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Profile Name MAP2K1 K57N
Gene Variant Detail

MAP2K1 K57N (gain of function)

Relevant Treatment Approaches MEK inhibitor (Pan) MEK1 Inhibitor

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Molecular Profile Indication/Tumor Type Response Type Relevant Treatment Approaches Therapy Name Approval Status Evidence Type Efficacy Evidence References
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 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
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 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 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 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