Product Name

Vemurafenib

CAS Number

918504-65-1

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Product Name:
Vemurafenib
CAS Number:
918504-65-1
Indication:
Treatment of unresectable or metastatic melanoma in patients with the BRAF-V600 mutation.
Mode of Action:

Vemurafenib is an orally available inhibitor of mutated BRAF-serine-threonine kinase. It is especially potent against the BRAF V600E mutation. This mutation involves the substitution of glutamic acid for valine at codon 600. The BRAF oncogene, most of which have the V600E mutation, activates mitogen-activated kinase (MAPK) pathway which results in cell growth, proliferation, and metastasis. Vemurafenib blocks these downstream processes to inhibit tumour growth and eventually trigger apoptosis. Vemurafenib does not have antitumour effects against melanoma cell lines with the wild-type BRAF mutation.

Metabolism:

Vemurafenib is metabolized by CYP3A4 and the metabolites make up 5% of the components in plasma. The parent compound makes up for the remaining 95%.

IUPAC:
N-{3-[5-(4-chlorophenyl)-1H-pyrrolo[2, 3-b]pyridine-3-carbonyl]-2, 4-difluorophenyl}propane-1-sulfonamide
ATC:
L01XE15
DrugBank:
DB08881
Formula:
C23H18ClF2N3O3S
Molecular Mass:
489.922
Synonyms:
BRAF(V600E) Kinase Inhibitor RO5185426
SMILES:
CCCS(=O)(=O)NC1=C(F)C(C(=O)C2=CNC3=NC=C(C=C23)C2=CC=C(Cl)C=C2)=C(F)C=C1
AHFS Code:
10:00
General Reference:
General Reference:

  1. Jordan EJ, Kelly CM: Vemurafenib for the treatment of melanoma. Expert Opin Pharmacother. 2012 Dec;13(17):2533-43. doi: 10.1517/14656566.2012.737780. Epub 2012 Oct 24. Pubmed

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