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Profile Name | MAP2K1 K57N |
Gene Variant Detail | |
Relevant Treatment Approaches | MEK inhibitor (Pan) MEK1 Inhibitor |
Molecular Profile | Indication/Tumor Type | Response Type | Relevant Treatment Approaches | Therapy Name | Approval Status | Evidence Type | Efficacy Evidence | References |
---|---|---|---|---|---|---|---|---|
MAP2K1 K57N | lymphatic system cancer | sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, a patient with refractory Erdheim-Chester disease harboring a MAP2K1 K57N mutation had a sustained clinical response to Mekinist (trametinib) for over 6 months (PMID: 26566875). | 26566875 |
MAP2K1 K57N | lung non-squamous non-small cell carcinoma | predicted - sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Mekinist (trametinib) treatment resulted in a radiographic response with a decrease in the size of multiple metastatic sites in a patient with non-squamous non-small cell lung cancer harboring MAP2K1 K57N (PMID: 36455195). | 36455195 |
MAP2K1 K57N | colorectal cancer | resistant | Panitumumab | Case Reports/Case Series | Actionable | In a retrospective analysis, two patients with metastatic RAS/BRAF wild-type colorectal cancer demonstrated progressive disease following treatment with Vectibix (panitumumab) and via analysis of archived pretreatment tumor biopsy samples and post-progression liquid biopsy both were found to harbor MAP2K1 K57N (PMID: 36419886). | 36419886 | |
MAP2K1 K57N | lung adenocarcinoma | sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Koselugo (selumetinib) inhibited phosphorylation of ERK in cells expressing MAP2K1 K57N and inhibited MAP2K1 K57N-dependent growth in cell culture (PMID: 18632602). | 18632602 |
MAP2K1 K57N | Advanced Solid Tumor | sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 K57N displayed sensitivity to the Mek inhibitor, Selumetinib (AZD6244), as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
MAP2K1 K57N | Advanced Solid Tumor | sensitive | PLX4720 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 K57N displayed sensitivity to the Braf inhibitor, PLX4720, as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 | |
MAP2K1 K57N | Advanced Solid Tumor | resistant | MEK1 Inhibitor | PD98059 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 K57N displayed resistance to the Mek inhibitor, PD98059, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
MAP2K1 K57N | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 K57N displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 | |
MAP2K1 K57N | Advanced Solid Tumor | resistant | GDC0879 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 K57N displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 | |
MAP2K1 K57N | Advanced Solid Tumor | resistant | MEK inhibitor (Pan) MEK1 Inhibitor | AZD8330 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 K57N displayed resistance to the Mek inhibitor, AZD8330, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
MAP2K1 K57N | Advanced Solid Tumor | sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Koselugo (selumetinib) inhibited colony formation of transformed cells expressing MAP2K1 K57N in culture (PMID: 25351745). | 25351745 |
MAP2K1 K57N | Advanced Solid Tumor | sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, Mekinist (trametinib) inhibited viability of a transformed cell line expressing MAP2K1 K57N in culture (PMID: 36442478). | 36442478 |
MAP2K1 K57N | Advanced Solid Tumor | sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Trametinib | Preclinical - Biochemical | Actionable | In a preclinical study, Mekinist (trametinib) inhibited Erk phosphorylation in transformed cells expressing MAP2K1 K57N in culture (PMID: 32641410). | 32641410 |
MAP2K1 K57N | Advanced Solid Tumor | predicted - sensitive | SCH772984 | Preclinical - Biochemical | Actionable | In a preclinical study, SCH772984 inhibited downstream signaling in transformed cells expressing MAP2K1 K57N in culture (PMID: 32641410). | 32641410 | |
MAP2K1 K57N | colorectal cancer | resistant | Cetuximab | Preclinical | Actionable | In a preclinical study, colorectal cancer cell lines expressing MAP2K1 K57N were insensitive to Erbitux (cetuximab) in culture (PMID: 26644315). | 26644315 | |
MAP2K1 K57N | colorectal cancer | resistant | Panitumumab | Preclinical | Actionable | In a preclinical study, colorectal cancer cell lines expressing MAP2K1 K57N were insensitive to Vectibix (panitumumab) in culture (PMID: 26644315). | 26644315 | |
MAP2K1 K57N | colorectal cancer | sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Cetuximab + Trametinib | Preclinical | Actionable | In a preclinical study, Erbitux (cetuximab) and Mekinist (trametinib) inhibited colorectal cancer cell lines expressing MAP2K1 K57N in culture (PMID: 26644315). | 26644315 |
MAP2K1 K57N | colorectal cancer | sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Panitumumab + Trametinib | Preclinical | Actionable | In a preclinical study, Vectibix (panitumumab) and Mekinist (trametinib) inhibited colorectal cancer cell lines expressing MAP2K1 K57N in culture (PMID: 26644315). | 26644315 |
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