EGFR (L858R)

EGFR · Variant type: point · HGVS: p.L858R

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Canertinib	99.9%	0.1%	96.49
2	Lazertinib	99.6%	0.4%	97.47
3	Neratinib	99.4%	0.6%	93.18
4	Mobocertinib	99.4%	0.6%	97.22
5	Erlotinib	99.2%	0.8%	99.75
6	Dacomitinib	99.1%	0.9%	97.99
7	Vandetanib	98.7%	1.3%	95.74
8	Pralsetinib	98.5%	1.5%	93.43
9	Osimertinib	98.2%	1.8%	97.24
10	Gefitinib	98.2%	1.8%	99.25
11	Afatinib	97.7%	2.3%	98.50
12	Brigatinib	96.8%	3.2%	82.96
13	Ibrutinib	95.9%	4.1%	94.74
14	Bosutinib	95.7%	4.3%	87.22
15	Fostamatinib	94.9%	5.1%	96.74
16	Dasatinib	88.8%	11.2%	87.97
17	Pacritinib	88.6%	11.4%	88.64
18	Lapatinib	85.8%	14.2%	99.25
19	Defactinib	80.4%	19.6%	92.68
20	Gilteritinib	77.2%	22.8%	88.97
21	Alpelisib	72.4%	27.6%	97.22
22	Alectinib	72.0%	28.0%	95.49
23	Capmatinib	67.0%	33.0%	99.75
24	Ponatinib	55.5%	44.5%	78.23
25	Darovasertib	44.2%	55.8%	96.99

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)
Canertinib	99.9%	98.4%	+1.4%
Lazertinib	99.6%	100.0%	-0.4%
Neratinib	99.4%	100.0%	-0.6%
Mobocertinib	99.4%	100.0%	-0.6%
Erlotinib	99.2%	99.4%	-0.2%
Dacomitinib	99.1%	99.8%	-0.7%
Vandetanib	98.7%	99.3%	-0.6%
Pralsetinib	98.5%	99.1%	-0.6%
Osimertinib	98.2%	99.1%	-0.9%
Gefitinib	98.2%	99.9%	-1.7%
Afatinib	97.7%	100.0%	-2.3%
Brigatinib	96.8%	98.5%	-1.6%
Ibrutinib	95.9%	99.3%	-3.4%
Bosutinib	95.7%	99.3%	-3.5%
Fostamatinib	94.9%	97.8%	-2.9%
Dasatinib	88.8%	97.9%	-9.2%
Pacritinib	88.6%	—	—
Lapatinib	85.8%	99.2%	-13.4%
Defactinib	80.4%	94.6%	-14.2%
Gilteritinib	77.2%	91.0%	-13.8%
Alpelisib	72.4%	—	—
Alectinib	72.0%	—	—
Capmatinib	67.0%	—	—
Ponatinib	55.5%	—	—
Darovasertib	44.2%	—	—

Cancer	Organ	Source
Lung Cancer	Lung	ref
carcinoma_lung	Lung	ref
other_lung	Lung	ref
carcinoma_breast	Breast	ref
carcinoma_large_intestine	Large Intestine	ref
carcinoma_oesophagus	Stomach/Digestive Tract	ref
Wilms_tumour_kidney	Kidney	ref
thymic_carcinoma_thymus	Thyroid	ref
carcinoma_thyroid	Thyroid	ref
carcinoma_upper_aerodigestive_tract	Brain/CNS	ref
carcinoma_ovary	Ovary	ref
carcinoma_NS	Other	ref
mesothelioma_peritoneum	Stomach/Digestive Tract	ref
other_skin	Skin	ref
carcinoma_prostate	Prostate	ref
carcinoma_stomach	Stomach/Digestive Tract	ref
thymoma_thymus	Thyroid	ref
carcinoma_small_intestine	Small Intestine	ref
LUAD-US	Lung	ref
LUSC-CN	Lung	ref
LUSC-KR	Lung	ref
LUAD	Lung	ref

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