Dabrafenib
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| Clinical data | |
|---|---|
| Trade names | Tafinlar |
| Pregnancy category |
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| ATC code | L01XE23 (WHO) |
| Legal status | |
| Legal status |
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| Identifiers | |
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| CAS Number | 1195765-45-7 |
| PubChem (CID) | 44462760 |
| ChemSpider | 25948204 |
| ChEBI | CHEBI:75045 |
| ChEMBL | CHEMBL2028663 |
| ECHA InfoCard | 100.215.965 |
| Chemical and physical data | |
| Formula | C23H20F3N5O2S2 |
| Molar mass | 519.56 g/mol |
| 3D model (Jmol) | Interactive image |
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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
- ↑ 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.