Zelboraf (vemurafenib; Roche/Chugai/Daiichi Sankyo) is an orally available agent that selectively targets the BRAF mutation. BRAF is part of the mitogen-activated protein kinase (MAPK) signal transduction pathway, which is critical in tumor cell proliferation. The MAPK pathway controls cell proliferation following growth receptor stimulation. The typical binding of the ligand to the receptor triggers a chain of events that includes the activation of a series of downstream effectors, one of these being the RAF series of serine/threonine kinases, including BRAF. However, melanoma cells with BRAF mutations are known to be “addicted” to BRAF, as the mutation renders the protein constitutively active, thereby eliminating the need for receptor-mediated activation, and the efficacy of Zelboraf has demonstrated the potential of BRAF inhibitor treatment.
LIST OF FIGURES 12 Figure 1: Zelboraf in melanoma – SWOT analysis
13 Figure 2: Datamonitor Healthcare’s drug assessment summary of Zelboraf for melanoma
14 Figure 3: Datamonitor Healthcare’s drug assessment summary of Zelboraf for melanoma
16 Figure 4: Zelboraf sales for melanoma across the US, Japan, and five major EU markets, by country, 2017–26
LIST OF TABLES
6 Table 1: Zelboraf drug profile
8 Table 2: Zelboraf pivotal trial data in melanoma
11 Table 3: Zelboraf ongoing late-phase clinical trial in melanoma
17 Table 4: Zelboraf sales for melanoma across the US, Japan, and five major EU markets, by country ($m), 2017–26
19 Table 5: Zelboraf patient numbers for melanoma across the US, Japan, and five major EU markets, by country, 2017–26
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