Dabrafenib
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Systematic (IUPAC) name | |
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N-{3-[5-(2-aminopyrimidin-4-yl)-2-tert-butyl-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide
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Clinical data | |
Trade names | Tafinlar |
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Identifiers | |
CAS Number | 1195765-45-7 |
ATC code | L01XE23 (WHO) |
PubChem | CID: 44462760 |
ChemSpider | 25948204 |
ChEBI | CHEBI:75045 |
ChEMBL | CHEMBL2028663 |
Chemical data | |
Formula | C23H20F3N5O2S2 |
Molecular mass | 519.56 g/mol |
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Dabrafenib (trade name Tafinlar, GSK2118436) is a drug for the treatment of cancers associated with a mutated version of the gene BRAF. Dabrafenib acts as an inhibitor of the associated enzyme B-Raf, which plays a role in the regulation of cell growth. Dabrafenib has clinical activity with a manageable safety profile in clinical trials of phase 1 and 2 in patients with BRAF(V600)-mutated metastatic melanoma.[1][2]
The Food and Drug Administration initially approved dabrafenib as a single agent treatment for patients with BRAF V600E mutation-positive advanced melanoma on May 30, 2013.[3] Clinical trial data demonstrated that resistance to dabrafinib and other BRAF inhibitors occurs within 6 to 7 months.[4] To overcome this resistance, the BRAF inhibitor dabrafenib was combined with the MEK inhibitor trametinib.[4] On January 8, 2014, the FDA approved this combination of dabrafenib and trametinib for BRAF V600E/K-mutant metastatic melanoma.[5][6]
References
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- Pyrimidines
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