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Drug Name	Trade Name	Synonyms	Drug Classes	Drug Description
PLX4720		PLX-4720\|PLX 4720	BRAF Inhibitor 26	PLX4720 is a 7-azaindole derivative and RAF kinase inhibitor with greater affinity for BRAF V600E than BRAF wild-type, which may induce cell cycle arrest and apoptosis, and lead to tumor growth inhibition and regression (PMID: 18287029).

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Molecular Profile	Indication/Tumor Type	Response Type	Therapy Name	Approval Status	Evidence Type	Efficacy Evidence	References
BRAF V600E	melanoma	sensitive	PLX4720	Preclinical - Cell line xenograft	Actionable	In a preclinical study, PLX4720 inhibited growth of melanoma cells harboring BRAF V600E in culture and in cell line xenograft models (PMID: 18287029).	18287029
BRAF V600E	colon cancer	sensitive	PLX4720	Preclinical - Cell line xenograft	Actionable	In a preclinical study, PLX4720 inhibited growth of colon cancer cells harboring BRAF V600E in culture and in cell line xenograft models (PMID: 18287029).	18287029
BRAF V600E	glioblastoma	decreased response	PLX4720	Preclinical - Cell line xenograft	Actionable	In a preclinical study, a glioblastoma cell line harboring BRAF V600E demonstrated a decreased response to treatment with PLX4720, demonstrating increased viability of CD133 positive cells in culture and in xenograft models (PMID: 26573800).	26573800
BRAF wild-type	melanoma	resistant	PLX4720	Preclinical - Cell line xenograft	Actionable	In a preclinical study, PLX4720 did not inhibit growth of BRAF wild-type melanoma cells in culture or in cell line xenograft models (PMID: 18287029).	18287029
NRAS Q61L	melanoma	resistant	PLX4720	Preclinical - Cell line xenograft	Actionable	In a preclinical study, PLX4720 did not inhibit growth of melanoma cells harboring NRAS Q61L in culture or in cell line xenograft models (PMID: 25500121, PMID: 23431193).	25500121 23431193
BRAF mutant	colorectal cancer	decreased response	PLX4720	Preclinical - Cell culture	Actionable	In a preclinical study, BRAF mutant colorectal cancer cell lines demonstrated reduced sensitivity to PLX4720 in culture (PMID: 26351322).	26351322
BRAF V600E MAP2K1 L115R	melanoma	resistant	PLX4720	Preclinical - Cell culture	Actionable	In a preclinical study, expression of MAP2K1 L115R in melanoma cells harboring BRAF V600E conferred resistance to PLX4720 treatment in culture (PMID: 19915144).	19915144
BRAF V600E MAP2K1 P124L	melanoma	resistant	PLX4720	Preclinical - Cell culture	Actionable	In a preclinical study, expression of MAP2K1 P124L in melanoma cells harboring BRAF V600E conferred resistance to PLX4720 treatment in culture (PMID: 19915144).	19915144
MAP2K1 C121S	Advanced Solid Tumor	sensitive	PLX4720	Preclinical - Cell culture	Actionable	In a preclinical study, Map2k1 C121S displayed sensitivity to the Braf inhibitor, PLX4720, as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091).	29753091
MAP2K1 F129L	Advanced Solid Tumor	sensitive	PLX4720	Preclinical - Cell culture	Actionable	In a preclinical study, Map2k1 F129L 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	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 I111S	Advanced Solid Tumor	sensitive	PLX4720	Preclinical - Cell culture	Actionable	In a preclinical study, Map2k1 I111S 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	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 Q56P	Advanced Solid Tumor	sensitive	PLX4720	Preclinical - Cell culture	Actionable	In a preclinical study, Map2k1 Q56P displayed sensitivity to the Braf inhibitor, PLX4720, as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091).	29753091
MAP2K1 V211D	Advanced Solid Tumor	sensitive	PLX4720	Preclinical - Cell culture	Actionable	In a preclinical study, Map2k1 V211D displayed sensitivity to the Braf inhibitor, PLX4720, as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091).	29753091
BRAF T529I BRAF V600E	Advanced Solid Tumor	predicted - resistant	PLX4720	Preclinical	Actionable	In a preclinical study, transformed cells expressing BRAF V600E and the gatepkeeper mutation BRAF T529I were insensitive to PLX4720-mediated inhibition of ERK signaling in culture (PMID: 20538618).	20538618
BRAF T529M BRAF V600E	Advanced Solid Tumor	predicted - resistant	PLX4720	Preclinical	Actionable	In a preclinical study, transformed cells expressing BRAF V600E and the gatepkeeper mutation BRAF T529M were insensitive to PLX4720-mediated inhibition of ERK signaling in culture (PMID: 20538618).	20538618
BRAF T529N BRAF V600E	Advanced Solid Tumor	resistant	PLX4720	Preclinical	Actionable	In a preclinical study, transformed cells expressing BRAF V600E and the gatepkeeper mutation BRAF T529N were insensitive to PLX4720 in culture (PMID: 20538618).	20538618
BRAF V600E	Advanced Solid Tumor	sensitive	PLX4720	Preclinical	Actionable	In a preclinical study, PLX4720 inhibited Erk phosphorylation and cell proliferation of transformed cells expression BRAF V600E in culture (PMID: 20538618).	20538618
BRAF V600E MAP2K1 C121S	melanoma	resistant	PLX4720	Preclinical	Actionable	In a preclinical study, expression of MAP2K1 C121S conferred resistance to PLX4720 in melanoma cells harboring BRAF V600E in culture (PMID: 21383288).	21383288
BRAF V600E MAP2K1 Q56P	melanoma	resistant	PLX4720	Preclinical	Actionable	In a preclinical study, expression of MAP2K1 Q56P in melanoma cells harboring BRAF V600E conferred resistance to PLX4720 treatment in culture (PMID: 19915144).	19915144

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