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 | 〇 | 〇 | 〇 | 〇 | 〇 | 295(88%) | 303(90%) |
| V600D mutation | 〇 | 〇 | 〇 | △a | 0 | 1 | |
| V600K mutation | 〇 | △a | 33(10%) | 24(7%) | |||
| Other mutations | 10 other V600 mutations | V600R mutation | 0 | 1 | |||
| Wild type | 〇 | 〇 | 〇 | 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