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| Therapy Name | Ceritinib |
| Synonyms | |
| Therapy Description |
Zykadia (ceritinib) inhibits ALK, including ALK mutations and fusions, and has additional activity against ROS1 fusions, potentially resulting in decreased tumor cell growth (PMID: 25322323, PMID: 26372962). Zykadia (ceritinib) is FDA approved for ALK-positive (rearrangements and fusions) metastatic non-small cell lung cancer (FDA.gov). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Ceritinib | Zykadia | LDK378 | ALK Inhibitor 32 ROS1 Inhibitor 20 | Zykadia (ceritinib) inhibits ALK, including ALK mutations and fusions, and has additional activity against ROS1 fusions, potentially resulting in decreased tumor cell growth (PMID: 25322323, PMID: 26372962). Zykadia (ceritinib) is FDA approved for ALK-positive (rearrangements and fusions) metastatic non-small cell lung cancer (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| ALK F1245I | neuroblastoma | sensitive | Ceritinib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of patient-derived neuroblastoma cells harboring ALK F1245I in culture and inhibited tumor growth in a patient-derived xenograft model (PMID: 37523146). | 37523146 |
| ALK rearrange ALK G1202R | lung non-small cell carcinoma | predicted - resistant | Ceritinib | Clinical Study - Cohort | Actionable | In a retrospective study, ALK G1202R was identified in 33% (23/70) of plasma samples at disease progression in ALK-positive non-small cell lung cancer patients who received second-generation ALK TKI treatment, including Alecensa (alectinib) (n=46), Zykadia (ceritinib) (n=4), Alunbrig (brigatinib) (n=3), Ensartinib (X-396) (n=1), or more than 2 lines of TKIs (n=16) (PMID: 31358542). | 31358542 |
| EML4 - ALK ALK E1210K | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells co-expressing EML4-ALK and ALK E1210K demonstrated sensitivity to treatment with Zykadia (ceritinib) in culture (PMID: 27432227). | 27432227 |
| EML4 - ALK ALK F1174V ALK G1202R | lung non-small cell carcinoma | sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, a non-small cell lung carcinoma patient harboring EML4-ALK who was previously treated with Xalkori (crizotinib) and subsequently developed the resistance mutation, ALK G1269A, was treated with Zykadia (ceritinib), later progressed, and was found to have lost ALK G1269A, but gained ALK F1174V and ALK G1202R (PMID: 24675041). | 24675041 |
| ALK rearrange ALK mut | lung non-small cell carcinoma | sensitive | Ceritinib | Clinical Study - Cohort | Actionable | In a retrospective analysis, patients with ALK-rearrangement positive non-small cell lung cancer who acquired ALK drug resistance mutations following Xalkori (crizotinib) treatment had a median progression-free survival (mPFS) of 5.4 months on Zykadia (ceritinib), which was not significantly different than the mPFS of 6.5 months for patients without ALK mutations (PMID: 25724526). | 25724526 |
| EML4 - ALK ALK G1269A | lung adenocarcinoma | sensitive | Ceritinib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) treatment inhibited viability of patient-derived organoids of lung adenocarcinoma harboring EML4-ALK and ALK G1269A in culture and resulted in tumor shrinkage in a patient-derived xenograft (PDX) model (PMID: 38360931). | 38360931 |
| ALK rearrange ALK L1196M ALK D1203N | lung adenocarcinoma | predicted - resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, Zykadia (ceritinib) treatment resulted in disease progression after 5 months of therapy in a patient with lung adenocarcinoma harboring ALK rearrangement and an acquired ALK L1196M, ALK D1203N was detected in the biopsies at disease progression (PMID: 31585938). | 31585938 |
| EML4 - ALK | mucosal melanoma | sensitive | Ceritinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zykadia (ceritinib) decreased viability of a mucosal melanoma cell line harboring EML4-ALK in culture and inhibited tumor growth in a cell line xenograft model (PMID: 29054983). | 29054983 |
| ALK F1174L | neuroblastoma | sensitive | Ceritinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited downstream signaling and viability in neuroblastoma cell lines harboring ALK F1174L in culture and reduced cell invasion in a cell line xenograft model (PMID: 38032104). | 38032104 |
| EML4 - ALK ALK C1156Y | lung non-small cell carcinoma | conflicting | Ceritinib | Case Reports/Case Series | Actionable | In a Phase I trial, Zykadia (ceritinib) treatment resulted in a partial response in a patient with non-small cell lung cancer harboring EML4-ALK (e18:e20) and ALK C1156Y (PMID: 34890832; NCT01283516). | 34890832 |
| EML4 - ALK ALK C1156Y | lung non-small cell carcinoma | conflicting | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with EML4-ALK positive non-small cell lung cancer with a secondary Xalkori (crizotinib) resistance mutation C1156Y, did not respond to Zykadia (ceritinib) therapy (PMID: 26698910). | 26698910 |
| EML4 - ALK ALK C1156Y | lung non-small cell carcinoma | conflicting | Ceritinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zykadia (ceritinib) demonstrated tumor growth inhibition in xenograft models of a human non-small cell lung cancer cell line harboring EML4-ALK with ALK C1156Y when compared to Xalkori (crizotinib) (PMID: 24675041). | 24675041 |
| EML4 - ALK ALK L1152R | lung cancer | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, lung cancer cells expressing ALK L1152R in the context of EML4-ALK demonstrated resistance to Zykadia (ceritinib) treatment in culture (PMID: 31925410). | 31925410 |
| ALK rearrange TP53 mut | lung non-small cell carcinoma | decreased response | Ceritinib | Clinical Study - Cohort | Actionable | In a clinical study, TP53 mutant ALK-rearranged non-small cell lung cancer patients demonstrated a lower median progression-free survival following treatment with Zykadia (ceritinib), Alecensa (alectinib), or Alunbrig (brigatinib) after Xalkori (crizotinib) vs. patients with wild-type TP53 (5.4 mo. vs. 9.9 mo.; p=0.039), and a lower median overall survival with treatment with Zykadia (ceritinib) after Xalkori (crizotinib) of 7.0 mo. vs. 50.0 mo. in patients with wild-type TP53 (p=0.001) (PMID: 30165392). | 30165392 |
| EML4 - ALK ALK V1180L | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of a cell line expressing EML4-ALK with ALK V1180L in culture (PMID: 31446141). | 31446141 |
| EML4 - ALK ALK V1180L | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited growth of a transformed cell line expressing EML4-ALK with ALK V1180L in culture (PMID: 25228534). | 25228534 |
| EML4 - ALK ALK V1180L | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK V1180L in culture (PMID: 33627640). | 33627640 |
| ALK fusion ALK T1151dup | lung non-small cell carcinoma | no benefit | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, Zykadia (ceritinib) treatment did not result in disease control in a patient with non-small cell lung cancer and uterine metastasis harboring an ALK fusion and ALK T1151dup (reported as ALK 1151Tins) whose disease progressed after prior Xalkori (crizotinib) and Alecensa (alectinib) treatments (PMID: 34184417). | 34184417 |
| ROS1 rearrange | lung non-small cell carcinoma | sensitive | Ceritinib | Phase II | Actionable | In a Phase II trial, treatment with Zykadia (ceritinib) resulted in an overall response rate of 62% (20/32, including 1 complete response), a disease control rate of 81% (26/32), and a progression-free survival of 9.3 months in all patients and 19.3 months in Xalkori (crizotinib)-naive patients with non-small cell lung cancer harboring a ROS1 rearrangement (PMID: 28520527; NCT01964157). | 28520527 |
| ROS1 rearrange | lung non-small cell carcinoma | sensitive | Ceritinib | Guideline | Actionable | Zykadia (ceritinib) is included in guidelines for patients with metastatic non-small cell lung cancer harboring a ROS1 rearrangement who have not received prior Xalkori (crizotinib) therapy (PMID: 30285222; ESMO.org). | 30285222 detail... |
| ROS1 rearrange | lung non-small cell carcinoma | sensitive | Ceritinib | Guideline | Actionable | Zykadia (ceritinib) is included in guidelines as first-line therapy for ROS1-rearranged non-small cell lung cancer, but is not indicated after patients become resistant to Xalkori (crizotinib) (NCCN.org). | detail... |
| ALK rearrange ALK G1123S | lung adenocarcinoma | predicted - resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, ALK G1123S was identified as an acquired mutation in a patient with ALK-rearranged lung adenocarcinoma whose disease relapsed 2 years after initial response to Zykadia (ceritinib) (PMID: 26134233). | 26134233 |
| EML4 - ALK ALK I1171S | Advanced Solid Tumor | conflicting | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171S in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK I1171S | Advanced Solid Tumor | conflicting | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited growth of transformed cells expressing EML4-ALK with ALK I1171S in culture (PMID: 27432227). | 27432227 |
| EML4 - ALK ALK I1171S | Advanced Solid Tumor | conflicting | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) reduced ALK phosphorylation and inhibited growth of transformed cells expressing EML4-ALK with ALK I1171S in culture (PMID: 31943796). | 31943796 |
| EML4 - ALK ALK I1171S | Advanced Solid Tumor | conflicting | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK I1171S were resistant to Zykadia (ceritinib)-mediated growth inhibition in culture (PMID: 27009859). | 27009859 |
| EML4 - ALK ALK I1171N | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells co-expressing EML4-ALK and ALK I1171N demonstrated sensitivity to treatment with Zykadia (ceritinib) in culture (PMID: 27432227). | 27432227 |
| EML4 - ALK ALK I1171N | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK L1256F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK L1256F were resistant to treatment with Zykadia (ceritinib) in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK G1202R ALK G1269A | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK G1202R and G1269A compound mutation in the context of EML4-ALK were resistant to Zykadia (ceritinib) treatment in culture (PMID: 34158340). | 34158340 |
| EML4 - ALK ALK D1203N ALK F1245V | Advanced Solid Tumor | predicted - resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK D1203N and F1245V demonstrated resistance to treatment with Zykadia (ceritinib) in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK T1151M | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cell lines harboring EML4-ALK with ALK T1151M were resistant to Zykadia (ceritinib) in culture (PMID: 27009859). | 27009859 |
| ALK rearrange ALK F1174L | lung adenocarcinoma | predicted - resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, ALK F1174L was identified in biopsies at disease progression after 4 months of Zykadia (ceritinib) treatment in a patient with lung adenocarcinoma harboring ALK rearrangement (PMID: 31585938). | 31585938 |
| ALK positive | neuroblastoma | predicted - sensitive | Ceritinib | Phase I | Actionable | In a Phase I trial, Zykadia (ceritinib) treatment was well tolerated and resulted in an overall response rate of 20% (6/30; 6 partial response), a disease control rate of 53% (16/30), and a median progression-free survival of 2.4 months in pediatric patients with ALK-positive neuroblastoma (PMID: 34780709; NCT01742286). | 34780709 |
| ALK rearrange ALK I1171X | lung non-small cell carcinoma | predicted - resistant | Ceritinib | Clinical Study - Cohort | Actionable | In a retrospective study, ALK I1171X was identified in 24% (17/70) of plasma samples at disease progression in ALK-positive non-small cell lung cancer patients who received second-generation ALK TKI treatment, including Alecensa (alectinib) (n=46), Zykadia (ceritinib) (n=4), Alunbrig (brigatinib) (n=3), Ensartinib (X-396) (n=1), or more than 2 lines of TKIs (n=16) (PMID: 31358542). | 31358542 |
| EML4 - ALK ALK F1174L ALK S1189C | lung adenocarcinoma | predicted - resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with lung adenocarcinoma harboring EML4-ALK along with ALK F1174L in cis with ALK S1189C did not respond to second-line Zykadia (ceritinib) treatment (PMID: 36506539). | 36506539 |
| EML4 - ALK ALK L1198F ALK G1202R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK G1202R and L1198F compound mutation in the context of EML4-ALK were resistant to Zykadia (ceritinib) treatment in culture (PMID: 34158340). | 34158340 |
| EML4 - ALK ALK L1198F ALK G1202R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK L1198F and G1202R were resistant to treatment with Zykadia (ceritinib) in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK L1198F ALK G1202R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R and ALK L1198F displayed enhanced resistance to growth inhibition mediated by Zykadia (ceritinib) in culture (PMID: 26698910). | 26698910 |
| ALK rearrange | lung non-squamous non-small cell carcinoma | sensitive | Ceritinib | Phase III | Actionable | In a Phase III trial, first-line treatment with Zykadia (ceritinib) resulted in an improved median progression-free survival of 16.6 months, compared to 8.1 months with chemotherapy, in patients with ALK-rearranged non-squamous non-small cell lung cancer (PMID: 28126333; NCT01828099). | 28126333 |
| EML4 - ALK ALK G1269A | lung non-small cell carcinoma | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, human lung cancer cell lines harboring EML4-ALK with ALK G1269A demonstrated sensitivity to Zykadia (ceritinib) in culture (PMID: 24675041). | 24675041 |
| EML4 - ALK ALK L1196M | lung non-small cell carcinoma | sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a Phase I trial, Zykadia (ceritinib) treatment resulted in 1 partial response and 1 patient with stable disease among 2 patients with non-small cell lung cancer harboring EML4-ALK (e13:e20) and ALK L1196M (PMID: 34890832; NCT01283516). | 34890832 |
| EML4 - ALK ALK L1196M | lung non-small cell carcinoma | sensitive | Ceritinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited cell survival and PI3K/AKT, MEK/ERK, and mTOR signaling in two human non-small cell lung carcinoma cell lines harboring the Xalkori (crizotinib) resistance mutation EML4-ALK ALK L1196M in culture and inhibited tumor growth in xenograft models of one of those cell lines (PMID: 24675041). | 24675041 |
| EML4 - ALK ALK S1206Y | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK S1206Y demonstrated growth inhibition with Zykadia (ceritinib) treatment in culture (PMID: 24675041). | 24675041 |
| EML4 - ALK ALK S1206Y | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited proliferation of transformed cells expressing EML4-ALK with ALK S1206Y in culture (PMID: 25727400). | 25727400 |
| ROS1 fusion ROS1 L1951R ROS1 L2026M | lung non-small cell carcinoma | resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical study, a non-small cell lung carcinoma patient co-harboring a ROS1 fusion, and two other mutations in trans, ROS1 L2026M, and ROS1 L1951R demonstrated resistance to treatment with Zykadia (ceritinib), and cells derived from this patient showed partially decreased SHP2 and ERK1/2 signaling and ROS1 activation (PMID: 29636358). | 29636358 |
| EML4 - ALK ALK C1156Y ALK L1198F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK C1156Y and ALK L1198F were resistant to growth inhibition mediated by Zykadia (ceritinib) in culture (PMID: 26698910). | 26698910 |
| EML4 - ALK ALK C1156Y ALK L1198F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK C1156Y and ALK L1198F were resistant to Zykadia (ceritinib) in culture (PMID: 35726063). | 35726063 |
| EML4 - ALK ALK C1156Y ALK L1198F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK C1156Y and L1198F compound mutation in the context of EML4-ALK were resistant to Zykadia (ceritinib) treatment in culture (PMID: 34158340). | 34158340 |
| EML4 - ALK ALK G1202del | Advanced Solid Tumor | decreased response | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells co-expressing EML4-ALK and ALK G1202del demonstrated a decreased response to treatment with Zykadia (ceritinib) in culture (PMID: 27432227). | 27432227 |
| ALK fusion | lung non-small cell carcinoma | sensitive | Ceritinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase I trial that supported FDA approval, Zykadia (ceritinib) resulted in a blinded independent review committee (BIRC)-assessed objective response rate of 44% (72/163) and a duration of response of 7.1 months in ALK-rearranged non-small cell lung cancer patients (PMID: 25754348; NCT01283516). | detail... detail... 25754348 |
| EML4 - ALK ALK L1198F | Advanced Solid Tumor | conflicting | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with L1198F were resistant to growth inhibition mediated by Zykadia (ceritinib) in culture (PMID: 26698910). | 26698910 |
| EML4 - ALK ALK L1198F | Advanced Solid Tumor | conflicting | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK L1198F in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK L1198F | Advanced Solid Tumor | conflicting | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, a cell line expressing EML4-ALK with ALK L1198F was resistant to Zykadia (ceritinib) in culture (PMID: 31446141). | 31446141 |
| EML4 - ALK ALK L1196M ALK D1203N | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK L1196M and D1203N were resistant to treatment with Zykadia (ceritinib) in culture (PMID: 33627640). | 33627640 |
| ALK R1275Q | neuroblastoma | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) decreased viability of neuroblastoma cell lines harboring ALK R1275Q in culture (PMID: 38032104). | 38032104 |
| ALK R1275Q | neuroblastoma | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited proliferation of neuroblastoma cells harboring ALK R1275Q in culture (PMID: 29907598). | 29907598 |
| ALK R1275Q | neuroblastoma | sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a Phase I trial, Zykadia (ceritinib) treatment resulted in 3 partial responses and 1 stable disease in 7 pediatric patients with neuroblastoma harboring ALK R1275Q (PMID: 34780709; NCT01742286). | 34780709 |
| EML4 - ALK | lung adenocarcinoma | predicted - sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, Zykadia (ceritinib) treatment in a pediatric patient with metastatic lung adenocarcinoma harboring EML4-ALK resulted in a very good partial response at 2 months with regression of enlarged lymph nodes, with a near-complete response after 18 months of treatment (PMID: 36640634). | 36640634 |
| EML4 - ALK | lung adenocarcinoma | predicted - sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, Zykadia (ceritinib) treatment resulted in a partial response lasting 8.7 months in a patient with lung adenocarcinoma harboring EML4-ALK, who progressed on prior Alecensa (alectinib) treatment (PMID: 34911818). | 34911818 |
| EML4 - ALK ALK G1202R ALK S1206F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R and ALK S1206F were resistant to Zykadia (ceritinib) in culture (PMID: 35726063). | 35726063 |
| EML4 - ALK | breast cancer | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, breast cancer cells expressing EML4-ALK were sensitive to treatment with Zykadia (ceritinib) in culture, demonstrating inhibition of cell growth (PMID: 32348852). | 32348852 |
| EML4 - ALK ALK L1196M ALK G1269A | lung adenocarcinoma | predicted - sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, fifth-line Zykadia (ceritinib) treatment resulted in a partial response with a progression-free survival of approximately 5 months in a patient with metastatic poorly differentiated lung adenocarcinoma harboring EML4-ALK, ALK G1269A, and ALK L1196M (PMID: 38961982). | 38961982 |
| ALK rearrange ALK L1196M | lung non-small cell carcinoma | predicted - resistant | Ceritinib | Clinical Study - Cohort | Actionable | In a retrospective study, ALK L1196M was identified in 17% (12/70) of plasma samples at disease progression in ALK-positive non-small cell lung cancer patients who received second-generation ALK TKI treatment, including Alecensa (alectinib) (n=46), Zykadia (ceritinib) (n=4), Alunbrig (brigatinib) (n=3), Ensartinib (X-396) (n=1), or more than 2 lines of TKIs (n=16) (PMID: 31358542). | 31358542 |
| EML4 - ALK ALK C1156Y ALK G1202R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK G1202R and C1156Y compound mutation in the context of EML4-ALK were resistant to Zykadia (ceritinib) treatment in culture (PMID: 34158340). | 34158340 |
| EML4 - ALK ALK L1198F ALK G1202R ALK G1269A | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK G1202R, L1198F, and G1269A compound mutation in the context of EML4-ALK were resistant to Zykadia (ceritinib) treatment in culture (PMID: 34158340). | 34158340 |
| ROS1 G2032R | Advanced Solid Tumor | predicted - resistant | Ceritinib | Preclinical - Biochemical | Actionable | In a preclinical study, Zykadia (ceritinib) treatment did not inhibit kinase activity of a transformed cell line expressing ROS1 G2032R in culture (PMID: 32918045). | 32918045 |
| EML4 - ALK ALK D1203N | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells co-expressing EML4-ALK and ALK D1203N demonstrated sensitivity to treatment with Zykadia (ceritinib) in culture (PMID: 27432227). | 27432227 |
| EML4 - ALK ALK D1203N | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK D1203N in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK F1174C | Advanced Solid Tumor | conflicting | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK F1174C were sensitive to treatment with Zykadia (ceritinib) in culture (PMID: 27432227). | 27432227 |
| EML4 - ALK ALK F1174C | Advanced Solid Tumor | conflicting | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK F1174C were resistant to growth inhibition mediated by Zykadia (ceritinib) in culture (PMID: 26698910). | 26698910 |
| EML4 - ALK ALK V1180L | lung adenocarcinoma | predicted - sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a retrospective analysis, Zykadia (ceritinib) treatment resulted in a partial response with a progression-free survival of 7.3 months, overall survival of 26.3 months, and a duration of treatment of 8.2 months in a patient with lung adenocarcinoma harboring EML4-ALK (e6:e20) with ALK V1180L (PMID: 39500140). | 39500140 |
| EML4 - ALK ALK I1171N ALK L1196M | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N and L1196M in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK I1171N | pulmonary neuroendocrine tumor | predicted - sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, Zykadia (ceritinib) treatment resulted in response after 1 month of treatment with tumor shrinkage in a patient with metastatic pulmonary atypical carcinoid tumor harboring EML4-ALK (e6:e20) and ALK I1171N (PMID: 35832448). | 35832448 |
| EML4 - ALK ALK T1151K | lung adenocarcinoma | predicted - resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, ALK T1151K was identified in the post-progression biopsy of a patient with lung adenocarcinoma harboring EML4-ALK after Xalkori (crizotinib) and Zykadia (ceritinib) therapies (PMID: 28676215). | 28676215 |
| ALK rearrange | lung non-small cell carcinoma | sensitive | Ceritinib | Phase II | Actionable | In a Phase II trial (ASCEND-7), Zykadia (ceritinib) demonstrated efficacy in ALK-positive non-small cell lung cancer patients with active brain metastasis, resulting in whole-body overall response rate (ORR) of 35.7% (15/42), 30.0% (12/40), 50.0% (6/12), and 59.1% (26/44) in those who received prior radiation/ALK inhibitor (ALKi), ALKi only, radiation only, no prior radiation/ALKi, respectively, and whole-body ORR of 16.7% (3/18) in patients with leptomeningeal carcinomatosis (PMID: 35091443; NCT02336451). | 35091443 |
| ALK rearrange | lung non-small cell carcinoma | sensitive | Ceritinib | Clinical Study - Cohort | Actionable | In a retrospective analysis, non-small cell lung cancer patients with brain metastases harboring an ALK rearrangement demonstrated a median overall survival of 49.5 months following treatment with the combination of an ALK-targeted tyrosine kinase inhibitor, including Zykadia (ceritinib), and radiotherapy (PMID: 26438117). | 26438117 |
| ALK rearrange | lung non-small cell carcinoma | sensitive | Ceritinib | Guideline | Actionable | Zykadia (ceritinib) is included in guidelines as first-line and as subsequent therapy for patients with advanced or metastatic ALK-rearranged non-small cell lung cancer (NCCN.org). | detail... |
| ALK rearrange | lung non-small cell carcinoma | sensitive | Ceritinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase I trial that supported FDA approval, Zykadia (ceritinib) resulted in a blinded independent review committee (BIRC)-assessed objective response rate of 44% (72/163) and a duration of response of 7.1 months in ALK-rearranged non-small cell lung cancer patients (PMID: 25754348; NCT01283516). | 25754348 detail... detail... |
| ALK rearrange | lung non-small cell carcinoma | sensitive | Ceritinib | Phase II | Actionable | In a Phase II trial (ASCEND-2), non-small cell lung cancer patients with brain metastases harboring an ALK rearrangement and previously treated with Xalkori (crizotinib) and chemotherapy demonstrated an overall response rate of 38.6% (54/140), a disease control rate of 77.1%, a median time to response of 1.8 months, a median duration of response of 9.7 months, and a median progression-free survival of 5.7 months when treated with Zykadia (ceritinib) (PMID: 27432917; NCT01685060). | 27432917 |
| ALK rearrange | lung non-small cell carcinoma | sensitive | Ceritinib | Guideline | Actionable | Zykadia (ceritinib) is included in guidelines for patients with metastatic non-small cell lung cancer harboring an ALK rearrangement (PMID: 30285222; ESMO.org). | detail... 30285222 |
| ALK rearrange | lung non-small cell carcinoma | sensitive | Ceritinib | Guideline | Actionable | Zykadia (ceritinib) is included in the Pan-Asian Guidelines Adaptation (PAGA) as first-line therapy for non-small cell lung cancer patients with ALK rearrangements, including patients with CNS involvement, and as subsequent therapy for patients that progress on Xalkori (crizotinib) (PMID: 30596843; ESMO.org). | detail... 30596843 |
| EML4 - ALK ALK L1196M ALK L1198F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK L1196M and L1198F compound mutation in the context of EML4-ALK were resistant to Zykadia (ceritinib) treatment in culture (PMID: 34158340). | 34158340 |
| EML4 - ALK ALK L1196M ALK L1198F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK L1196M and ALK L1198F displayed enhanced resistance to growth inhibition mediated by Zykadia (ceritinib) in culture (PMID: 26698910). | 26698910 |
| EML4 - ALK ALK I1171T ALK F1174V | lung non-small cell carcinoma | predicted - sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a Phase I trial, Zykadia (ceritinib) treatment resulted in a partial response in a patient with non-small cell lung cancer harboring EML4-ALK (e13:e20), ALK F1174V, and ALK I1171T (PMID: 34890832; NCT01283516). | 34890832 |
| ALK D1091N | neuroblastoma | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) decreased viability of a neuroblastoma cell line harboring ALK D1091N in culture (PMID: 38032104). | 38032104 |
| EML4 - ALK ALK L1196P | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing EML4-ALK and ALK L1196P were resistant to Zykadia (ceritinib) in culture (PMID: 38448512). | 38448512 |
| EML4 - ALK ALK L1152P | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK L1152P in the context of EML4-ALK demonstrated reduced sensitivity to Zykadia (ceritinib) compared to cells expressing EML4-ALK in culture (PMID: 27780853). | 27780853 |
| EML4 - ALK ALK T1151K | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK T1151K in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK L1198R | Advanced Solid Tumor | predicted - resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing EML4-ALK and ALK L1198R were moderately resistant to Zykadia (ceritinib) in culture (PMID: 38448512). | 38448512 |
| EML4 - ALK ALK L1196Q | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK L1196Q in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK C1237Y | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing EML4-ALK and ALK C1237Y were resistant to Zykadia (ceritinib) in culture (PMID: 38448512). | 38448512 |
| ALK rearrange ALK T1151R | lung adenocarcinoma | predicted - resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, ALK T1151R was identified on post-progression biopsy in a patient with lung adenocarcinoma harboring an ALK rearrangement who had been on Zykadia (ceritinib) treatment for 6 months (PMID: 31027750). | 31027750 |
| EML4 - ALK ALK F1174C ALK L1198F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK F1174C and ALK L1198F displayed enhanced resistance to growth inhibition mediated by Zykadia (ceritinib) in culture (PMID: 26698910). | 26698910 |
| EML4 - ALK ALK E1154K ALK G1202R ALK I1268V | lung adenocarcinoma | predicted - resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, Zykadia (ceritinib) treatment resulted rapid disease progression in a patient with lung adenocarcinoma harboring EML4-ALK, with acquired ALK G1202R and ALK E1154K in tumor biopsies, and ALK G1202R and ALK I1268V in ctDNA (PMID: 31585938). | 31585938 |
| ALK I1171T | ganglioneuroblastoma | predicted - sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, Zykadia (ceritinib) treatment resulted in a 43.6% decrease of the primary tumor after 6.5 months of treatment, and complete resolution of metastases at 21 months after initiation of treatment in a pediatric patient with ganglioneuroblastoma harboring ALK I1171T (PMID: 29907598). | 29907598 |
| ALK F1174V ALK amp | neuroblastoma | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited proliferation of neuroblastoma cells harboring ALK amplification and ALK F1174V in culture (PMID: 29907598). | 29907598 |
| ALK L1196M | neuroblastoma | predicted - sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a Phase I trial, Zykadia (ceritinib) treatment resulted in a partial response with a progression-free survival over 544 days in a pediatric patient with neuroblastoma harboring ALK L1196M (PMID: 34780709; NCT01742286). | 34780709 |
| ALK A348D | hematologic cancer | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK A348D were sensitive to treatment with Zykadia (ceritinib) in culture, demonstrating decreased cell viability (PMID: 26032424). | 26032424 |
| EML4 - ALK ALK G1202R ALK S1206F ALK G1269A | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R, S1206F, and G1269A were resistant to Zykadia (ceritinib) in culture (PMID: 35726063). | 35726063 |
| EML4 - ALK ALK F1174C ALK D1203N | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK, ALK D1203N, and ALK F1174C demonstrated resistance to treatment with Zykadia (ceritinib) in culture (PMID: 27432227). | 27432227 |
| ALK rearrange | inflammatory myofibroblastic tumor | sensitive | Ceritinib | Phase I | Actionable | In a Phase I trial, Zykadia (ceritinib) treatment was well tolerated and resulted in an overall response rate of 70% (7/10; 7 partial responses) and a disease control rate of 80% (8/10) in pediatric patients with inflammatory myofibroblastic tumor harboring ALK rearrangement, with median progression-free survival not reached (PMID: 34780709; NCT01742286). | 34780709 |
| ALK rearrange | inflammatory myofibroblastic tumor | sensitive | Ceritinib | Guideline | Actionable | Zykadia (ceritinib) is included in guidelines as first-line therapy for patients with advanced, recurrent, metastatic, or inoperable inflammatory myofibroblastic tumor harboring ALK translocations (NCCN.org). | detail... |
| EML4 - ALK ALK I1171S ALK G1269A | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171S and G1269A in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK I1171S ALK G1269A | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) reduced ALK phosphorylation and inhibited growth of transformed cells expressing EML4-ALK with ALK I1171S and ALK G1269A in culture (PMID: 31943796). | 31943796 |
| EML4 - ALK | lung non-small cell carcinoma | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited phosphorylation of Alk and inhibited growth of human non-small cell lung cancer cell lines harboring EML4-ALK in culture (PMID: 25173427). | 25173427 |
| EML4 - ALK | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited growth of a transformed cell line expressing EML4-ALK in culture (PMID: 25228534). | 25228534 |
| EML4 - ALK ALK F1174I | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK F1174I in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK I1171T | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171T in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK I1171T | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited growth of a transformed cell line expressing EML4-ALK with ALK I1171T in culture (PMID: 25228534). | 25228534 |
| EML4 - ALK ALK F1245V | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK F1245V in culture (PMID: 33627640). | 33627640 |
| ALK fusion | Erdheim-Chester disease | sensitive | Ceritinib | Guideline | Actionable | Zykadia (ceritinib) is included in guidelines as first-line or subsequent-line therapy for patients with Erdheim-Chester disease harboring ALK fusions (NCCN.org). | detail... |
| EML4 - ALK ALK G1269A | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited growth of transformed cells expressing EML4-ALK with ALK G1269A in culture (PMID: 27009859). | 27009859 |
| EML4 - ALK ALK G1269A | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited proliferation of transformed cells expressing EML4-ALK with ALK G1269A in culture (PMID: 25727400). | 25727400 |
| EML4 - ALK ALK G1269A | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK G1269A in culture (PMID: 33627640). | 33627640 |
| ALK positive | Advanced Solid Tumor | predicted - sensitive | Ceritinib | Phase I | Actionable | In a Phase I trial, Zykadia (ceritinib) treatment was well tolerated and resulted in an overall response rate of 14% (1/7), a disease control rate of 43% (3/7), and a progression-free survival of 1.9 months in pediatric patients with ALK-positive advanced solid tumors other than neuroblastoma, anaplastic large cell lymphoma, or inflammatory myofibroblastic tumor (PMID: 34780709; NCT01742286). | 34780709 |
| EML4 - ALK ALK I1171S | lung adenocarcinoma | predicted - sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, Zykadia (ceritinib) treatment resulted in tumor shrinkage with a progression-free survival of at least 8 months in a patient with metastatic lung adenocarcinoma harboring EML4-ALK and ALK I1171S (PMID: 36324562). | 36324562 |
| EML4 - ALK ALK L1198F ALK G1269A | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1269A and ALK L1198F were resistant to growth inhibition mediated by Zykadia (ceritinib) in culture (PMID: 26698910). | 26698910 |
| EML4 - ALK ALK G1202R ALK L1204V ALK G1269A | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK G1202R, L1204V, and G1269A compound mutation in the context of EML4-ALK were resistant to Zykadia (ceritinib) treatment in culture (PMID: 34158340). | 34158340 |
| EML4 - ALK ALK F1174C | lung non-small cell carcinoma | resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, a non-small cell lung carcinoma patient harboring EML4-ALK who developed resistance to Xalkori (crizotinib) treatment was subsequently treated with Zykadia (ceritinib), eventually progressed, and was found to have acquired ALK F1174C (PMID: 24675041). | 24675041 |
| EML4 - ALK ALK G1202R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R were resistant to treatment with Zykadia (ceritinib) in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK G1202R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R demonstrated resistance to Zykadia (ceritinib) in culture (PMID: 25727400). | 25727400 |
| EML4 - ALK ALK G1202R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R were resistant to growth inhibition mediated by Zykadia (ceritinib) in culture (PMID: 26698910). | 26698910 |
| EML4 - ALK ALK G1123S | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, a cell line expressing EML4-ALK with ALK G1123S was resistant to Zykadia (ceritinib) in culture (PMID: 31446141). | 31446141 |
| EML4 - ALK ALK I1171N ALK D1203N | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) did not inhibit viability of cells expressing EML4-ALK, ALK I1171N, and ALK D1203N in culture (PMID: 39269178). | 39269178 |
| EML4 - ALK ALK I1171N ALK G1269A | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N and G1269A in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK F1174V | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK F1174V in culture (PMID: 33627640). | 33627640 |
| ALK F1174L ALK amp | neuroblastoma | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited proliferation of neuroblastoma cells harboring ALK amplification and ALK F1174L in culture (PMID: 29907598). | 29907598 |
| EML4 - ALK ALK I1171N ALK F1174I | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK I1171N and F1174I were resistant to treatment with Zykadia (ceritinib) in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK L1196Q | lung non-small cell carcinoma | predicted - resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, ALK L1196Q was identified in the post-progression biopsy of a patient with non-small cell lung cancer harboring EML4-ALK who was treated with Zykadia (ceritinib) (PMID: 33166721). | 33166721 |
| ALK F856S | hematologic cancer | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK F856S were sensitive to treatment with Zykadia (ceritinib) in culture, demonstrating decreased cell viability (PMID: 26032424). | 26032424 |
| EML4 - ALK ALK T1151M ALK G1202R | lung non-small cell carcinoma | resistant | Ceritinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, a patient-derived non-small cell lung cancer cell line harboring EML4-ALK, ALK G1202R, and ALK T1151M was resistant to Zykadia (ceritinib) treatment in culture (PMID: 39269178). | 39269178 |
| EML4 - ALK ALK R1192P | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK R1192P were resistant to Zykadia (ceritinib) mediated growth inhibition in culture (PMID: 27009859). | 27009859 |
| EML4 - ALK ALK I1171N ALK L1198H | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK I1171N and L1198H were resistant to treatment with Zykadia (ceritinib) in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK F1174L ALK D1203N ALK G1269A | lung adenocarcinoma | predicted - resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, ALK D1203N were identified as a newly acquired mutation in the pleural effusion from a patient with lung adenocarcinoma after his disease progressed on Zykadia (ceritinib) treatment, in addition to the EML4-ALK, ALK F1174L, and ALK G1269A acquired after disease progression on Xalkori (crizotinib) and Belizatinib (TSR-011) sequentially (PMID: 28434515). | 28434515 |
| EML4 - ALK ALK F1174L | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK F1174L were resistant to Zykadia (ceritinib)-mediated growth inhibition in culture (PMID: 27009859). | 27009859 |
| EML4 - ALK ALK G1202R | lung non-small cell carcinoma | resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, a non-small cell lung carcinoma patient harboring EML4-ALK who acquired the secondary drug resistance mutation, ALK S1206Y, when treated with Xalkori (crizotinib) was subsequently treated with Zykadia (ceritinib), developed drug resistance, and was then found to have lost the ALK S1206Y mutation, but gained ALK G1202R (PMID: 24675041). | 24675041 |
| EML4 - ALK ALK G1202R | lung non-small cell carcinoma | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R were insensitive to Zykadia (ceritinib) in culture (PMID: 24675041). | 24675041 |
| EML4 - ALK ALK C1156Y | Advanced Solid Tumor | predicted - sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited proliferation of transformed cells expressing EML4-ALK with ALK C1156Y in culture (PMID: 25727400). | 25727400 |
| EML4 - ALK ALK C1156Y | Advanced Solid Tumor | predicted - sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK C1156Y in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK C1156Y | Advanced Solid Tumor | predicted - sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed human cells expressing ALK C1156Y in the context of EML4-ALK demonstrated minimal sensitivity to Zykadia (ceritinib) in culture (PMID: 24675041). | 24675041 |
| EML4 - ALK ALK C1156Y | Advanced Solid Tumor | predicted - sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited growth of transformed cells expressing EML4-ALK with ALK C1156Y in culture (PMID: 26698910). | 26698910 |
| ALK rearrange ALK L1152R | lung adenocarcinoma | predicted - resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with ALK-rearranged lung adenocarcinoma, which also harbored RB1 deletion and TP53 G154V and R158C mutations, demonstrated a partial response following treatment with Zykadia (ceritinib), however, progressed after 4 months and was found to have an acquired ALK L1152R mutation in a biopsy of a pleural nodule (PMID: 27091190). | 27091190 |
| EML4 - ALK ALK L1152R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK L1152R in the context of EML4-ALK demonstrated reduced sensitivity to Zykadia (ceritinib) compared to cells expressing EML4-ALK in culture (PMID: 27780853). | 27780853 |
| EML4 - ALK ALK L1152R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK L1152R demonstrated resistance to Zykadia (ceritinib) in culture (PMID: 25727400). | 25727400 |
| EML4 - ALK ALK L1122V ALK L1196M ALK D1203N ALK G1269A | lung adenocarcinoma | predicted - resistant | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, ALK D1203N and L1122V were identified in post-progression biopsy in a patient with metastatic lung adenocarcinoma harboring EML4-ALK, ALK G1269A, and ALK L1196M, who previously achieved a partial response on Zykadia (ceritinib) treatment (PMID: 38961982). | 38961982 |
| EML4 - ALK ALK I1171N ALK F1174L | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N and F1174L in culture (PMID: 33627640). | 33627640 |
| ALK rearrange | Cancer of Unknown Primary | sensitive | Ceritinib | Guideline | Actionable | Zykadia (ceritinib) is included in guidelines for patients with cancer of unknown primary harboring ALK rearrangements (PMID: 36563965, PMID: 30285222; ESMO.org). | detail... 30285222 36563965 |
| EML4 - ALK ALK E1129V | lung non-small cell carcinoma | predicted - sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a Phase I trial, Zykadia (ceritinib) treatment resulted in a partial response with a progression-free survival lasting at least 400 days in a patient with non-small cell lung cancer harboring EML4-ALK (e6:e20) and ALK E1129V (PMID: 34890832; NCT01283516). | 34890832 |
| ALK rearrange | anaplastic large cell lymphoma | sensitive | Ceritinib | Guideline | Actionable | Zykadia (ceritinib) is included in guidelines as initial, second-line, and subsequent therapy for patients with anaplastic large cell lymphoma harboring ALK rearrangements (NCCN.org). | detail... |
| ALK rearrange | anaplastic large cell lymphoma | sensitive | Ceritinib | Phase I | Actionable | In a Phase I trial, Zykadia (ceritinib) treatment was well tolerated and resulted in an overall response rate of 75% (6/8; 2 complete responses, 4 partial responses) and a disease control rate of 88% (7/8) in pediatric patients with anaplastic large cell lymphoma harboring ALK rearrangement, with median progression-free survival not reached (PMID: 34780709; NCT01742286). | 34780709 |
| EML4 - ALK ALK I1171N ALK L1256F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK I1171N and L1256F were resistant to treatment with Zykadia (ceritinib) in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK L1196M ALK G1202R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK L1196M and G1202R were resistant to treatment with Zykadia (ceritinib) in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK L1196M ALK G1202R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, cells expressing EML4-ALK, ALK L1196M, and ALK G1202R were resistant to Zykadia (ceritinib) in culture (PMID: 38448512). | 38448512 |
| EML4 - ALK ALK L1196M ALK G1202R | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK G1202R and L1196M compound mutation in the context of EML4-ALK were resistant to Zykadia (ceritinib) treatment in culture (PMID: 34158340). | 34158340 |
| ALK F1174L NRAS Q61K | neuroblastoma | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, expression of NRAS Q61K in a neuroblastoma cell line harboring ALK F1174L conferred resistance to Zykadia (ceritinib) in culture (PMID: 35689207). | 35689207 |
| EML4 - ALK ALK L1196M | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited tumor growth in a cell line xenograft model expressing EML4-ALK with ALK L1196M (PMID: 35820889). | 35820889 |
| EML4 - ALK ALK L1196M | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK L1196M in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK L1196M | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited growth of transformed cells expressing EML4-ALK with ALK L1196M in culture (PMID: 26698910) | 26698910 |
| EML4 - ALK ALK L1196M | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Zykadia (ceritinib) inhibited proliferation of transformed cells expressing EML4-ALK with ALK L1196M in culture (PMID: 25727400). | 25727400 |
| EML4 - ALK ALK L1196M | Advanced Solid Tumor | sensitive | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells co-expressing EML4-ALK and ALK L1196M demonstrated sensitivity to treatment with Zykadia (ceritinib) in culture (PMID: 27432227). | 27432227 |
| EML4 - ALK ALK L1196M ALK G1202R | lung non-small cell carcinoma | resistant | Ceritinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, a patient-derived non-small cell lung cancer cell line harboring EML4-ALK, ALK G1202R, and ALK L1196M was resistant to Zykadia (ceritinib) treatment in culture (PMID: 39269178). | 39269178 |
| EML4 - ALK ALK F1245C | lung non-small cell carcinoma | sensitive | Ceritinib | Case Reports/Case Series | Actionable | In a clinical case study, a non-small cell lung cancer patient harboring EML4-ALK variant 3 that demonstrated resistance to treatment with Xalkori (crizotinib) after acquisition of ALK F1245C, achieved a complete radiographic response with no evidence of progression at 6 months following treatment with Zykadia (ceritinib) (PMID: 26775591). | 26775591 |
| EML4 - ALK ALK I1171N ALK L1198F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK I1171N and ALK L1198F were resistant to Zykadia (ceritinib) in culture (PMID: 35726063). | 35726063 |
| EML4 - ALK ALK I1171N ALK L1198F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK I1171N and L1198F were resistant to treatment with Zykadia (ceritinib) in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK I1171N ALK L1198F | Advanced Solid Tumor | resistant | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing ALK I1171N and L1198F compound mutation in the context of EML4-ALK were resistant to Zykadia (ceritinib) treatment in culture (PMID: 34158340). | 34158340 |
| EML4 - ALK ALK D1203N ALK E1210K | Advanced Solid Tumor | decreased response | Ceritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK, ALK D1203N, and ALK E1210K demonstrated a decreased response to treatment with Zykadia (ceritinib) compared to cells expressing EML4-ALK in culture (PMID: 27432227). | 27432227 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02513667 | Phase II | Ceritinib | Ceritinib in Combination With Stereotactic Ablative Radiation Metastatic Lung Adenocarcinoma | Terminated | USA | 0 |
| NCT02645149 | Phase II | Trametinib Pazopanib Ceritinib Ribociclib + Trametinib | Molecular Profiling and Matched Targeted Therapy for Patients With Metastatic Melanoma (MatchMel) | Recruiting | AUS | 0 |
| NCT01947608 | Phase I | Ceritinib | Expanded Treatment Protocol With LDK378 in ALK(+) NSCLC | No longer available | USA | ARG | 8 |
| NCT01828112 | Phase III | Docetaxel Pemetrexed Disodium Ceritinib | LDK378 Versus Chemotherapy in ALK Rearranged (ALK Positive) Patients Previously Treated With Chemotherapy (Platinum Doublet) and Crizotinib | Completed | USA | TUR | NLD | LBN | ITA | ISR | IRL | GBR | FRA | ESP | DEU | CHE | CAN | BEL | 6 |
| NCT02343679 | Phase II | Ceritinib | Novartis PhII Ceritinib (LDK378) in R/R ALK+ Hem Malignancies | Withdrawn | USA | 0 |
| NCT02299505 | Phase I | Ceritinib | Pharmacokinetic and Safety Study of Lower Doses of Ceritinib Taken With a Low-fat Meal Versus 750 mg of Ceritinib in the Fasted State in Adult Patients With (ALK-positive) Metastatic Non-small Cell Lung Cancer (NSCLC) | Completed | USA | TUR | POL | NLD | LBN | ITA | GRC | GBR | ESP | DEU | CZE | CAN | BRA | BGR | BEL | AUT | AUS | 7 |
| NCT03737994 | Phase II | Cisplatin + Lorlatinib Carboplatin + Lorlatinib Ceritinib Alectinib + Cisplatin Alectinib + Carboplatin Ceritinib + Cisplatin Pemetrexed Disodium Carboplatin + Ceritinib Cisplatin + Ensartinib Carboplatin + Ensartinib Brigatinib + Cisplatin Brigatinib Alectinib Brigatinib + Carboplatin Ensartinib Cisplatin + Pemetrexed Disodium Crizotinib Carboplatin + Pemetrexed Disodium Lorlatinib | Targeted Treatment for ALK Positive Patients Who Have Previously Been Treated for Non-squamous Non-small Cell Lung Cancer | Active, not recruiting | USA | 0 |
| NCT02584933 | FDA approved | Ceritinib | Roll-over Study to Allow Access to Certinib (LDK378) for Patients Who Are on Ceritinib Treatment in a Novartis-sponsored Study | Active, not recruiting | USA | POL | LBN | ITA | FRA | ESP | DEU | CZE | BRA | BGR | BEL | AUS | 9 |
| NCT02587650 | Phase II | Ceritinib Capmatinib Regorafenib Entrectinib | Capmatinib, Ceritinib, Regorafenib, or Entrectinib in Treating Patients With BRAF/NRAS Wild-Type Stage III-IV Melanoma | Terminated | USA | 0 |
| NCT02605746 | Phase I | Ceritinib | Preoperative Ceritinib (LDK378) in Glioblastoma Multiforme and CNS Metastasis | Completed | USA | 0 |
| NCT02551718 | Phase I | Bosutinib Irinotecan Romidepsin Busulfan Melphalan Nilotinib Crizotinib Cytarabine Mitoxantrone Dasatinib Pazopanib Paclitaxel Clofarabine Hydroxyurea Tretinoin Carfilzomib Nelarabine Bexarotene Pentostatin Everolimus Cabozantinib Mercaptopurine Methotrexate Cladribine Thioguanine Daunorubicin Ponatinib Etoposide Afatinib Gefitinib Gemcitabine Regorafenib Arsenic trioxide Trametinib Imatinib Erlotinib Dabrafenib Decitabine Axitinib Azacitidine Ruxolitinib Fludarabine Lapatinib Ceritinib Sirolimus Sorafenib Lomustine Sunitinib Cabazitaxel Temsirolimus Topotecan Bortezomib Pralatrexate | High Throughput Drug Sensitivity Assay and Genomics- Guided Treatment of Patients With Relapsed or Refractory Acute Leukemia | Completed | USA | 0 |
| NCT02289144 | Phase II | Ceritinib | Ceritinib in Mutation and Oncogene Directed Therapy in Thyroid Cancer | Withdrawn | USA | 0 |
| NCT01772797 | Phase I | Ceritinib Luminespib | Phase Ib Study of LDK378 and AUY922 in ALK-rearranged Non-small Cell Lung Cancer | Completed | USA | ITA | ESP | AUS | 1 |
| NCT04817956 | Phase II | Ceritinib Melphalan Cobimetinib + Vemurafenib Alectinib Pemigatinib Entrectinib Bortezomib Dostarlimab-gxly Atezolizumab Alpelisib Atezolizumab + Bevacizumab Olaparib Selpercatinib Capmatinib Dactinomycin Dabrafenib + Trametinib Vismodegib Niraparib Imatinib Pertuzumab/trastuzumab/hyaluronidase-zzxf | Improving Public Cancer Care by Implementing Precision Medicine in Norway (IMPRESS-N) | Recruiting | NOR | 0 |
| NCT02186821 | Phase II | Ceritinib | Ceritinib (LDK378) for Patients Whose Tumors Have Aberrations in ALK or ROS1 (SIGNATURE) | Terminated | USA | 0 |
| NCT02638909 | Phase II | Ceritinib | Study of Oral Ceritinib in Patients With ALK-Activated Gastrointestinal Malignancies | Terminated | USA | 0 |
| NCT03501368 | Phase II | Ceritinib | Study of Ceritinib in Patients With Unresectable Melanoma | Active, not recruiting | USA | 0 |
| NCT03784014 | Phase III | Ceritinib Dabrafenib + Trametinib Capmatinib Durvalumab + Olaparib Nilotinib Futibatinib Trametinib Palbociclib Glasdegib Lapatinib | Molecular Profiling of Advanced Soft-tissue Sarcomas (MULTISARC) | Active, not recruiting | FRA | 0 |
| NCT01742286 | Phase I | Ceritinib | Phase I Study of LDK378 in Pediatric, Malignancies With a Genetic Alteration in Anaplastic Lymphoma Kinase (ALK) | Completed | USA | NLD | ITA | GBR | FRA | ESP | DEU | CAN | AUS | 1 |
| NCT02336451 | Phase II | Ceritinib | A Phase II Study to Evaluate the Efficacy and Safety of Oral Ceritinib in Patients With ALK-positive NSCLC Metastatic to the Brain and/or to Leptomeninges | Completed | USA | TUR | NLD | ITA | GBR | FRA | ESP | DEU | CAN | BRA | BEL | AUS | 5 |
| NCT02422589 | Phase I | Warfarin Midazolam Ceritinib | A Phase I, Multi-center, Open Label, Drug-drug Interaction Study to Assess the Effect of Ceritinib on the Pharmacokinetics of Warfarin and Midazolam in Patients With ALK-positive Advanced Tumors | Completed | USA | ITA | ESP | DNK | 0 |
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