TRKA (L657M)

NTRK1 · Variant type: point · HGVS: p.L657M

Drug response on this variant

#	Drug	Inhibition on variant	Residual	KISS
1	Ponatinib	96.4%	3.6%	78.23
2	Entrectinib	95.0%	5.0%	93.69
3	Bosutinib	90.0%	10.0%	87.22
4	Crizotinib	88.7%	11.3%	91.39
5	Nintedanib	88.6%	11.4%	90.23
6	Repotrectinib	85.3%	14.7%	84.21
7	Cabozantinib	80.7%	19.3%	92.73
8	Pacritinib	79.1%	20.9%	88.64
9	Tivozanib	74.0%	26.0%	92.42
10	Pralsetinib	62.8%	37.2%	93.43
11	Sunitinib	61.7%	38.3%	91.73
12	Ripretinib	61.6%	38.4%	92.95
13	Gilteritinib	50.5%	49.5%	88.97
14	Defactinib	46.6%	53.4%	92.68
15	Brigatinib	37.5%	62.5%	82.96
16	Alectinib	37.4%	62.6%	95.49
17	Alpelisib	36.1%	63.9%	97.22
18	Darovasertib	33.8%	66.2%	96.99
19	Tenalisib	26.1%	73.9%	97.98
20	Neratinib	15.2%	84.8%	93.18
21	Tepotinib	10.8%	89.2%	99.75
22	Pirtobrutinib	10.8%	89.2%	99.49
23	Sorafenib	9.9%	90.1%	96.72
24	Abemaciclib	9.0%	91.0%	91.48
25	Selpercatinib	8.6%	91.4%	96.72

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)
Ponatinib	96.4%	98.4%	-2.0%
Entrectinib	95.0%	99.0%	-4.1%
Bosutinib	90.0%	67.0%	+23.0%
Crizotinib	88.7%	95.8%	-7.1%
Nintedanib	88.6%	93.8%	-5.2%
Repotrectinib	85.3%	98.9%	-13.6%
Cabozantinib	80.7%	93.6%	-12.9%
Pacritinib	79.1%	89.4%	-10.3%
Tivozanib	74.0%	85.7%	-11.6%
Pralsetinib	62.8%	98.7%	-35.8%
Sunitinib	61.7%	82.8%	-21.1%
Ripretinib	61.6%	93.6%	-32.0%
Gilteritinib	50.5%	92.6%	-42.1%
Defactinib	46.6%	80.3%	-33.8%
Brigatinib	37.5%	—	—
Alectinib	37.4%	—	—
Alpelisib	36.1%	97.5%	-61.4%
Darovasertib	33.8%	—	—
Tenalisib	26.1%	59.0%	-32.9%
Neratinib	15.2%	—	—
Tepotinib	10.8%	—	—
Pirtobrutinib	10.8%	—	—
Sorafenib	9.9%	—	—
Abemaciclib	9.0%	—	—
Selpercatinib	8.6%	—	—

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