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NSCLC常见驱动基因、变异形式以及目前国内外批准上市的药物

The common driver genes of NSCLC, variation types and drugs currently approved for sale

Driver genes	Variation types	Variationrates		Target inhibitors	IC50 value （nmol/L）	Approved by CFDA	Approved by FDA
		Asians	Caucasians
Y: yes; N: no; NR: not reported; a: EGFR sensitive mutation and T790M resistant mutation; b: EGFR L858R/T790M double mutations; c: T-DM1, ado-trastuzumab emtansine; d: L858R; e: recommended by NCCN guideline; f: dabrafenib combined with trametinib has been approved by FDA to treat NSCLC with BRAF V600E mutation; NSCLC: non-small cell lung cancer; NCCN: National Comprehensive Cancer Network; FDA: Food and Drug Administration; EGFR: epidermal growth factor receptor.
EGFR	Mutation	30%-40%[3, 4]	10%-15%[3, 4]	Gefitinib	2-37	Y	Y
				Erlotinib	2	Y	Y
				Icotinib	5	Y	N
				Afatinib	0.4d	Y	Y
				Osimertiniba	1	Y	Y
				Avitinibb	0.18	N	N
				Rociletiniba	62-187	N	N
ALK	Rearrangement	≤4%[3]		Crizotinib	24	Y	Y
				Ceritinib	0.2	N	Y
				Alectinib	1.9	N	Y
				Brigatinib	0.6	N	Y
				Ioratinib	0.7	N	N
ROS-1	Rearrangement	1%-3%[3]		Crizotinib	-	Y	Y
				loratinib	< 0.02	N	Ne
				Ceritinib	-	N	N
MET	Amplification	1%-7% primary or 20%		Crizotinib	11	N	Ne
		acquired[3]		Capmatinib	0.13±0.05	N	N
	Exon 14 skipping Mutation	3%[3]		Tivantinib	0.355 μmol/L (Ki)	N	N
HER-2	Amplification	2%[3, 4]		Afatinib	14	N	N
				Trastuzumab	NR	N	Ne
	Mutation	1.6%-4%[3]		T-DM1c	NR	N	N
BRAF	Mutation (V600E)	1.6%[5]	3.5%[5]	Vemurafenib	31	N	N
				Dabrafenib	0.6	N	Yf
RET	Rearrangement	0.7%-2%[7, 8]		Cabozantinib	4	N	N
				Vandetanib	40	N	N
MEK1/2	Mutation	1%[6]		Trametinib	2	N	N
				Selumetinib	14	N	N