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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
E6201			FLT3 Inhibitor 69 MEK1 Inhibitor 27	E6201 is a dual inhibitor of MEK1 and FLT3, which may lead to decreased tumor cell growth (Blood Nov 2013, 122 (21) 2683; PMID: 23039341, PMID: 29867224, PMID: 30264293).

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Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
BRAF V600E	melanoma	sensitive	E6201	Case Reports/Case Series	Actionable	In a Phase I trial, a patient with metastatic melanoma and brain metastasis harboring BRAF V600E demonstrated an ongoing near complete response with an overall survival of more than 8 years, and preclinical analysis of melanoma cell lines harboring homozygous or heterozygous BRAF V600E in culture were sensitive to treatment with E6201 (PMID: 30264293).	30264293
BRAF mut PTEN mut	melanoma	decreased response	E6201	Preclinical - Cell line xenograft	Actionable	In a preclinical study, E6201 resulted in a cytostatic response in melanoma cell lines harboring both BRAF and PTEN mutations in culture and only inhibited tumor growth at very high doses in cell line xenograft models (PMID: 23039341).	23039341
BRAF mut PTEN wild-type	melanoma	sensitive	E6201	Preclinical - Cell line xenograft	Actionable	In a preclinical study, E6201 resulted in a cytocidal response in PTEN wild-type melanoma cell lines harboring BRAF mutations in culture and inhibited tumor growth in cell line xenograft models (PMID: 23039341).	23039341
FLT3 exon 14 ins	leukemia	sensitive	E6201	Preclinical - Cell line xenograft	Actionable	In a preclinical study, E6201 induced growth inhibition and apoptosis in leukemia cell lines harboring FLT3 internal tandem duplications (ITD) and reduced tumor burden in xenograft models (PMID: 26822154).	26822154
FLT3 Y599_D600insSTDNEYFYVDFREYEY	acute myeloid leukemia	predicted - sensitive	E6201	Preclinical - Cell line xenograft	Actionable	In a preclinical study, E6201 induced cell death, inhibited cell growth, and decreased tumor burden in acute myeloid leukemia cells harboring FLT3-ITD mutations in culture and in cell line xenograft models (Blood Nov 2013, 122 (21) 2683).	detail...
FLT3 D835G	acute myeloid leukemia	sensitive	E6201	Preclinical - Cell culture	Actionable	In a preclinical study, E6201 induced apoptosis in blast samples derived from acute myeloid leukemia patients harboring FLT3 D835G in culture (PMID: 26822154).	26822154
FLT3 D835Y	acute myeloid leukemia	sensitive	E6201	Preclinical - Cell culture	Actionable	In a preclinical study, E6201 induced apoptosis in blast samples derived from acute myeloid leukemia patients harboring FLT3 D835Y in culture (PMID: 26822154).	26822154
FLT3 exon 14 ins	acute myeloid leukemia	sensitive	E6201	Preclinical - Cell culture	Actionable	In a preclinical study, E6201 induced apoptosis in blast samples derived from acute myeloid leukemia patients harboring FLT3 internal tandem duplications (ITD) in culture (PMID: 26822154).	26822154
BRAF mutant	melanoma	sensitive	E6201	Preclinical	Actionable	In a preclinical study, E6201 inhibited proliferation of several melanoma cell lines in culture and hypersensitivity was associated with BRAF mutations (PMID: 23039341).	23039341
BRAF V600E	melanoma	sensitive	E6201	Preclinical	Actionable	In a preclinical study, E6201 inhibited Mapk pathway activation and proliferation of melanoma cell lines harboring BRAF V600E mutation in culture (PMID: 24448821).	24448821
BRAF V600E MAP2K1 C121S	melanoma	sensitive	E6201	Preclinical	Actionable	In a preclinical study, E6201 inhibited Mapk pathway activation and proliferation of melanoma cell line harboring BRAF V600E mutation and overexpressing MAP2K1 C121S in culture (PMID: 24448821).	24448821
FLT3 D835G	leukemia	sensitive	E6201	Preclinical	Actionable	In a preclinical study, E6201 inhibited proliferation and induced apoptosis in FLT3 inhibitor-resistant leukemia cell lines over expressing FLT3 D835G in culture (PMID: 26822154).	26822154
FLT3 D835Y	leukemia	sensitive	E6201	Preclinical	Actionable	In a preclinical study, E6201 inhibited proliferation and induced apoptosis in FLT3 inhibitor-resistant leukemia cell lines over expressing FLT3 D835Y in culture (PMID: 26822154).	26822154
FLT3 exon 14 ins FLT3 F691L	leukemia	sensitive	E6201	Preclinical	Actionable	In a preclinical study, E6201 inhibited proliferation and induced apoptosis in FLT3 inhibitor-resistant leukemia cell lines harboring FLT3 F691L in addition to FLT3 internal tandem duplications (ITD) in culture (PMID: 26822154).	26822154
FLT3 exon 14 ins FLT3 N676D FLT3 Y842C	leukemia	sensitive	E6201	Preclinical	Actionable	In a preclinical study, E6201 inhibited proliferation and induced apoptosis in FLT3 inhibitor-resistant leukemia cell lines harboring FLT3 N676D and Y842C in addition to FLT3 internal tandem duplications (ITD) in culture (PMID: 26822154).	26822154
FLT3 exon 14 ins FLT3 Y842C	leukemia	sensitive	E6201	Preclinical	Actionable	In a preclinical study, E6201 inhibited proliferation and induced apoptosis in FLT3 inhibitor-resistant leukemia cell lines harboring FLT3 Y842C in addition to FLT3 internal tandem duplications (ITD) in culture (PMID: 26822154).	26822154
FLT3 mutant	acute myeloid leukemia	sensitive	E6201	Preclinical	Actionable	In a preclinical study, acute myeloid leukemia cell lines harboring FLT3 mutations demonstrated increased sensitivity to E6201 induced growth inhibition and apoptosis in culture compared to FLT3 wild-type cells (PMID: 26822154).	26822154
HRAS wild-type	melanoma	sensitive	E6201	Preclinical	Actionable	In a preclinical study, E6201 inhibited proliferation of several melanoma cell lines in culture and hypersensitivity was associated with wild-type HRAS (PMID: 23039341).	23039341
NRAS wild-type	melanoma	sensitive	E6201	Preclinical	Actionable	In a preclinical study, E6201 inhibited proliferation of several melanoma cell lines in culture and hypersensitivity was associated with wild-type NRAS (PMID: 23039341).	23039341
PTEN wild-type	melanoma	sensitive	E6201	Preclinical	Actionable	In a preclinical study, E6201 inhibited proliferation of several melanoma cell lines in culture and sensitivity was associated with wild-type PTEN (PMID: 23039341).	23039341

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Clinical Trial	Phase	Therapies	Title	Recruitment Status	Covered Countries	Other Countries
NCT02418000	Phase Ib/II	E6201	A Study of E6201 for the Treatment of Advanced Hematologic Malignancies With FLT3 Mutation	Terminated	USA	0
NCT03332589	Phase I	Dabrafenib + E6201 E6201	E6201 Plus Dabrafenib for the Treatment of Metastatic Melanoma Central Nervous System Metastases (CNS)	Terminated	USA	0

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