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. 2022 May 20;10(1):76–88. doi: 10.1016/j.gendis.2022.05.006

Table 1.

Functional difference and FDA approved treatment of discussed inhibitors.

Inhibitors Specific target Mechanism FDA approved treatment Reference
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