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TRKA (G595R/G667C)

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NTRK1 · Variant type: compound · HGVS: p.G595R;p.G667C

Components

p.G595Rp.G667C

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Ponatinib91.5%8.5%78.23
2Repotrectinib90.4%9.6%84.21
3Cabozantinib80.7%19.3%92.73
4Sorafenib60.3%39.7%96.72
5Defactinib39.4%60.6%92.68
6Regorafenib31.5%68.5%95.99
7Asciminib20.3%79.7%100.00
8Trametinib18.6%81.4%99.50
9Binimetinib16.8%83.2%100.00
10Ribociclib15.7%84.3%99.25
11Nintedanib15.6%84.4%90.23
12Lorlatinib13.4%86.6%97.24
13Imatinib12.7%87.3%99.00
14Futibatinib11.5%88.5%98.48
15Everolimus11.0%89.0%100.00
16Selumetinib10.8%89.2%100.00
17Dacomitinib10.1%89.9%97.99
18Pazopanib9.9%90.1%97.49
19Gefitinib9.8%90.2%99.25
20Duvelisib9.4%90.6%100.00
21Encorafenib9.2%90.8%98.50
22Leniolisib8.2%91.8%100.00
23Erdafitinib7.9%92.1%95.71
24Darovasertib7.3%92.7%96.99
25Temsirolimus6.2%93.8%100.00

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)
Ponatinib91.5%98.4%-6.9%
Repotrectinib90.4%98.9%-8.5%
Cabozantinib80.7%93.6%-12.9%
Sorafenib60.3%
Defactinib39.4%80.3%-40.9%
Regorafenib31.5%
Asciminib20.3%
Trametinib18.6%
Binimetinib16.8%
Ribociclib15.7%
Nintedanib15.6%93.8%-78.2%
Lorlatinib13.4%63.2%-49.8%
Imatinib12.7%
Futibatinib11.5%
Everolimus11.0%
Selumetinib10.8%
Dacomitinib10.1%
Pazopanib9.9%
Gefitinib9.8%
Duvelisib9.4%
Encorafenib9.2%
Leniolisib8.2%
Erdafitinib7.9%
Darovasertib7.3%
Temsirolimus6.2%

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