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Profile Name | MAP2K1 F53L |
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 F53L | colorectal cancer | sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Trametinib | Preclinical | Actionable | In a preclinical study, a colorectal cancer cell line harboring MAP2K1 F53L demonstrated sensitivity to Mekinist (trametinib) in culture, resulting in decreased cell viability (PMID: 26582713). | 26582713 |
MAP2K1 F53L | colorectal cancer | resistant | Cetuximab | Preclinical - Cell culture | Actionable | In a preclinical study, expression of MAP2K1 F53L conferred resistance to Erbitux (cetuximab) in colorectal cancer cells in culture (PMID: 28179366). | 28179366 | |
MAP2K1 F53L | colorectal cancer | sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Cetuximab + Trametinib | Preclinical - Cell culture | Actionable | In a preclinical study, the combination of Erbitux (cetuximab) and Mekinist (trametinib) decreased viability of colorectal cancer cells harboring MAP2K1 F53L in culture (PMID: 28179366). | 28179366 |
MAP2K1 F53L | Advanced Solid Tumor | sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Selumetinib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 F53L displayed sensitivity to the Mek inhibitor, Selumetinib (AZD6244), as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
MAP2K1 F53L | Advanced Solid Tumor | sensitive | PLX4720 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 F53L displayed sensitivity to the Braf inhibitor, PLX4720, as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 | |
MAP2K1 F53L | Advanced Solid Tumor | resistant | MEK1 Inhibitor | PD98059 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 F53L displayed resistance to the Mek inhibitor, PD98059, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
MAP2K1 F53L | Advanced Solid Tumor | resistant | Regorafenib | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 F53L displayed resistance to Stivarga (regorafenib; BAY 73-4506), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 | |
MAP2K1 F53L | Advanced Solid Tumor | resistant | GDC0879 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 F53L displayed resistance to the Braf inhibitor, GDC-0879, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 | |
MAP2K1 F53L | Advanced Solid Tumor | resistant | MEK inhibitor (Pan) MEK1 Inhibitor | AZD8330 | Preclinical - Cell culture | Actionable | In a preclinical study, Map2k1 F53L displayed resistance to the Mek inhibitor, AZD8330, as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). | 29753091 |
MAP2K1 F53L | histiocytic sarcoma | predicted - sensitive | MEK inhibitor (Pan) MEK1 Inhibitor | Trametinib | Case Reports/Case Series | Actionable | In a clinical case study, Mekinist (trametinib) treatment resulted in resolution of symptoms within 3 days and a durable complete response for over 2 years in a patient with histiocytic sarcoma harboring MAP2K1 F53L (PMID: 29768143). | 29768143 |
MAP2K1 F53L | 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 F53L in culture (PMID: 25351745). | 25351745 |
MAP2K1 F53L | 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 F53L in culture (PMID: 36442478). | 36442478 |
MAP2K1 F53L | 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 F53L in culture (PMID: 32641410). | 32641410 |