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. 2015 Oct;80(4):765-7.
doi: 10.1111/bcp.12651. Epub 2015 Jun 11.

Vemurafenib/dabrafenib and trametinib

Affiliations

Vemurafenib/dabrafenib and trametinib

Robert Rissmann et al. Br J Clin Pharmacol. 2015 Oct.
No abstract available

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Figures

Figure 1
Figure 1
The RAS-RAF-MEK-ERK pathway and the mechanism of action of vemurafenib, dabrafenib and trametinib. Oncogenic mutations in the BRAF protein cause overactivation of this pathway, leading to increased cell proliferation, cell survival, and angiogenesis (A). Vemurafenib and dabrafenib selectively inhibit mutated BRAF proteins, whereas trametinib inhibits MEK and downstream ERK signalling. TF, transcription factor (B)

References

    1. Flaherty KT, Yasothan U, Kirkpatrick P. Vemurafenib. Nat Rev Drug Discov. 2011;10:811–12. - PubMed
    1. European Medicines Agency. Zelboraf: EPAR – Product Information. March 19 2012. Available at http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Info... (updated August 5 2014, last accessed 11 February 2015)
    1. European Medicines Agency. Tafinlar: EPAR – Product Information. September 18 2013. Available at http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Info... (updated January 1 2015, last accessed 11 February 2015)
    1. European Medicines Agency. Mekinist: EPAR – Product Information. July 9 201. Available at http://www.ema.europa.eu/docs/en_GB/document_library/EPAR_-_Product_Info... (updated February 4 2015, last accessed 11 February 2015)
    1. Flaherty KT, Infante JR, Daud A, Gonzalez R, Kefford RF, Sosman J, Hamid O, Schuchter L, Cebon J, Ibrahim N, Kudchadkar R, Burris HA, III, Falchook G, Algazi A, Lewis K, Long GV, Puzanov I, Lebowitz P, Singh A, Little S, Sun P, Allred A, Ouellet D, Kim KB, Patel K, Weber J. Combined BRAF and MEK inhibition in melanoma with BRAF V600 mutations. N Engl J Med. 2012;367:1694–703. - PMC - PubMed

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