Table 3.
Summary of Targeted Therapies.
| Reagent | Cancers | Class | FDA-approved indications for melanoma | Observed efficacy |
|---|---|---|---|---|
| Vemurafenib | • Melanoma | BRAF Inhibitor | BRAF-V600E/V600K mutated advanced melanoma (2011) | 84% 6-month OS rate; 48% response rate (phase III) 74 |
| Trametinib | • Melanoma | MEK inhibitor | BRAF-V600E/V600K mutated advanced melanoma (2013) | 81% 6-month OS rate; 4.8 months PFS (phase III) 77 |
| • Lung cancer | ||||
| • Thyroid cancer | ||||
| Dabrafenib | • Melanoma | BRAF inhibitor | BRAF-V600E/V600K mutated advanced melanoma (2013) | 18.2 months OS; 81 10.5 months PFS, 81 12% 5-year PFS rate; 82 24% 5-year OS rate 82 (phase III) |
| • Lung cancer | ||||
| Cobimetinib | • Melanoma | MEK inhibitor | Combination with vemurafenib for BRAF-V600E/V600K mutated melanoma (2015) | 22.3 months OS; (phase III), 9.9 months PFS (combination with vemurafenib) (phase III) 83 |
| Encorafenib | • Melanoma | BRAF inhibitor | Combination with binimetinib for BRAF V600E/V600K mutated melanoma (2018) | 23.5 months median OS; 87 9.6 months PFS (phase III) 86 |
| • Colorectal cancer | ||||
| Binimetinib | • Melanoma | MEK inhibitor | Combination with encorafenib for BRAF V600E/V600K mutated melanoma (2018) | 11 months median OS; 2.5 months PFS; 15.2% ORR (phase III) 89 |
| Sorafenib | • Melanoma | BRAF inhibitor | Not approved | 2.8% response rate (phase II) 91 |
| • Liver cancer | ||||
| • Thyroid cancer | ||||
| • Kidney cancer |