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 | |
| Clinical data | |
| Trade names | Tafinlar |
| Pregnancy category |
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| Legal status |
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| Identifiers | |
| CAS Number | 1195765-45-7 |
| ATC code | L01XE23 |
| PubChem | CID 44462760 |
| ChemSpider | 25948204 |
| ChEBI | CHEBI:75045 |
| ChEMBL | CHEMBL2028663 |
| Chemical data | |
| Formula | C23H20F3N5O2S2 |
| Molar mass | 519.56 g/mol |
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Dabrafenib (trade name Tafinlar) 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 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] As a result of this research, on January 8, 2014, the FDA approved the combination of dabrafenib and trametinib for the treatment of patients with BRAF V600E/K-mutant metastatic melanoma.[5][6]
References
- ↑ Gibney, G. T.; Zager, J. S. (2013). "Clinical development of dabrafenib in BRAF mutant melanoma and other malignancies". Expert Opinion on Drug Metabolism & Toxicology 9 (7): 1. doi:10.1517/17425255.2013.794220. PMID 23621583.
- ↑ Huang, T.; Karsy, M.; Zhuge, J.; Zhong, M.; Liu, D. (2013). "B-Raf and the inhibitors: From bench to bedside". Journal of Hematology & Oncology 6: 30. doi:10.1186/1756-8722-6-30. PMC 3646677. PMID 23617957.
- ↑ "GSK melanoma drugs add to tally of U.S. drug approvals". Reuters. May 30, 2013.
- 1 2 "Combined BRAF and MEK Inhibition in Melanoma with BRAF V600 Mutations" 367 (18). New England Journal of Medicine. November 1, 2012: 1694–703. doi:10.1056/NEJMoa1210093. PMC 3549295. PMID 23020132.
- ↑ "Dabrafenib/Trametinib Combination Approved for Advanced Melanoma". OncLive. January 9, 2013.
- ↑ Maverakis E, Cornelius LA, Bowen GM, Phan T, Patel FB, Fitzmaurice S, He Y, Burrall B, Duong C, Kloxin AM, Sultani H, Wilken R, Martinez SR, Patel F (2015). "Metastatic melanoma - a review of current and future treatment options". Acta Derm Venereol 95 (5): 516–524. doi:10.2340/00015555-2035. PMID 25520039.
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