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Association details:
Biomarker:MAP2K1 mutation
Cancer:Melanoma
Drug:Mekinist (trametinib) (MEK inhibitor)
Direction:Resistant
Evidence:
Evidence Level:
Resistant: D – Preclinical
New
Title:

The genetic landscape of clinical resistance to RAF inhibition in metastatic melanoma

Excerpt:
All MEK1 mutations examined conferred robust resistance to both RAF and MEK inhibition following doxycycline induction, with fold change in GI50 (half-maximal inhibitory concentration) of 10–80 fold for dabrafenib (Fig. 3C) and 3–20 fold for trametinib (Fig. 3D) as compared to wild-type MEK1, noting that only 50% growth inhibition was maximally achieved.
DOI:
10.1158/2159-8290.CD-13-0617