Therapy Detail
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| Therapy Name | Gilteritinib |
| Synonyms | |
| Therapy Description |
Xospata (gilteritinib) is a small molecule inhibitor of FLT3 and AXL that has activity against FLT3-ITD, FLT3 F691L, and FLT3 D835 mutations, potentially resulting in decreased tumor growth (J Clin Oncol 32:5s, 2014 (suppl; abstr 7070), PMID: 25891481). Xospata (gilteritinib) is FDA approved for use in patients with relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation (ITD, D835X, and I836X) (FDA.gov). |
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| Drug Name | Trade Name | Synonyms | Drug Classes | Drug Description |
|---|---|---|---|---|
| Gilteritinib | Xospata | ASP2215 | AXL Inhibitor 30 FLT3 Inhibitor 69 | Xospata (gilteritinib) is a small molecule inhibitor of FLT3 and AXL that has activity against FLT3-ITD, FLT3 F691L, and FLT3 D835 mutations, potentially resulting in decreased tumor growth (J Clin Oncol 32:5s, 2014 (suppl; abstr 7070), PMID: 25891481). Xospata (gilteritinib) is FDA approved for use in patients with relapsed or refractory acute myeloid leukemia (AML) with a FLT3 mutation (ITD, D835X, and I836X) (FDA.gov). |
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| Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
|---|---|---|---|---|---|---|---|
| EML4 - ALK ALK I1171N ALK F1174I | lung non-small cell carcinoma | sensitive | Gilteritinib | Preclinical - Pdx | Actionable | In a preclinical study, Xospata (gilteritinib) induced complete tumor regression in a patient-derived xenograft (PDX) model of non-small cell lung cancer harboring EML4-ALK and expressing ALK I1171N and F1174I, and also induced tumor regression when administered to separate PDX tumors which had demonstrated resistance to Alecensa (alectinib) or Lorbrena (lorlatinib) treatment (PMID: 33627640). | 33627640 |
| FLT3 exon21 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (PMID: 32171751; ESMO.org). | 32171751 detail... |
| FLT3 exon21 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (NCCN.org). | detail... |
| FLT3 exon 14 ins FLT3 D835X NRAS Q61K | acute myeloid leukemia | predicted - resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a clinical study, two patients with acute myeloid leukemia harboring FLT3-ITD and a D835 mutation progressed on Xospata (gilteritinib) treatment and were found to have acquired NRAS Q61K (PMID: 31088841). | 31088841 |
| FLT3 exon 14 ins FLT3 Y693N FLT3 D835V | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D835V and FLT3 Y693N were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835A | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835A in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835A | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835A in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 D835H | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835H in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835H | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835H in culture (PMID: 35395091). | 35395091 |
| CBL Y371H FLT3 pos | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited proliferation of cells expressing wild-type FLT3 and CBL Y371H in culture (PMID: 31943762). | 31943762 |
| FLT3 D835X | acute myeloid leukemia | sensitive | Gilteritinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III trial (ADMIRAL) that supported FDA approval, Xospata (gilteritinib) improved median overall survival (9.3 vs 5.6 mo, HR. 0.64, p<0.001) compared to chemotherapy, resulted in superior median event-free survival (2.8 vs 0.7 mo, HR 0.79) and rate of complete remission with full or partial hematologic recovery (34.0% vs 15.3%) in patients with relapsed or refractory acute myeloid leukemia harboring a FLT3 internal tandem duplication (ITD), D835, or I836 mutation (PMID: 31665578; NCT02421939). | detail... 31665578 detail... |
| EML4 - ALK ALK I1171N | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK D1203N ALK F1245V | Advanced Solid Tumor | predicted - resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK D1203N and F1245V demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK G1269A | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK G1269A in culture (PMID: 33627640). | 33627640 |
| FLT3 exon14 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (NCCN.org). | detail... |
| FLT3 exon14 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (PMID: 32171751; ESMO.org). | detail... 32171751 |
| EML4 - ALK ALK F1245V | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK F1245V in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 I836del | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 I836del in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK I1171N ALK L1256F | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited Alk phosphorylation and viability of transformed cells expressing EML4-ALK with ALK I1171N and L1256F in culture (PMID: 36201110). | 36201110 |
| EML4 - ALK ALK I1171N ALK L1256F | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N and L1256F in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 G822E | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G822E in culture (PMID: 32040554). | 32040554 |
| FLT3 A680V | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3 A680V were sensitive to treatment with Xospata (gilteritinib) in culture, demonstrating decreased cell viability and decreased Flt3 phosphorylation (PMID: 33563661). | 33563661 |
| FLT3 exon 14 ins FLT3 N841H | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N841H in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK I1171S | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171S in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 D835E | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835E in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 D835E | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835E in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 G697S | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 G697S demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 G697S | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD and FLT3 G697S were resistant to Xospata (gilteritinib) treatment in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 G631R | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G631R in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK F1174I ALK G1202R | Advanced Solid Tumor | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R and F1174I were resistant to Xospata (gilteritinib) in culture (PMID: 36201110). | 36201110 |
| EML4 - ALK ALK L1196M ALK D1203N | Advanced Solid Tumor | predicted - resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK L1196M and D1203N demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 33627640). | 33627640 |
| FLT3 D839G | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 D839G in culture (PMID: 32040554). | 32040554 |
| CBL Q365_E366insSK FLT3 wild-type | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited growth of transformed hematologic cells expressing CBL Q365_E366insSK and wild-type FLT3 in culture (PMID: 31309543). | 31309543 |
| EML4 - ALK ALK G1202R | Advanced Solid Tumor | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R were resistant to treatment with Xospata (gilteritinib) in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK G1202R | Advanced Solid Tumor | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R were resistant to Xospata (gilteritinib) in culture (PMID: 36201110). | 36201110 |
| FLT3 D835Y | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited growth of transformed hematologic cells expressing FLT3 D835Y in culture (PMID: 31309543). | 31309543 |
| FLT3 D835Y | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 D835Y in culture (PMID: 32040554). | 32040554 |
| FLT3 D835Y | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of cultured cells expressing FLT3 D835Y (PMID: 38231480). | 38231480 |
| FLT3 exon 14 ins FLT3 D835X NRAS G12D NRAS G12S | acute myeloid leukemia | predicted - resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a clinical study, a patient with acute myeloid leukemia harboring FLT3-ITD and a D835 mutation progressed on Xospata (gilteritinib) treatment and was found to have acquired NRAS G12S and G12D (PMID: 31088841). | 31088841 |
| FLT3 exon 14 ins FLT3 Y842C | acute myeloid leukemia | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in acute myeloid leukemia cells harboring FLT3 ITD with FLT3 Y842C in culture (PMID: 32040554). | 32040554 |
| FLT3 N676K | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of cultured cells expressing FLT3 N676K (PMID: 38231480). | 38231480 |
| FLT3 N676K | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 N676K in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK I1171T | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171T in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 F691L | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Xospata (gilteritinib) was not active against cells expressing FLT3-ITD with FLT3 F691L in culture and resulted in minimal survival benefit in a cell line xenograft model (PMID: 38231480). | 38231480 |
| FLT3 exon 14 ins FLT3 F691L | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD and FLT3 F691L were moderately resistant to Xospata (gilteritinib) treatment in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 F691L | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD and FLT3 F691L demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 33780043). | 33780043 |
| FLT3 exon 14 ins FLT3 F691L | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 F691L demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 F691L | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing both FLT3 exon 14 insertions (ITD) and FLT3 F691L were less sensitive to Xospata (gilteritinib)-induced growth inhibition compared to cells expressing FLT3 ITD in culture (PMID: 31309543). | 31309543 |
| CBL Q365_E366insSK FLT3 pos | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited proliferation of cells expressing wild-type FLT3 and CBL Q365_E366insSK in culture (PMID: 31943762). | 31943762 |
| FLT3 exon 14 ins FLT3 G669R | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G669R in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 N676K | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 N676K in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 N676K | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N676K in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins JAK3 V722I | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing a FLT3-ITD mutation and JAK3 V722I were resistant to treatment with Xospata (gilteritinib) in culture (PMID: 33149267). | 33149267 |
| FLT3 exon 14 ins FLT3 F691L FLT3 D835Y | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3-ITD, FLT3 F691L, and FLT3 D835Y demonstrated resistance to Xospata (gilteritinib) in culture (PMID: 34768286). | 34768286 |
| FLT3 exon20 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (NCCN.org). | detail... |
| FLT3 exon20 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (PMID: 32171751; ESMO.org). | 32171751 detail... |
| FLT3 exon 14 ins FLT3 N841Y | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N841Y in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK I1171N ALK G1269A | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N and G1269A in culture (PMID: 33627640). | 33627640 |
| FLT3 N841Y | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 N841Y in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 N841I | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N841I in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 F691L FLT3 D835Y | acute myeloid leukemia | predicted - resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a Phase I trial, a patient with acute myeloid leukemia harboring FLT3 ITD with FLT3 D835Y and F691L was resistant to Xospata (gilteritinib) (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins NRAS G12C | acute myeloid leukemia | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring FLT3-ITD and NRAS G12C were resistant to Xospata (gilteritinib) as demonstrated by increased cell growth and RAS/MAPK pathway activation in culture (PMID: 31088841). | 31088841 |
| FLT3 exon 14 ins NRAS G12C | acute myeloid leukemia | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring FLT3-ITD and expressing NRAS G12C were resistant to Xospata (gilteritinib) in culture (PMID: 38231480). | 38231480 |
| FLT3 exon 14 ins NRAS G12C | acute myeloid leukemia | resistant | Gilteritinib | Preclinical - Biochemical | Actionable | In a preclinical study, acute myeloid leukemia cells harboring a FLT3-ITD mutation and expressing NRAS G12C demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 35395091). | 35395091 |
| FLT3 D835V | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 D835V in culture (PMID: 32040554). | 32040554 |
| FLT3 D835V | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of cultured cells expressing FLT3 D835V (PMID: 38231480). | 38231480 |
| FLT3 exon 14 ins FLT3 D835Y | acute myeloid leukemia | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of primary patient-derived acute myeloid leukemia blasts harboring FLT3-ITD with FLT3 D835Y in culture (PMID: 38231480). | 38231480 |
| FLT3 exon 14 ins FLT3 D835Y | acute myeloid leukemia | sensitive | Gilteritinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, a patient-derived acute myeloid leukemia cell line harboring a FLT3 internal tandem duplication (ITD) and FLT3 D835Y demonstrated sensitivity to Xospata (gilteritinib) treatment in culture, resulting in reduced cell viability (PMID: 27908881). | 27908881 |
| FLT3 exon 14 ins FLT3 D835Y | acute myeloid leukemia | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in acute myeloid leukemia cells harboring FLT3 ITD with FLT3 D835Y in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835Y | acute myeloid leukemia | sensitive | Gilteritinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of acute myeloid leukemia cells harboring a FLT3-ITD mutation and FLT3 D835Y in culture, and reduced tumor growth and increased survival in cell line xenograft models (PMID: 33268594). | 33268594 |
| FLT3 exon 14 ins FLT3 D835Y | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835Y in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 D835Y | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of cultured cells expressing FLT3-ITD with FLT3 D835Y and improved survival in a cell line xenograft model (PMID: 38231480). | 38231480 |
| FLT3 exon 14 ins FLT3 D835Y | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835Y in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835Y | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 D835Y in culture (PMID: 34768286). | 34768286 |
| FLT3 exon 14 ins FLT3 D839A | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D839A in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D839N | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D839N in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835I | acute myeloid leukemia | predicted - sensitive | Gilteritinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, a patient-derived acute myeloid leukemia cell line harboring a FLT3 internal tandem duplication (ITD) and FLT3 D835I demonstrated sensitivity to Xospata (gilteritinib) treatment in culture, resulting in reduced cell viability and inhibition of Flt3 phosphorylation (PMID: 27908881). | 27908881 |
| FLT3 exon 14 ins FLT3 M837K | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 M837K in culture (PMID: 31088841). | 31088841 |
| FLT3 exon 14 ins FLT3 M837K | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 M837K in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 N841K | acute myeloid leukemia | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in acute myeloid leukemia cells harboring FLT3 ITD with FLT3 N841K in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK F1174C ALK G1202R | Advanced Solid Tumor | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R and F1174C were resistant to Xospata (gilteritinib) in culture (PMID: 36201110). | 36201110 |
| FLT3 exon 14 ins FLT3 R834Q | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 R834Q in culture (PMID: 32040554). | 32040554 |
| FLT3 N841Y | acute myeloid leukemia | predicted - sensitive | Gilteritinib | Case Reports/Case Series | Actionable | In a Phase I trial, Xospata (gilteritinib) resulted in a partial response in an acute myeloid leukemia patient harboring FLT3 N841Y (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D839G | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D839G in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D839G | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 D839G in culture (PMID: 34768286). | 34768286 |
| FLT3 I836del | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 I836del in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835H | acute myeloid leukemia | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in acute myeloid leukemia cells harboring FLT3 ITD with FLT3 D835H in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins | acute myeloid leukemia | sensitive | Gilteritinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III trial (ADMIRAL) that supported FDA approval, Xospata (gilteritinib) improved median overall survival (9.3 vs 5.6 mo, HR. 0.64, p<0.001), median event-free survival (2.8 vs 0.7 mo, HR 0.79), and rate of complete remission with full or partial hematologic recovery (34.0% vs 15.3%) compared to chemotherapy in patients with relapsed or refractory acute myeloid leukemia harboring a FLT3 internal tandem duplication (ITD; exon 14 insertion), D835, or I836 mutation (PMID: 31665578; NCT02421939). | detail... 31665578 detail... |
| FLT3 exon 14 ins | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in the guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a FLT3 internal tandem duplication (FLT3-ITD) mutation (PMID: 32171751; ESMO.org). | detail... 32171751 |
| FLT3 exon 14 ins | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in the guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a FLT3 internal tandem duplication (FLT3-ITD) mutation (NCCN.org). | detail... |
| FLT3 exon 14 ins | acute myeloid leukemia | sensitive | Gilteritinib | Phase Ib/II | Actionable | In a Phase I/II trial, treatment with Gilteritinib (ASP2215) at a dose of 80mg/day or higher resulted in an overall response rate of 55% (77/141) in patients with relapsed or refractory acute myeloid leukemia harboring FLT3 internal tandem duplication mutations (PMID: 28645776; NCT02014558). | 28645776 |
| FLT3 exon 14 ins | acute myeloid leukemia | sensitive | Gilteritinib | Phase III | Actionable | In a Phase III trial, post-hematopoietic cell transplantation maintenance Xospata (gilteritinib) treatment improved relapse-free survival in patients with acute myeloid leukemia harboring a FLT3 internal tandem duplication (FLT3-ITD) mutation who had detectable minimal residual disease pre- or post-hematopoietic cell transplantation compared to placebo, but was not beneficial in patients without minimal residual disease (PMID: 38471061; NCT02997202). | 38471061 |
| FLT3 D835F | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 D835F in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 C35S | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 C35S in culture (PMID: 31088841). | 31088841 |
| FLT3 exon 14 ins FLT3 D698N FLT3 D835V | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D835V and FLT3 D698N were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 F691L FLT3 Y842H | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3-ITD, FLT3 F691L, and FLT3 Y842H demonstrated resistance to Xospata (gilteritinib) in culture (PMID: 34768286). | 34768286 |
| EML4 - ALK ALK I1171N ALK F1174L | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N and F1174L in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 D698N | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD and FLT3 D698N were moderately resistant to Xospata (gilteritinib) treatment in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 D698N | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D698N demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK L1198F ALK G1202R | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK L1198F and G1202R in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 D835I | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835I in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835I | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835I in culture (PMID: 35395091). | 35395091 |
| EML4 - ALK ALK D1203N | Advanced Solid Tumor | predicted - resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK D1203N demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 D835del | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835del in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 D835del | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835del in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 F691L FLT3 D835V | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D835V and FLT3 F691L were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 G846R | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G846R in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 E786K | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 E786K in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 S705N | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 S705N in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK I1171N ALK L1196M | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N and L1196M in culture (PMID: 33627640). | 33627640 |
| CBL Y371del FLT3 pos | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited proliferation of cells expressing wild-type FLT3 and CBL Y371del in culture (PMID: 31943762). | 31943762 |
| FLT3 exon 14 ins FLT3 D835V | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of cultured cells expressing FLT3-ITD with FLT3 D835V (PMID: 38231480). | 38231480 |
| FLT3 exon 14 ins FLT3 D835V | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835V in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 D835V | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835V in culture (PMID: 32040554). | 32040554 |
| FLT3 N841T | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 N841T in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835V | acute myeloid leukemia | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of primary patient-derived acute myeloid leukemia blasts harboring FLT3-ITD with FLT3 D835V in culture (PMID: 38231480). | 38231480 |
| FLT3 exon 14 ins FLT3 D835V | acute myeloid leukemia | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in acute myeloid leukemia cells harboring FLT3 ITD with FLT3 D835V in culture (PMID: 32040554). | 32040554 |
| FLT3 F594_W603dup | acute myeloid leukemia | predicted - sensitive | Gilteritinib | Case Reports/Case Series | Actionable | In a clinical study, Xospata (gilteritinib) treatment led to decreased disease burden (<10%) in an acute myeloid leukemia patient harboring FLT3 F594_W603dup (PMID: 33563661; NCT02670525). | 33563661 |
| FLT3 exon 14 ins FLT3 Y842C | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell line xenograft | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of cultured cells expressing FLT3-ITD with FLT3 Y842C and improved survival in a cell line xenograft model (PMID: 38231480). | 38231480 |
| FLT3 exon 14 ins FLT3 Y842C | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 Y842C in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins JAK2 V617F | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing a FLT3-ITD mutation and JAK2 V617F were resistant to treatment with Xospata (gilteritinib) in culture (PMID: 33149267). | 33149267 |
| FLT3 exon 14 ins FLT3 A848P | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 A848P in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited growth of transformed hematologic cells expressing FLT3 exon 14 insertions (ITD) in culture (PMID: 31309543). | 31309543 |
| FLT3 exon 14 ins | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD in culture (PMID: 35395091). | 35395091 |
| KIT D816V | hematologic cancer | predicted - sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) demonstrated moderate inhibition of Kit phosphorylation and growth of transformed hematologic cells expressing KIT D816V in culture (PMID: 31309543). | 31309543 |
| FLT3 exon 14 ins IDH2 R140Q | acute myeloid leukemia | predicted - sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, high dosage Xospata (gilteritinib) treatment resulted in reduced viability and colony formation of cells isolated from a transgenic mouse model of acute myeloid leukemia harboring a FLT3-ITD mutation and IDH2 R140Q in culture (PMID: 33268594). | 33268594 |
| FLT3 D835V | acute myeloid leukemia | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of primary patient-derived acute myeloid leukemia blasts harboring FLT3 D835V in culture (PMID: 38231480). | 38231480 |
| FLT3 exon 14 ins FLT3 D835N | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835N in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 D835N | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835N in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 F691L | acute myeloid leukemia | resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a Phase I trial, three patients with acute myeloid leukemia harboring FLT3 ITD with FLT3 F691L were resistant to Xospata (gilteritinib) (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 F691L | acute myeloid leukemia | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring FLT3 ITD with FLT3 F691L were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK C1156Y ALK G1202R | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R and C1156Y were resistant to Xospata (gilteritinib) in culture (PMID: 36201110). | 36201110 |
| EML4 - ALK ALK E1129V ALK G1202R | Advanced Solid Tumor | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R and E1129V were resistant to Xospata (gilteritinib) in culture (PMID: 36201110). | 36201110 |
| FLT3 exon16 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (NCCN.org). | detail... |
| FLT3 exon16 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (PMID: 32171751; ESMO.org). | 32171751 detail... |
| EML4 - ALK ALK I1171N ALK F1174I | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N and F1174I in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 M855T | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 M855T in culture (PMID: 32040554). | 32040554 |
| FLT3 exon19 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (NCCN.org). | detail... |
| FLT3 exon19 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (PMID: 32171751; ESMO.org). | 32171751 detail... |
| EML4 - ALK | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 Y693C FLT3 D835V | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D835V and FLT3 Y693C were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). | 32040554 |
| FLT3 I836X | acute myeloid leukemia | sensitive | Gilteritinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III trial (ADMIRAL) that supported FDA approval, Xospata (gilteritinib) improved median overall survival (9.3 vs 5.6 mo, HR. 0.64, p<0.001) compared to chemotherapy, resulted in superior median event-free survival (2.8 vs 0.7 mo, HR 0.79) and rate of complete remission with full or partial hematologic recovery (34.0% vs 15.3%) in patients with relapsed or refractory acute myeloid leukemia harboring a FLT3 internal tandem duplication (ITD), D835, or I836 mutation (PMID: 31665578; NCT02421939). | detail... 31665578 detail... |
| FLT3 exon15 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (NCCN.org). | detail... |
| FLT3 exon15 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (PMID: 32171751; ESMO.org). | detail... 32171751 |
| EML4 - ALK ALK V1180L | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK V1180L in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK L1198F | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK L1198F in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 K429E | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 K429E in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 K429E | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 K429E in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 N609T | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N609T in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK I1171N ALK L1198F | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N and ALK L1198F in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 N701K | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD and FLT3 N701K demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 33780043). | 33780043 |
| FLT3 exon 14 ins FLT3 D835X NRAS G13D | acute myeloid leukemia | predicted - resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a clinical study, a patient with acute myeloid leukemia harboring FLT3-ITD and a D835 mutation progressed on Xospata (gilteritinib) treatment and was found to have acquired NRAS G13D (PMID: 31088841). | 31088841 |
| EML4 - ALK ALK L1196Q | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK L1196Q in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 G846S | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G846S in culture (PMID: 32040554). | 32040554 |
| BRAF G469A CBL C404Y FLT3 exon 14 ins FLT3 D835X | acute myeloid leukemia | predicted - resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a clinical study, a patient with acute myeloid leukemia harboring FLT3-ITD and a D835 mutation progressed on Xospata (gilteritinib) treatment and was found to have acquired CBL C404Y and BRAF G469A (PMID: 31088841). | 31088841 |
| FLT3 D835E | acute myeloid leukemia | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of primary patient-derived acute myeloid leukemia blasts harboring FLT3 D835E in culture (PMID: 38231480). | 38231480 |
| FLT3 exon17 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (NCCN.org). | detail... |
| FLT3 exon17 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (PMID: 32171751; ESMO.org). | 32171751 detail... |
| FLT3 exon 14 ins FLT3 Y842H | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited proliferation of transformed cells expressing FLT3-ITD and FLT3 Y842H in culture (PMID: 34768286). | 34768286 |
| FLT3 exon 14 ins FLT3 Y842H | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 Y842H in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 E778K | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 E778K in culture (PMID: 32040554). | 32040554 |
| KIT D816V | acute myeloid leukemia | predicted - sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) demonstrated moderate inhibition of Kit phosphorylation and growth of erythroleukemia cells expressing KIT D816V in culture (PMID: 31309543). | 31309543 |
| FLT3 exon22 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (NCCN.org). | detail... |
| FLT3 exon22 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (PMID: 32171751; ESMO.org). | 32171751 detail... |
| EML4 - ALK ALK L1196M ALK G1202R | Advanced Solid Tumor | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK G1202R and L1196M were resistant to Xospata (gilteritinib) in culture (PMID: 36201110). | 36201110 |
| EML4 - ALK ALK L1196M ALK G1202R | Advanced Solid Tumor | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing EML4-ALK with ALK L1196M and G1202R demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 33627640). | 33627640 |
| FLT3 Y842C | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 Y842C in culture (PMID: 32040554). | 32040554 |
| FLT3 Y842C | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of cultured cells expressing FLT3 Y842C (PMID: 38231480). | 38231480 |
| EML4 - ALK ALK L1256F | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK L1256F in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK T1151K | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK T1151K in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK I1171N ALK L1198H | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171N and ALK L1198H in culture (PMID: 33627640). | 33627640 |
| FLT3 rearrange | myeloid neoplasm | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with a myeloid/lymphoid neoplasm with eosinophilia harboring a FLT3 rearrangement (NCCN.org). | detail... |
| FLT3 exon 14 ins FLT3 D835X NRAS G13R | acute myeloid leukemia | predicted - resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a clinical study, two patients with acute myeloid leukemia harboring FLT3-ITD and a D835 mutation progressed on Xospata (gilteritinib) treatment and were found to have acquired NRAS G13R (PMID: 31088841). | 31088841 |
| EML4 - ALK ALK C1156Y | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK C1156Y in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 D835G | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835G in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 D835G | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835G in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D698N | Advanced Solid Tumor | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells co-expressing FLT3 ITD and FLT3 D698N were resistant to treatment with Xospata (gilteritinib) in culture (Blood (2019) 134 (Supplement_1): 2672). | detail... |
| FLT3 exon 14 ins FLT3 F691L FLT3 D835I | acute myeloid leukemia | predicted - resistant | Gilteritinib | Preclinical - Patient cell culture | Actionable | In a preclinical study, a patient-derived acute myeloid leukemia cell line harboring a FLT3 internal tandem duplication (ITD) with FLT3 F691L and FLT3 D835I demonstrated resistance to Xospata (gilteritinib) treatment in culture (PMID: 27908881). | 27908881 |
| FLT3 exon 14 ins NRAS G12D | acute myeloid leukemia | predicted - resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) failed to inhibit growth of acute myeloid leukemia cells harboring a FLT3-ITD mutation and NRAS G12D in culture (PMID: 33268594). | 33268594 |
| FLT3 exon 14 ins FLT3 F691L FLT3 D835X | acute myeloid leukemia | predicted - resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a clinical study, four patients with acute myeloid leukemia harboring FLT3-ITD and a D835 mutation progressed on Xospata (gilteritinib) treatment and were found to have acquired FLT3 F691L (PMID: 31088841). | 31088841 |
| FLT3 exon 14 ins FLT3 N841T | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N841T in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 Y693C | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD and FLT3 Y693C were moderately resistant to Xospata (gilteritinib) treatment in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 Y693C | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 Y693C demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 N841K | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 N841K in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835F | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D835F in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835F | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited growth of transformed hematologic cells expressing FLT3-ITD and FLT3 D835F in culture (PMID: 35395091). | 35395091 |
| EML4 - ALK ALK I1171S ALK G1269A | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK I1171S and G1269A in culture (PMID: 33627640). | 33627640 |
| FLT3 R845S | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 R845S in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D839H | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 D839H in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK I1171N | lung non-small cell carcinoma | sensitive | Gilteritinib | Preclinical - Pdx & cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited growth of patient-derived non-small cell lung cancer cells harboring EML4-ALK with ALK I1171N in culture, and induced tumor regression and suppressed Alk phosphorylation and downstream signaling in xenograft models (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 Y693N | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 Y693N demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 Y693N | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3-ITD and FLT3 Y693N were moderately resistant to Xospata (gilteritinib) treatment in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins FLT3 G757E | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G757E in culture (PMID: 32040554). | 32040554 |
| FLT3 mutant | acute myeloid leukemia | sensitive | Gilteritinib | Phase Ib/II | Actionable | In a Phase I/II trial, treatment with Gilteritinib (ASP2215) resulted in an overall response rate of 49% (93/191) in patients with relapsed or refractory acute myeloid leukemia harboring FLT3 mutations, compared to 12% (7/58) in patients with wild-type FLT3 (PMID: 28645776; NCT02014558). | detail... 28645776 |
| FLT3 mutant | acute myeloid leukemia | sensitive | Gilteritinib | FDA approved - Has Companion Diagnostic | Actionable | In a Phase III trial (ADMIRAL) that supported FDA approval, Xospata (gilteritinib) improved median overall survival (9.3 vs 5.6 mo, HR. 0.64, p<0.001) compared to chemotherapy, resulted in superior median event-free survival (2.8 vs 0.7 mo, HR 0.79) and rate of complete remission with full or partial hematologic recovery (34.0% vs 15.3%) in patients with relapsed or refractory acute myeloid leukemia harboring a FLT3 internal tandem duplication (ITD), D835, or I836 mutation (PMID: 31665578; NCT02421939). | detail... detail... 31665578 |
| EML4 - ALK ALK L1196M | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK L1196M in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 15 ins | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in the guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a FLT3 internal tandem duplication (FLT3-ITD) mutation (PMID: 32171751; ESMO.org). | 32171751 detail... |
| FLT3 exon 15 ins | acute myeloid leukemia | sensitive | Gilteritinib | FDA approved - On Companion Diagnostic | Actionable | In a Phase III trial (ADMIRAL) that supported FDA approval, Xospata (gilteritinib) improved median overall survival (9.3 vs 5.6 mo, HR. 0.64, p<0.001), median event-free survival (2.8 vs 0.7 mo, HR 0.79), and rate of complete remission with full or partial hematologic recovery (34.0% vs 15.3%) compared to chemotherapy in patients with relapsed or refractory acute myeloid leukemia harboring a FLT3 internal tandem duplication (ITD; exon 14/15 insertion), D835, or I836 mutation (PMID: 31665578; NCT02421939). | detail... 31665578 detail... |
| FLT3 exon 15 ins | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in the guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a FLT3 internal tandem duplication (FLT3-ITD) mutation (NCCN.org). | detail... |
| FLT3 exon23 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (PMID: 32171751; ESMO.org). | 32171751 detail... |
| FLT3 exon23 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (NCCN.org). | detail... |
| FLT3 exon18 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (NCCN.org). | detail... |
| FLT3 exon18 | acute myeloid leukemia | sensitive | Gilteritinib | Guideline | Actionable | Xospata (gilteritinib) is included in guidelines for patients with relapsed or refractory acute myeloid leukemia harboring a mutation in the FLT3 tyrosine kinase domain (exons 14-23) (PMID: 32171751; ESMO.org). | 32171751 detail... |
| FLT3 N701K | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed hematologic cells expressing FLT3 N701K were resistance to treatment with Xospata (gilteritinib) in culture (PMID: 33780043). | 33780043 |
| CBL Q367_E373delinsRLK FLT3 exon 14 ins FLT3 D835X NRAS G12D | acute myeloid leukemia | predicted - resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a clinical study, a patient with acute myeloid leukemia harboring FLT3-ITD and a D835 mutation progressed on Xospata (gilteritinib) treatment and was found to have acquired NRAS G12D and CBL Q367_E373delinsRLK (PMID: 31088841). | 31088841 |
| FLT3 exon 14 ins FLT3 M837I | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 M837I in culture (PMID: 32040554). | 32040554 |
| EML4 - ALK ALK F1174V | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK F1174V in culture (PMID: 33627640). | 33627640 |
| EML4 - ALK ALK C1156Y ALK I1171N | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) treatment inhibited Alk phosphorylation and viability of transformed cells expressing EML4-ALK with ALK I1171N and C1156Y in culture (PMID: 36201110). | 36201110 |
| FLT3 exon 14 ins FLT3 D835X NRAS G13C NRAS G13R | acute myeloid leukemia | predicted - resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a clinical study, a patient with acute myeloid leukemia harboring FLT3-ITD and a D835 mutation progressed on Xospata (gilteritinib) treatment and was found to have acquired NRAS G13C and G13R (PMID: 31088841). | 31088841 |
| EML4 - ALK ALK F1174I | Advanced Solid Tumor | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited viability of transformed cells expressing EML4-ALK with ALK F1174I in culture (PMID: 33627640). | 33627640 |
| FLT3 exon 14 ins FLT3 D835X NRAS Q61R | acute myeloid leukemia | predicted - resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a clinical study, a patient with acute myeloid leukemia harboring FLT3-ITD and a D835 mutation progressed on Xospata (gilteritinib) treatment and was found to have acquired NRAS Q61R in addition to WT1 L378Pfs*6 (PMID: 31088841). | 31088841 |
| FLT3 exon 14 ins FLT3 M664I | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 M664I in culture (PMID: 32040554). | 32040554 |
| CBL Y371H FLT3 wild-type | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) inhibited growth of transformed hematologic cells expressing CBL Y371H and wild-type FLT3 in culture (PMID: 31309543). | 31309543 |
| FLT3 exon 14 ins NRAS Q61K | acute myeloid leukemia | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring a FLT3-ITD mutation and expressing NRAS Q61K demonstrated resistance to treatment with Xospata (gilteritinib) in culture (PMID: 35395091). | 35395091 |
| FLT3 exon 14 ins NRAS Q61K | acute myeloid leukemia | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, acute myeloid leukemia cells harboring FLT3-ITD and NRAS Q61K were resistant to Xospata (gilteritinib) as demonstrated by increased cell growth and RAS/MAPK pathway activation in culture (PMID: 31088841). | 31088841 |
| FLT3 N841I | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 N841I in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 G846D | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 G846D in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 H721Y | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 H721Y in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 R845G | hematologic cancer | sensitive | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, Xospata (gilteritinib) resulted in reduced cell viability in transformed cells expressing FLT3 ITD with FLT3 R845G in culture (PMID: 32040554). | 32040554 |
| FLT3 exon 14 ins FLT3 D835X NRAS Q61H | acute myeloid leukemia | predicted - resistant | Gilteritinib | Case Reports/Case Series | Actionable | In a clinical study, a patient with acute myeloid leukemia harboring FLT3-ITD and a D835 mutation progressed on Xospata (gilteritinib) treatment and was found to have acquired NRAS Q61H (PMID: 31088841). | 31088841 |
| FLT3 exon 14 ins FLT3 G697S FLT3 D835V | hematologic cancer | resistant | Gilteritinib | Preclinical - Cell culture | Actionable | In a preclinical study, transformed cells expressing FLT3 ITD with FLT3 D835V and FLT3 G697S were resistant to Xospata (gilteritinib) in culture (PMID: 32040554). | 32040554 |
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| Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
|---|---|---|---|---|---|---|
| NCT02456883 | Phase I | Gilteritinib | Study to Investigate the Absorption, Metabolism and Excretion of [14C] ASP2215 in Patients With Advanced Solid Tumors | Completed | USA | 0 |
| NCT04027309 | Phase III | Midostaurin Gilteritinib | A Study of Gilteritinib Versus Midostaurin in Combination With Induction and Consolidation Therapy Followed by One-year Maintenance in Patients With Newly Diagnosed Acute Myeloid Leukemia or Myelodysplastic Syndromes With Excess Blasts-2 With FLT3 Mutations Eligible for Intensive Chemotherapy (HOVON 156 AML) | Active, not recruiting | SWE | NOR | NLD | LUX | LTU | IRL | FRA | FIN | ESP | DEU | CHE | BEL | AUT | AUS | 0 |
| NCT02421939 | Phase III | Cytarabine Cytarabine + Fludarabine + Idarubicin Cytarabine + Etoposide + Mitoxantrone Azacitidine Gilteritinib Filgrastim | A Study of ASP2215 Versus Salvage Chemotherapy in Patients With Relapsed or Refractory Acute Myeloid Leukemia (AML) With FMS-like Tyrosine Kinase (FLT3) Mutation | Active, not recruiting | USA | TUR | POL | ITA | ISR | GBR | FRA | ESP | DEU | CAN | BEL | 3 |
| NCT02561455 | Phase Ib/II | Gilteritinib | Rollover Study for Subjects Who Have Participated in an Astellas Sponsored ASP2215 Trial | Completed | USA | 0 |
| NCT03070093 | Expanded access | Gilteritinib | Expanded Access Study of Gilteritinib (ASP2215) in Patients With FMS-like Tyrosine Kinase 3 (FLT3) Mutated Relapsed or Refractory Acute Myeloid Leukemia (AML) or FLT3-Mutated AML in Complete Remission (CR) With Minimal Residual Disease (MRD) | Approved for marketing | USA | CAN | 1 |
| NCT02236013 | Phase I | Cytarabine + Idarubicin Gilteritinib | A Study of ASP2215 in Combination With Induction and Consolidation Chemotherapy in Patients With Newly Diagnosed Acute Myeloid Leukemia | Completed | USA | 0 |
| NCT02752035 | Phase II | Gilteritinib Azacitidine + Gilteritinib Azacitidine | A Study of ASP2215 (Gilteritinib) by Itself, ASP2215 Combined With Azacitidine or Azacitidine by Itself to Treat Adult Patients Who Have Recently Been Diagnosed With Acute Myeloid Leukemia With a FLT3 Gene Mutation and Who Cannot Receive Standard Chemotherapy | Active, not recruiting | USA | POL | ITA | GBR | FRA | ESP | DEU | CAN | BEL | AUS | 3 |
| NCT06225427 | Phase I | Gilteritinib | Gilteritinib for the Treatment of ALK NSCLC | Recruiting | USA | 0 |
| NCT02997202 | Phase III | Gilteritinib | A Trial of the FMS-like Tyrosine Kinase 3 (FLT3) Inhibitor Gilteritinib Administered as Maintenance Therapy Following Allogeneic Transplant for Patients With FLT3/Internal Tandem Duplication (ITD) Acute Myeloid Leukemia (AML) | Completed | USA | POL | NZL | ITA | GRC | GBR | FRA | ESP | DNK | DEU | CAN | BEL | AUS | 3 |
| NCT02927262 | Phase III | Gilteritinib | A Study of ASP2215 (Gilteritinib), Administered as Maintenance Therapy Following Induction/Consolidation Therapy for Subjects With FMS-like Tyrosine Kinase 3 (FLT3/ITD) Acute Myeloid Leukemia (AML) in First Complete Remission | Completed | USA | SWE | ROU | POL | ITA | ISR | HUN | GRC | GBR | FRA | ESP | DNK | DEU | CZE | CAN | BRA | 5 |
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