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Therapy Name | Gilteritinib + Trametinib |
Synonyms | |
Therapy Description | |
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). |
Trametinib | Mekinist | GSK1120212 | MEK inhibitor (Pan) 26 MEK1 Inhibitor 26 MEK2 Inhibitor 24 | Mekinist (trametinib) inhibits MEK 1 and 2, which potentially leads to reduced tumor cell proliferation (PMID: 27956260). Mekinist (trametinib) is FDA approved for melanoma patients harboring BRAF V600E or BRAF V600K mutations, and in combination with Tafinlar (dabrafenib) for BRAF V600E/K-mutant melanoma, BRAF V600E- mutant non-small cell lung cancer, BRAF V600E-mutant anaplastic thyroid cancer, for adult and pediatric patients of 6 years or older with unresectable or metastatic solid tumors harboring BRAF V600E, and for pediatric patients of 1 year or older with low-grade glioma harboring BRAF V600E (FDA.gov). |
Molecular Profile | Indication/Tumor Type | Response Type | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
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FLT3 exon 14 ins NRAS G12C | acute myeloid leukemia | sensitive | Gilteritinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Xospata (gilteritinib) and Mekinist (trametinib) inhibited cell growth in acute myeloid leukemia cells harboring FLT3-ITD and NRAS G12C in culture (PMID: 31088841). | 31088841 |
FLT3 exon 14 ins NRAS Q61K | acute myeloid leukemia | sensitive | Gilteritinib + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Xospata (gilteritinib) and Mekinist (trametinib) inhibited cell growth in acute myeloid leukemia cells harboring FLT3-ITD and NRAS Q61K in culture (PMID: 31088841). | 31088841 |
Clinical Trial | Phase | Therapies | Title | Recruitment Status | Covered Countries | Other Countries |
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