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TRKA (G595R/G667S)

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NTRK1 · Variant type: compound · HGVS: p.G595R;p.G667S

Components

p.G595Rp.G667S

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Repotrectinib100.0%0.0%84.21
2Ponatinib98.8%1.2%78.23
3Darovasertib92.2%7.8%96.99
4Cabozantinib88.0%12.0%92.73
5Entrectinib83.0%17.0%93.69
6Pralsetinib77.4%22.6%93.43
7Defactinib64.0%36.0%92.68
8Nintedanib39.4%60.6%90.23
9Sunitinib24.3%75.7%91.73
10Tenalisib21.4%78.6%97.98
11Asciminib17.4%82.6%100.00
12Fedratinib16.1%83.9%96.21
13Gilteritinib15.1%84.9%88.97
14Pacritinib12.4%87.6%88.64
15Everolimus11.0%89.0%100.00
16Axitinib10.3%89.7%93.23
17Bosutinib8.8%91.2%87.22
18Deucravacitinib8.7%91.3%98.99
19Pirtobrutinib8.1%91.9%99.49
20Erdafitinib8.0%92.0%95.71
21Ripretinib7.7%92.3%92.95
22Futibatinib7.7%92.3%98.48
23Ruxolitinib7.7%92.3%98.25
24Afatinib7.4%92.6%98.50
25Ribociclib7.3%92.7%99.25

Wild-type vs variant — drug response delta

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

DrugVariant inhWT inhΔ (variant − WT)
Repotrectinib100.0%98.9%+1.1%
Ponatinib98.8%98.4%+0.4%
Darovasertib92.2%
Cabozantinib88.0%93.6%-5.5%
Entrectinib83.0%99.0%-16.0%
Pralsetinib77.4%98.7%-21.2%
Defactinib64.0%80.3%-16.3%
Nintedanib39.4%93.8%-54.4%
Sunitinib24.3%82.8%-58.4%
Tenalisib21.4%59.0%-37.6%
Asciminib17.4%
Fedratinib16.1%56.2%-40.1%
Gilteritinib15.1%92.6%-77.5%
Pacritinib12.4%89.4%-77.1%
Everolimus11.0%
Axitinib10.3%
Bosutinib8.8%67.0%-58.2%
Deucravacitinib8.7%
Pirtobrutinib8.1%
Erdafitinib8.0%
Ripretinib7.7%93.6%-85.9%
Futibatinib7.7%
Ruxolitinib7.7%
Afatinib7.4%
Ribociclib7.3%

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