Dabrafenib

China [CN]

Dabrafenib Core Information

Generic Name: Dabrafenib  Chinese Name: 达拉非尼 (Dabrafenib) CAS Number: 1195765-45-7 Molecular Formula: C₂₁H₂₁F₃N₅O₂S₂ Molecular Weight: 496.55 g/mol Chemical Name: N-[3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl]-2,6-difluorobenzenesulfonamide

Drug Type and Mechanism of Action

Drug Type: Oral selective BRAF kinase inhibitor

Mechanism of Action:

Potently inhibits BRAF V600 mutants (V600E/K/D), blocking the MAPK/ERK signaling pathway

Inhibits tumor cell proliferation and induces apoptosis; has weak inhibitory effect on BRAF wild-type

Often used in combination with MEK inhibitors (such as Trametinib) to overcome monotherapy resistance and prolong PFS

Core Clinical Value (Latest as of 2026)

Approved Indications:

Unresectable/metastatic melanoma (BRAF V600 mutation)

Non-small cell lung cancer (NSCLC) (BRAF V600E mutation)

Locally advanced/metastatic anaplastic thyroid carcinoma (ATC) (BRAF V600E mutation)

Dosage Regimen: 150 mg, twice daily, orally on an empty stomach (1 hour before or 2 hours after meals)

Combination Therapy: Dabrafenib + Trametinib is the standard first-line treatment for BRAF V600 mutated tumors

Safety: Common side effects include fever (50%+), rash, fatigue, and arthralgia; Grade 3–4 fever requires discontinuation/dose reduction; caution should be exercised regarding cardiomyopathy, ocular toxicity, and cutaneous squamous cell carcinoma.