EGFR (T790M/L792F/C797S/L858R)

EGFR · Variant type: compound · HGVS: p.T790M;p.L792F;p.C797S;p.L858R

Components

p.T790Mp.L792Fp.C797Sp.L858R

#	Drug	Inhibition on variant	Residual	KISS
1	Dacomitinib	98.9%	1.1%	97.99
2	Ibrutinib	98.5%	1.5%	94.74
3	Lapatinib	98.5%	1.5%	99.25
4	Brigatinib	95.1%	4.9%	82.96
5	Pacritinib	94.8%	5.2%	88.64
6	Fostamatinib	91.9%	8.1%	96.74
7	Alectinib	88.4%	11.6%	95.49
8	Gilteritinib	87.0%	13.0%	88.97
9	Deucravacitinib	81.8%	18.2%	98.99
10	Lazertinib	70.8%	29.2%	97.47
11	Pralsetinib	58.4%	41.6%	93.43
12	Neratinib	53.5%	46.5%	93.18
13	Defactinib	48.9%	51.1%	92.68
14	Sunitinib	47.6%	52.4%	91.73
15	Vandetanib	44.9%	55.1%	95.74
16	Entrectinib	44.6%	55.4%	93.69
17	Avapritinib	44.2%	55.8%	97.73
18	Fedratinib	43.5%	56.5%	96.21
19	Canertinib	40.4%	59.6%	96.49
20	Repotrectinib	39.0%	61.0%	84.21
21	Erlotinib	37.8%	62.2%	99.75
22	Cabozantinib	35.7%	64.3%	92.73
23	Regorafenib	27.6%	72.4%	95.99
24	Tepotinib	27.5%	72.5%	99.75
25	Everolimus	20.7%	79.3%	100.00

Positive Δ means the drug hits the variant harder than wild-type (mutation-selective); negative Δ means it loses potency (resistance).

Drug	Variant inh	WT inh	Δ (variant − WT)
Dacomitinib	98.9%	99.8%	-0.9%
Ibrutinib	98.5%	99.3%	-0.9%
Lapatinib	98.5%	99.2%	-0.7%
Brigatinib	95.1%	98.5%	-3.3%
Pacritinib	94.8%	—	—
Fostamatinib	91.9%	97.8%	-5.8%
Alectinib	88.4%	—	—
Gilteritinib	87.0%	91.0%	-4.1%
Deucravacitinib	81.8%	—	—
Lazertinib	70.8%	100.0%	-29.2%
Pralsetinib	58.4%	99.1%	-40.8%
Neratinib	53.5%	100.0%	-46.5%
Defactinib	48.9%	94.6%	-45.7%
Sunitinib	47.6%	—	—
Vandetanib	44.9%	99.3%	-54.4%
Entrectinib	44.6%	—	—
Avapritinib	44.2%	—	—
Fedratinib	43.5%	—	—
Canertinib	40.4%	98.4%	-58.0%
Repotrectinib	39.0%	—	—
Erlotinib	37.8%	99.4%	-61.7%
Cabozantinib	35.7%	—	—
Regorafenib	27.6%	—	—
Tepotinib	27.5%	—	—
Everolimus	20.7%	—	—

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