2020
DOI: 10.2174/1871520620666200422073622
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Promising Strategies for Overcoming BRAF Inhibitor Resistance Based on Known Resistance Mechanisms

Abstract: Background: Almost 50% of metastatic melanomas harbor BRAF mutations. Since 2011, BRAF inhibitors have exhibited striking clinical benefits in BRAF-mutant melanoma patients. Unfortunately, their therapeutic effects are often temporary. The resistance mechanisms vary and can be broadly classified as MAPK reactivationdependent and -independent. Elucidation of these resistance mechanisms provides new insights into strategies for overcoming resistance. Indeed, several alternative treatment strategies, including c… Show more

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Cited by 3 publications
(2 citation statements)
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“…Therefore, having used the “powerful weapons” in the fight against melanoma, the management of this recurrence has raised concerns. Targeted therapy, which the patient had started years ago, was considered a good choice, as the tumor cell resistance mechanisms that may have formed may have been eliminated by stopping BRAFi and MEKi for a significant period of time [ 2 , 3 , 5 , 6 ].…”
Section: Case Presentationmentioning
confidence: 99%
“…Therefore, having used the “powerful weapons” in the fight against melanoma, the management of this recurrence has raised concerns. Targeted therapy, which the patient had started years ago, was considered a good choice, as the tumor cell resistance mechanisms that may have formed may have been eliminated by stopping BRAFi and MEKi for a significant period of time [ 2 , 3 , 5 , 6 ].…”
Section: Case Presentationmentioning
confidence: 99%
“…For example, FDA has approved the combination of BRAF inhibitors (Vemurafenib and Dabrafenib) and MEK inhibitor trametinib for the treatment of BRAF inhibition resistance. And clinical studies of PI3K/AKT inhibitor plus MAPK inhibitor, everolimus (RAD001) plus bevacizumab, everolimus (RAD001) plus temozolomide (TMZ), and targeted therapy plus immunotherapy have also been conducted, but there is a lack of more data to support these therapies, so further exploration is needed ( 82 ). The strategies for resistance to BRAF inhibitors were listed in Table 1 .…”
Section: The Therapy Of Braf Activationmentioning
confidence: 99%