Gene mutation | Tyrosine kinase inhibitor | Clinical trial | Outcome |
---|---|---|---|
BRAF/MEK | Dabrafenib + trametinib | COMBI-d (75) | 3-y OS: 44% vs. 32% (dabrafenib + placebo) (HR, 0.75) |
Encorafenib + binimetinib | COLUMBUS (76) | 5-y OS: 34.7% vs. 21.4% (vemurafenib) | |
Vemurafenib + cobimetinib | coBRIM (77) | mOS: 22.3 vs. 17.4 mo (vemurafenib) (HR, 0.7) | |
NRAS | Binimetinib | NEMO (41) | mPFS: 2.8 vs. 1.5 mo (dacarbazine) (HR, 0.62) |
KIT | Imatinib | Guo et al. (38) | mPFS: 3.5 mo with 1-y OS rate of 51% |
Nilotinib | Guo et al. (78) | mPFS: 4.2 mo and mOS: 18.0 mo | |
TRK | Larotrectinib | Hong et al. (39) | ORR: 79% of TRK-fusion–positive cancers |
Entrectinib | Doebele et al. (40) | ORR: 57% of TRK-fusion–positive cancers |
HR = hazard ratio; mOS = median OS; mPFS = median PFS; ORR = overall response rate.