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TRKA (G595R/A608D)

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NTRK1 · Variant type: compound · HGVS: p.G595R;p.A608D

Components

p.G595Rp.A608D

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Repotrectinib98.7%1.3%84.21
2Ponatinib95.3%4.7%78.23
3Entrectinib93.6%6.4%93.69
4Ripretinib81.8%18.3%92.95
5Cabozantinib76.5%23.5%92.73
6Darovasertib66.8%33.2%96.99
7Tivozanib43.7%56.3%92.42
8Pralsetinib38.0%62.0%93.43
9Defactinib30.8%69.2%92.68
10Alpelisib18.0%82.0%97.22
11Apatinib15.0%85.0%97.73
12Pexidartinib13.3%86.7%99.49
13Crizotinib12.7%87.3%91.39
14Abrocitinib12.1%87.9%99.50
15Upadacitinib11.7%88.3%97.98
16Bosutinib10.2%89.8%87.22
17Mitapivat9.4%90.6%100.00
18Tenalisib9.4%90.6%97.98
19Tucatinib9.3%90.7%99.75
20Umbralisib9.0%91.0%98.74
21Nintedanib8.8%91.3%90.23
22Tepotinib8.5%91.5%99.75
23Afatinib7.9%92.1%98.50
24Fedratinib7.8%92.2%96.21
25Ruxolitinib7.5%92.5%98.25

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)
Repotrectinib98.7%98.9%-0.2%
Ponatinib95.3%98.4%-3.0%
Entrectinib93.6%99.0%-5.4%
Ripretinib81.8%93.6%-11.8%
Cabozantinib76.5%93.6%-17.1%
Darovasertib66.8%
Tivozanib43.7%85.7%-42.0%
Pralsetinib38.0%98.7%-60.6%
Defactinib30.8%80.3%-49.5%
Alpelisib18.0%97.5%-79.5%
Apatinib15.0%
Pexidartinib13.3%
Crizotinib12.7%95.8%-83.1%
Abrocitinib12.1%
Upadacitinib11.7%
Bosutinib10.2%67.0%-56.8%
Mitapivat9.4%
Tenalisib9.4%59.0%-49.7%
Tucatinib9.3%
Umbralisib9.0%
Nintedanib8.8%93.8%-85.0%
Tepotinib8.5%
Afatinib7.9%
Fedratinib7.8%56.2%-48.4%
Ruxolitinib7.5%

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