ARS-853 |
KRASG12C
|
Covalent inhibitor |
_ |
42 |
ARS-1620 |
KRASG12C
|
Covalent inhibitor |
_ |
43 |
AMG510 |
KRASG12C
|
Covalent inhibitor |
Locally advanced or metastatic NSCLC with KRASG12C mutation |
44, 45, 46
|
MRTX849 |
KRASG12C
|
Covalent inhibitor |
KRASG12C-mutated NSCLC |
47 |
PLX4720 |
BRAFV600E
|
An ATP-competitive RAF kinase inhibitor |
_ |
48 |
Vemurafenib |
BRAFV600E
|
An ATP-competitive RAF kinase inhibitor |
Metastatic melanoma with BRAFV600E mutation, Erdheim–Chester Disease with BRAFV600 mutation |
49, 50, 51
|
Dabrafenib |
BRAFV600E/K/D
|
An ATP-competitive RAF kinase inhibitor |
Unresectable or metastatic melanoma with BRAFV600E mutation |
52, 53, 54, 55, 56, 57, 58, 59
|
Encorafenib |
BRAFV600E/K
|
An ATP-competitive RAF kinase inhibitor |
Unresectable or metastatic melanoma with BRAFV600E/K mutation |
60 |
Trametinib |
MEK1/2 |
Allosteric non-ATP competitive inhibitor |
Unresectable or metastatic melanoma with BRAFV600E/K, BRAF positive anaplastic thyroid cancer, Metastatic NSCLC with BRAFV600E mutation |
61,62
|
Binimetinib |
MEK1/2 |
Allosteric inhibitor |
Unresectable or metastatic melanoma with BRAFV600E/K or NRAS mutation |
63,64
|
Cobimetinib |
MEK1/2 |
Allosteric inhibitor |
Advanced melanoma with BRAFV600E/K mutation |
65, 66, 67, 68, 69, 70, 71
|
ONC201 |
AKT/ERK |
_ |
Small cell lung cancer |
72, 73, 74, 75
|
LY3214996 |
ERK1/2 |
Reversible ATP-competitive kinase inhibitor |
_ |
76,77
|
Ulixertinib |
ERK1/2 |
Reversible ATP-competitive kinase inhibitor |
_ |
78, 79, 80, 81, 82
|
MK-8353 |
ERK1/2 |
Reversible ATP-competitive kinase inhibitor |
_ |
83, 84, 85, 86, 87
|
GDC-0994 |
ERK1/2 |
Reversible ATP-competitive kinase inhibitor |
_ |
88, 89, 90, 91
|
Rineterkib |
RAF/ERK1/2 |
_ |
_ |
92, 93, 94
|