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TRKA (G595R/L657M)

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NTRK1 · Variant type: compound · HGVS: p.G595R;p.L657M

Components

p.G595Rp.L657M

Drug response on this variant

#DrugInhibition on variantResidualKISS
1Repotrectinib96.0%4.0%84.21
2Ponatinib94.7%5.3%78.23
3Cabozantinib69.4%30.6%92.73
4Darovasertib58.1%41.9%96.99
5Tivozanib51.0%49.0%92.42
6Ripretinib26.8%73.2%92.95
7Defactinib19.8%80.2%92.68
8Pralsetinib10.4%89.6%93.43
9Brigatinib10.0%90.0%82.96
10Lorlatinib9.4%90.6%97.24
11Avapritinib9.4%90.6%97.73
12Zanubrutinib7.1%92.9%98.24
13Abrocitinib6.5%93.5%99.50
14Sorafenib6.3%93.7%96.72
15Tepotinib6.2%93.8%99.75
16Mitapivat6.0%94.0%100.00
17Vemurafenib5.8%94.2%96.49
18Upadacitinib5.6%94.4%97.98
19Tucatinib5.0%95.0%99.75
20Neratinib4.8%95.2%93.18
21Erdafitinib4.5%95.5%95.71
22Idelalisib4.3%95.7%100.00
23Pazopanib4.0%96.0%97.49
24Selumetinib4.0%96.0%100.00
25Ribociclib3.7%96.3%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)
Repotrectinib96.0%98.9%-2.9%
Ponatinib94.7%98.4%-3.6%
Cabozantinib69.4%93.6%-24.2%
Darovasertib58.1%
Tivozanib51.0%85.7%-34.6%
Ripretinib26.8%93.6%-66.8%
Defactinib19.8%80.3%-60.5%
Pralsetinib10.4%98.7%-88.3%
Brigatinib10.0%
Lorlatinib9.4%63.2%-53.9%
Avapritinib9.4%
Zanubrutinib7.1%
Abrocitinib6.5%
Sorafenib6.3%
Tepotinib6.2%
Mitapivat6.0%
Vemurafenib5.8%
Upadacitinib5.6%
Tucatinib5.0%
Neratinib4.8%
Erdafitinib4.5%
Idelalisib4.3%
Pazopanib4.0%
Selumetinib4.0%
Ribociclib3.7%

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