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. 2024 Jan 2;19:5. doi: 10.1186/s13023-023-03000-0

Table 2.

Vemurafenib development for malignant melanoma with mutations in specific amino acids

BRAF in vitro In vivo Clinical trial (Phase III)
Kinase inhibition Inhibition of cell phosphorylation Growth inhibition Inclusion criteria Vemurafenib (n = 336) Control (n = 337)
V600E mutation 295(88%) 303(90%)
V600D mutation a 0 1
V600K mutation a 33(10%) 24(7%)
Other mutations 10 other V600 mutations V600R mutation 0 1
Wild type 1 1

Mutated cell lines used in non-clinical studies of cancer drugs with mutations in specific amino acids and inclusion criteria for clinical trials

Growth inhibitory effects were evaluated in vitro using cancer cells with target mutations

aThe Cobas® BRAF V600 mutation test shows cross-reactivity to BRAF V600K and V600D