Vemurafenib

China [CN]

Vemurafenib Core Information

Generic Name: Vemurafenib  Chinese Name: 维莫非尼  CAS Number: 918504-65-1  Molecular Formula: C₂₃H₁₈ClF₃N₅O₃S  Molecular Weight: 536.96 g/mol  Chemical Name: N-[3-[[5-(4-chlorophenyl)-1H-pyrrolo[2,3-b]pyridin-3-yl]carbonyl]-2,4-difluorophenyl]-1-propanesulfonamide

Drug Type and Mechanism of Action

Drug Type: Oral selective BRAF kinase inhibitor

Mechanism of Action:

Highly selective inhibition of BRAF V600E mutant, blocking the MAPK/ERK pathway

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

Used as monotherapy for BRAF V600 mutant melanoma, and can be used in combination with MEK inhibitors to improve efficacy

Core Clinical Value (Latest as of 2026)

Approved Indications:

Unresectable/metastatic melanoma (BRAF V600 mutation)

Erdheim-Chester disease (ECD, a rare histiocytic tumor, BRAF V600 mutation)

Dosage Regimen: 960 mg, twice daily, orally with food

Safety: Common side effects include arthralgia, rash, photosensitivity, alopecia, nausea; Grade 3–4 skin toxicity, QT interval prolongation, and liver damage require monitoring

Physicochemical Properties (API)

Appearance: White to pale yellow crystalline powder

Solubility: Soluble in DMSO (100 mg/mL), methanol (25 mg/mL); poorly soluble in water

Storage: Stable for ≥2 years at -20℃ (powder); store at room temperature in a sealed container, protected from light and moisture

Chirality: No chiral center, single configuration