceutical factory is more than 2,000 yuan (the price may fluctuate due to the exchange rate), and the price is relatively cheap.