ALK Inhibitor TAE684

ALK I11711
ALK Inhibitor TAE684	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	accepted	EID1285 The I1171T ALK kinase domain mutaion was found in the MGH056-1 cell line which was derived from an ALK rearranged NSCLC patient who had progressed on crizotinib and then on alectinib given at lower do… (full text at CIViC) PMID 25228534 · Katayama et al., 2014 · Open in CIViC	civic

ALK I11711

Lung Non-Small Cell CarcinomaCURATED_BROADER

Predictive

Supports Sensitivity Response

accepted

EID1285

The I1171T ALK kinase domain mutaion was found in the MGH056-1 cell line which was derived from an ALK rearranged NSCLC patient who had progressed on crizotinib and then on alectinib given at lower do… (full text at CIViC)

PMID 25228534 · Katayama et al., 2014 · Open in CIViC

ALK e6::e202
ALK Inhibitor TAE684	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	2	accepted	EID1194 In a panel of 602 cancer cell lines, 3/134 NSCLC cell lines showed <0.5% cell viability following treatment with the ALK inhibitor TAE684. Of these, NCI-H2228 harbored EML4-ALK variant 3a/b (EML4 exon… (full text at CIViC) PMID 18451166 · McDermott et al., 2008 · Open in CIViC	civic
〃	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Does Not Support Sensitivity Response	2	accepted	EID1195 Exon-array and RT-PCR was used to screen a panel of 83 NSCLC cell lines for EML4-ALK variants. The cell lines NCI-H3122 (containing EML4-ALK variant 1) and NCI-H2228 (containing the EML4 exon 6 and AL… (full text at CIViC) PMID 18594010 · Koivunen et al., 2008 · Open in CIViC	civic

ALK e6::e202

Lung Non-Small Cell CarcinomaCURATED_BROADER

Predictive

Supports Sensitivity Response

accepted

EID1194

In a panel of 602 cancer cell lines, 3/134 NSCLC cell lines showed <0.5% cell viability following treatment with the ALK inhibitor TAE684. Of these, NCI-H2228 harbored EML4-ALK variant 3a/b (EML4 exon… (full text at CIViC)

PMID 18451166 · McDermott et al., 2008 · Open in CIViC

〃

Lung Non-Small Cell CarcinomaCURATED_BROADER

Predictive

Does Not Support Sensitivity Response

accepted

EID1195

Exon-array and RT-PCR was used to screen a panel of 83 NSCLC cell lines for EML4-ALK variants. The cell lines NCI-H3122 (containing EML4-ALK variant 1) and NCI-H2228 (containing the EML4 exon 6 and AL… (full text at CIViC)

PMID 18594010 · Koivunen et al., 2008 · Open in CIViC

ALK T1151dup + ALK Fusion1
ALK Inhibitor TAE684	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Resistance	3	accepted	EID1348 Treatment of Ba/F3 cells expressing EML4-ALK 1151 insT with TAE684 produced an IC50 value (28.3 nM) 20x higher cells expressing EML4-ALK wildtype variant 1. The crizotinib resistant clones were produc… (full text at CIViC) PMID 22277784 · Katayama et al., 2012 · Open in CIViC	civic

ALK T1151dup + ALK Fusion1

Lung Non-Small Cell CarcinomaCURATED_BROADER

Predictive

Supports Resistance

accepted

EID1348

Treatment of Ba/F3 cells expressing EML4-ALK 1151 insT with TAE684 produced an IC50 value (28.3 nM) 20x higher cells expressing EML4-ALK wildtype variant 1. The crizotinib resistant clones were produc… (full text at CIViC)

PMID 22277784 · Katayama et al., 2012 · Open in CIViC

ALK V1180L + ALK Fusion1
ALK Inhibitor TAE684	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Sensitivity Response	3	accepted	EID1290 The V1180L mutation in the kinase domain of rearranged ALK was found in an alectinib resistant cell line named H3122 CHR-A1, which was derived from the alectinib sensitive EML4-ALK variant 1 containin… (full text at CIViC) PMID 25228534 · Katayama et al., 2014 · Open in CIViC	civic

ALK V1180L + ALK Fusion1

Lung Non-Small Cell CarcinomaCURATED_BROADER

Predictive

Supports Sensitivity Response

accepted

EID1290

The V1180L mutation in the kinase domain of rearranged ALK was found in an alectinib resistant cell line named H3122 CHR-A1, which was derived from the alectinib sensitive EML4-ALK variant 1 containin… (full text at CIViC)

PMID 25228534 · Katayama et al., 2014 · Open in CIViC

ROS1 Fusion + ROS1 L2155S1
ALK Inhibitor TAE684 + Crizotinib + ForetinibSubstitutes	Lung Non-Small Cell CarcinomaCURATED_BROADER	Predictive	D	Supports Resistance	3	accepted	EID1256 The L2155S mutation in ROS1 was identified in the HCC78CR1, -2 and -3 cell lines which harbor the SLC34A2–ROS1 rearrangement and in 2 patients with NSCLC with progressive disease following crizotinib … (full text at CIViC) PMID 25688157 · Song et al., 2015 · Open in CIViC	civic

ROS1 Fusion + ROS1 L2155S1

ALK Inhibitor TAE684 + Crizotinib + ForetinibSubstitutes

Lung Non-Small Cell CarcinomaCURATED_BROADER

Predictive

Supports Resistance

accepted

EID1256

The L2155S mutation in ROS1 was identified in the HCC78CR1, -2 and -3 cell lines which harbor the SLC34A2–ROS1 rearrangement and in 2 patients with NSCLC with progressive disease following crizotinib … (full text at CIViC)

PMID 25688157 · Song et al., 2015 · Open in CIViC

ALK C1156Y + ALK Fusion1
ALK Inhibitor TAE684	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	submitted	EID11078 From a mutation assay that generated crizotinib resistant mutations in EML4::ALK, the five most resistant mutations found were introduced into Ba/F3 cells and tested with the ALK inhibitor TAE684. EML… (full text at CIViC) PMID 22034911 · Zhang et al., 2011 · Open in CIViC	civic

ALK C1156Y + ALK Fusion1

Predictive

Supports Sensitivity Response

submitted

EID11078

From a mutation assay that generated crizotinib resistant mutations in EML4::ALK, the five most resistant mutations found were introduced into Ba/F3 cells and tested with the ALK inhibitor TAE684. EML… (full text at CIViC)

PMID 22034911 · Zhang et al., 2011 · Open in CIViC

ALK F1174C + ALK Fusion1
ALK Inhibitor TAE684	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	submitted	EID11079 From a mutation assay that generated crizotinib resistant mutations in EML4::ALK, the five most resistant mutations found were introduced into Ba/F3 cells and tested with the ALK inhibitor TAE684. EML… (full text at CIViC) PMID 22034911 · Zhang et al., 2011 · Open in CIViC	civic

ALK F1174C + ALK Fusion1

Predictive

Supports Sensitivity Response

submitted

EID11079

PMID 22034911 · Zhang et al., 2011 · Open in CIViC

ALK G1269S + ALK Fusion1
ALK Inhibitor TAE684	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	submitted	EID11077 From a mutation assay that generated crizotinib resistant mutations in EML4::ALK, the five most resistant mutations found were introduced into Ba/F3 cells and tested with the ALK inhibitor TAE684. EML… (full text at CIViC) PMID 22034911 · Zhang et al., 2011 · Open in CIViC	civic

ALK G1269S + ALK Fusion1

Predictive

Supports Sensitivity Response

submitted

EID11077

PMID 22034911 · Zhang et al., 2011 · Open in CIViC

ALK L1196M + ALK Fusion1
ALK Inhibitor TAE684	Malignant NeoplasmALIAS	Predictive	D	Supports Sensitivity Response	3	submitted	EID11080 From a mutation assay that generated crizotinib resistant mutations in EML4::ALK, the five most resistant mutations found were introduced into Ba/F3 cells and tested with the ALK inhibitor TAE684. EML… (full text at CIViC) PMID 22034911 · Zhang et al., 2011 · Open in CIViC	civic

ALK L1196M + ALK Fusion1

Predictive

Supports Sensitivity Response

submitted

EID11080

PMID 22034911 · Zhang et al., 2011 · Open in CIViC

ALK S1206R + ALK Fusion1
ALK Inhibitor TAE684	Malignant NeoplasmALIAS	Predictive	D	Does Not Support Sensitivity Response	2	submitted	EID11081 From a mutation assay that generated crizotinib resistant mutations in EML4::ALK, the five most resistant mutations found were introduced into Ba/F3 cells and tested with the ALK inhibitor TAE684. EML… (full text at CIViC) PMID 22034911 · Zhang et al., 2011 · Open in CIViC	civic

ALK S1206R + ALK Fusion1

Predictive

Does Not Support Sensitivity Response

submitted

EID11081

PMID 22034911 · Zhang et al., 2011 · Open in CIViC

ALK F1174L1
ALK Inhibitor TAE684	Neuroblastoma	Predictive	D	Supports Sensitivity Response	4	accepted	EID142 SH-SY5Y and Kelly cells with mutant ALK (F1174L) and Ba/F3 cells overexpressing ALK harboring the F1174L mutation are sensitive to TAE684-mediated growth inhibition. PMID 18923525 · George et al., 2008 · Open in CIViC	civic

ALK F1174L1

Neuroblastoma

Predictive

Supports Sensitivity Response

accepted

EID142

SH-SY5Y and Kelly cells with mutant ALK (F1174L) and Ba/F3 cells overexpressing ALK harboring the F1174L mutation are sensitive to TAE684-mediated growth inhibition.

PMID 18923525 · George et al., 2008 · Open in CIViC

ALK R1275Q2
ALK Inhibitor TAE684	Neuroblastoma	Predictive	D	Supports Sensitivity Response	2	accepted	EID39 This study identified previously unknown mutations in the ALK gene in 8% (7/93) of primary neuroblastomas and neuroblastoma cell lines (6/30). R1275Q was found in the germline of one patient sample an… (full text at CIViC) PMID 18923525 · George et al., 2008 · Open in CIViC	civic
〃	Neuroblastoma	Predictive	D	Supports Resistance	3	accepted	EID48 The SMS-KCNR cell line harboring the R1275Q mutation was resistant to TAE684. PMID 18923525 · George et al., 2008 · Open in CIViC	civic

ALK R1275Q2

Neuroblastoma

Predictive

Supports Sensitivity Response

accepted

EID39

This study identified previously unknown mutations in the ALK gene in 8% (7/93) of primary neuroblastomas and neuroblastoma cell lines (6/30). R1275Q was found in the germline of one patient sample an… (full text at CIViC)

PMID 18923525 · George et al., 2008 · Open in CIViC

〃

Neuroblastoma

Predictive

Supports Resistance

accepted

EID48

The SMS-KCNR cell line harboring the R1275Q mutation was resistant to TAE684.

PMID 18923525 · George et al., 2008 · Open in CIViC