Dabrafenib is a small molecule kinase inhibitor that inhibits tumor cell proliferation by targeting BRAF serine/threonine kinase activity, blocking abnormal activation of the MAPK signaling pathway.

1、 Drug name

1. Common name: Dabrafenib;

2. Product Name: TAFINLAR ®。

2、 Indications

1. Monotherapy or combination therapy with trametinib for BRAFV600E or V600K mutation positive unresectable or metastatic melanoma.

2. Combination therapy with trametinib for adjuvant therapy after BRAFV600E/K mutation positive melanoma surgery (after lymph node involvement and complete resection).

3. Combination therapy with trametinib for BRAFV600E mutation positive metastatic non-small cell lung cancer (NSCLC).

4. Combination therapy with trametinib for locally advanced or metastatic undifferentiated thyroid cancer (ATC) with BRAFV600E mutation positivity.

5. Combination therapy with trametinib for BRAFV600E mutation positive unresectable or metastatic solid tumors aged 6 years and above (with previous treatment failures and no satisfactory alternative options).

6. Combination therapy with trametinib for low-grade gliomas (LGG) aged 1 year and above with BRAFV600E mutation positive and requiring systemic treatment.

7. Note: Not applicable to patients with wild-type BRAF solid tumors or colorectal cancer.

3、 Specifications and characteristics

Capsules: 75mg

4、 Main components

1. Active ingredient: dabrafenib esylate.

2. Accessories include microcrystalline cellulose, colloidal silica, etc.

5、 Usage and dosage

1. Adults: Recommended dosage is 150mg orally, twice daily (with an interval of about 12 hours).

2. Children: Adjust the dosage according to body weight (e.g. 75-150mg twice daily for those weighing ≥ 26kg; Calculate the dosage of suspension tablets based on body weight for individuals weighing 1-25kg.

3. Medication time: Take 1 hour before or 2 hours after meals, avoid taking with food.

4. Omission treatment: If it is less than 6 hours before the next medication, skip it and do not make up for it.

5. Vomiting treatment: Do not take additional medication after vomiting, follow the original plan for the next dose.

6、 Dose adjustment

1. Adverse reaction adjustment: Suspend, reduce or permanently discontinue medication based on toxicity level (if fever occurs, pause; if severe skin toxicity occurs, permanently discontinue medication).

2. Liver dysfunction: Mild to moderate without adjustment, severe without clear recommended dosage.

7、 Medication precautions

1. Risk of newly diagnosed malignant tumors: Regular skin examinations are required during treatment to monitor non skin malignant tumor symptoms.

2. Bleeding risk: Combination therapy with trametinib may cause bleeding, be alert to symptoms of intracranial or gastrointestinal bleeding.

3. Cardiotoxicity: Monitor left ventricular function before and during treatment.

4. Eye problems: Seek medical attention immediately if there are changes in vision.

5. Fever reaction: common and possibly severe, requiring timely symptomatic treatment.

8、 Medication for special populations

1. Pregnant women: May cause fetal damage, effective contraception (non hormonal) is required until 2 weeks after the last dose.

2. Breastfeeding period: Breastfeeding is prohibited within 2 weeks after discontinuation of medication.

3. Children: Suitable for LGG patients aged ≥ 1 year and solid tumor patients aged ≥ 6 years, dosage should be adjusted according to body weight.

9、 Adverse reactions

1. Common adverse reactions include fever, rash, headache, joint pain, fatigue, nausea, vomiting, diarrhea, etc.

2. Serious adverse reactions may involve: cardiomyopathy, uveitis, severe skin toxicity, etc.

10、 Contraindications

There are no clear contraindications, but it is contraindicated for patients with wild-type BRAF tumors.

11、 Drug interactions

1. CYP3A4/CYP2C8 strong inhibitors (such as ketoconazole) may increase the blood concentration of dalafenib.

2. Dalafenib reduces the efficacy of CYP3A4/CYP2C9 substrates (such as warfarin) and requires monitoring of INR.

12、 Storage method

1. Capsules: Store in the original bottle and place in a dry environment at 20-25 ° C.

2. Desiccant: The desiccant inside the bottle should be retained and not discarded.

Dabrafenibinformation