Tafinlar®Dabrafenib Mesylate

Tafinlar® Dabrafenib Mesylate Capsules

Brand Name:泰菲乐 ®(Tafinlar®)

Generic Name:Dabrafenib Mesylate

Strength:75 mg per capsule, 120 capsules per bottle

Manufacturer: Glaxo Operations (UK) Ltd. (original manufacturer, later transferred to Novartis)

Marketing Authorization Holder:Novartis Pharma AG; Domestic marketing authorization holder: Beijing Novartis Pharma Co., Ltd.

Approval Date in China:December 19, 2019

Registration Number:国药准字HJ20190066

Storage:Store in a light-proof, airtight container below 30°C in a dry place; keep the desiccant inside the original bottle after opening, and avoid access by children.

Price&Cost:Contact Us now for the best price of Dabrafenib Mesylate（Tafinlar）

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1. Indications and Usage 

  • Unresectable or Metastatic Melanoma: Treatment of patients with BRAF V600E or V600K mutation-positive unresectable or metastatic melanoma (often in combination with trametinib) .
  • Non-Small Cell Lung Cancer (NSCLC): Treatment of patients with BRAF V600E mutation-positive metastatic NSCLC .
  • Anaplastic Thyroid Cancer (ATC): Treatment of patients with BRAF V600E mutation-positive anaplastic thyroid cancer .

2. Dosage and Administration 

  • Administration: Oral administration. Capsules must be swallowed whole (do not open, crush, or break). Take on an empty stomach (at least 1 hour before or 2 hours after a meal) .
  • Dosing Regimen:
    • Monotherapy: 150 mg twice daily (approx. every 12 hours) .
    • Combination Therapy (with Trametinib): Dabrafenib 150 mg twice daily + Trametinib 2 mg once daily .
  • Missed Dose: Do not take a missed dose if it is less than 6 hours before the next scheduled dose. Resume at the next scheduled time .

3. Mechanism of Action 

Dabrafenib is a BRAF kinase inhibitor.
It selectively inhibits the activity of mutant BRAF (V600E, V600K, V600D) kinases, which leads to inhibition of the RAS-RAF-MEK-ERK signaling pathway, resulting in reduced cell proliferation and induction of apoptosis in tumor cells .

4. Safety and Warnings 

  • Cutaneous Squamous Cell Carcinoma (cuSCC): Treatment-emergent cuSCC or keratoacanthoma may occur due to paradoxical activation of the MAPK pathway in BRAF wild-type cells. Monitor skin examinations every 2 months during treatment and for up to 6 months after discontinuation .
  • Hyperglycemia: Monitor blood glucose levels, especially in patients with pre-existing diabetes .
  • Ocular Toxicity: Retinal vein occlusion (RVO) and uveitis may occur. Baseline and periodic ophthalmologic examinations are recommended .
  • Hemorrhage: Severe and fatal hemorrhagic events have been reported. Monitor for signs of bleeding .
  • Embryo-Fetal Toxicity: May cause fetal harm. Effective contraception is required for females of reproductive potential .

5. Adverse Reactions 

Common adverse reactions (incidence ≥20%) when used as monotherapy include:
  • Pyrexia , Headache, Fatigue.
  • Arthralgia , Palmar-plantar erythrodysesthesia 
  • Rash, Pruritus, Hyperkeratosis 
  • Diarrhea, Vomiting, Nausea .

6. Drug Interactions 

  • CYP450 Substrate/Inducer:
    • Dabrafenib is metabolized primarily by CYP3A4 and CYP2C8. Avoid strong inhibitors (e.g., ketoconazole) and strong inducers (e.g., rifampin) .
    • Dabrafenib induces CYP3A4, CYP2C9, etc. It may decrease the exposure of sensitive substrates (e.g., oral contraceptives, warfarin). Monitor these drugs closely .

7. Pharmaceutical Information 

  • Chemical Name: Dabrafenib mesylate.
  • Molecular Formula: C23H23Br2FN3O4S·CH4O3S .
  • Molecular Weight: 815.53 .
  • Storage: Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F) .

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