EGFR (T790M/C797S)

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

Components

p.T790Mp.C797S

#	Drug	Inhibition on variant	Residual	KISS
1	Brigatinib	99.1%	0.9%	82.96
2	Dacomitinib	92.5%	7.5%	97.99
3	Pacritinib	91.0%	9.1%	88.64
4	Gilteritinib	90.1%	9.9%	88.97
5	Afatinib	89.8%	10.2%	98.50
6	Neratinib	89.5%	10.5%	93.18
7	Fostamatinib	85.9%	14.1%	96.74
8	Canertinib	82.2%	17.8%	96.49
9	Vandetanib	65.0%	35.0%	95.74
10	Pirtobrutinib	63.7%	36.3%	99.49
11	Lazertinib	62.5%	37.5%	97.47
12	Entrectinib	61.1%	38.9%	93.69
13	Gefitinib	60.1%	39.9%	99.25
14	Erlotinib	58.0%	42.0%	99.75
15	Alectinib	41.7%	58.3%	95.49
16	Defactinib	41.7%	58.3%	92.68
17	Mobocertinib	41.7%	58.3%	97.22
18	Ibrutinib	40.4%	59.6%	94.74
19	Lorlatinib	37.9%	62.1%	97.24
20	Fedratinib	37.6%	62.4%	96.21
21	Pralsetinib	37.4%	62.6%	93.43
22	Ceritinib	33.3%	66.7%	95.44
23	Bosutinib	33.3%	66.7%	87.22
24	Repotrectinib	32.7%	67.3%	84.21
25	Osimertinib	29.7%	70.3%	97.24

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)
Brigatinib	99.1%	98.5%	+0.7%
Dacomitinib	92.5%	99.8%	-7.3%
Pacritinib	91.0%	—	—
Gilteritinib	90.1%	91.0%	-1.0%
Afatinib	89.8%	100.0%	-10.2%
Neratinib	89.5%	100.0%	-10.5%
Fostamatinib	85.9%	97.8%	-11.9%
Canertinib	82.2%	98.4%	-16.3%
Vandetanib	65.0%	99.3%	-34.4%
Pirtobrutinib	63.7%	—	—
Lazertinib	62.5%	100.0%	-37.5%
Entrectinib	61.1%	—	—
Gefitinib	60.1%	99.9%	-39.8%
Erlotinib	58.0%	99.4%	-41.4%
Alectinib	41.7%	—	—
Defactinib	41.7%	94.6%	-52.9%
Mobocertinib	41.7%	100.0%	-58.3%
Ibrutinib	40.4%	99.3%	-59.0%
Lorlatinib	37.9%	—	—
Fedratinib	37.6%	—	—
Pralsetinib	37.4%	99.1%	-61.8%
Ceritinib	33.3%	—	—
Bosutinib	33.3%	99.3%	-66.0%
Repotrectinib	32.7%	—	—
Osimertinib	29.7%	99.1%	-69.4%

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