Therapy Detail

Therapy Name Selumetinib
Synonym
Therapy Description

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Drug Name Trade Name Synonyms Drug Classes Drug Description
Selumetinib AZD6244|ARRY-142886 MEK inhibitor (Pan) 20 MEK1 Inhibitor 20 MEK2 Inhibitor 18 Selumetinib (AZD6244) inhibits mitogen-activated protein kinase kinases (MEK or MAPK/ERK kinases) 1 and 2, which may prevent the activation of MEK1/2-dependent effector proteins and transcription factors, reducing cellular proliferation in various cancers (PMID: 27467210).
Molecular Profile Indication/Tumor Type Response Type Therapy Name Approval Status Evidence Type Efficacy Evidence References
KRAS G12C pancreatic ductal adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, pancreatic ductal adenocarcinoma cells harboring KRAS G12C demonstrated reduced sensitivity to Selumetinib (AZD6244) in culture when compared to the combined therapy of Selumetinib (AZD6244) and SHP099 (PMID: 30045908). 30045908
MAP2K1 I103N melanoma resistant Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) did not inhibit proliferation of melanoma cells expressing Map2k1 I103N (PMID: 19915144). 19915144
Unknown unknown Advanced Solid Tumor not applicable Selumetinib Phase I Actionable In a Phase I trial, treatment with Selumetinib (AZD6244) demonstrated safety and preliminary efficacy patients with advanced solid tumors, with several patients achieving prolonged stable disease (PMID: 18390968). 18390968
Unknown unknown Advanced Solid Tumor not applicable Selumetinib Clinical Study Actionable In a meta-analysis, Selumetinib (AZD6244) was shown to have modest clinical efficacy as a monotherapy in a variety of solid tumors (PMID: 24716986). 24716986
MAP2K1 Q56P lung adenocarcinoma sensitive Selumetinib Preclinical Actionable In a preclinical study, a lung adenocarcinoma cell line harboring MAP2K1 Q56P demonstrated sensitivity to Selumetinib (AZD6244), resulting in decreased cell viability (PMID: 26582713). 26582713
ERBB2 S653C urinary bladder cancer decreased response Selumetinib Preclinical Actionable In a preclinical study, bladder cancer cells over expressing ERBB2 (HER2) S653C demonstrated reduced sensitivity to Selumetinib (AZD6244) in culture (PMID: 24971884). 24971884
MAP2K1 F53L Advanced Solid Tumor sensitive 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
KRAS G12C lung adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS G12C mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
Unknown unknown breast cancer not applicable Selumetinib Phase I Actionable In a Phase I trial, treatment with Selumetinib (AZD6244) demonstrated safety and preliminary efficacy patients with advanced solid tumors, including patients with breast cancer, with several patients achieving prolonged stable disease (PMID: 18390968). 18390968
MAP2K1 Q56P stomach cancer sensitive Selumetinib Preclinical Actionable In a preclinical study, selumetinib (AZD6244) inhibited growth of a gastric cancer cell line that requires MAP2K1 Q56P and inhibited phosphorylation of ERK in these cells (PMID: 22327936). 22327936
BRAF mutant melanoma sensitive Selumetinib Phase II Actionable In a Phase II trial in patients with advanced melanoma, 5/6 patients exhibiting a response to selumetinib had BRAF-mutant tumors (PMID: 22048237). 22048237
FGFR3-TACC3 urinary bladder cancer no benefit Selumetinib Preclinical Actionable In a preclinical study, bladder cancer cells harboring FGFR3-TACC were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
ERBB2 S310F urinary bladder cancer decreased response Selumetinib Preclinical Actionable In a preclinical study, bladder cancer cells over expressing ERBB2 (HER2) S310F demonstrated reduced sensitivity to Selumetinib (AZD6244) in culture (PMID: 24971884). 24971884
KRAS Q61H lung adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS Q61H mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
BRAF V600E thyroid cancer sensitive Selumetinib Preclinical - Cell line xenograft Actionable In a preclinical study, Selumetinib (AZD6244) inhibited growth of both parental thyroid cancer cell lines harboring BRAF V600E and those acquired Sprycel (dasatinib)-resistance in culture (PMID: 27222538). 27222538
GNA11 Q209L uveal melanoma predicted - sensitive Selumetinib Case Reports/Case Series Actionable In a Phase II trial, Selumetinib (AZD6244) treatment resulted in partial response in a patient with uveal melanoma harboring GNA11 Q209L (PMID: 24938562; NCT01143402). 24938562
FGFR3 S249C renal pelvis transitional cell carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, renal pelvis transitional cell carcinoma cells harboring FGFR3 S249C were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
MAP2K1 Q56P Advanced Solid Tumor sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 Q56P displayed sensitivity to the Mek inhibitor, Selumetinib (AZD6244), as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
KRAS G13C lung adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS G13C mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
BRAF V600E MAP2K1 H119P melanoma resistant Selumetinib Preclinical Actionable In a preclinical study, melanoma cells harboring BRAF V600E treated with Selumetinib (AZD6244) in culture demonstrated resistance, which was a result of the resistance mutation, MAP2K1 H119P (PMID: 19915144). 19915144
HRAS Q61L lung squamous cell carcinoma sensitive Selumetinib Preclinical - Cell line xenograft Actionable In a preclinical study, Selumetinib (AZD6244) inhibited growth of a lung squamous cell carcinoma cell line harboring HRAS Q61L in culture, and inhibited tumor growth in xenograft models (PMID: 26544513). 26544513
BRAF V600E MAP2K1 P124S melanoma decreased response Selumetinib Preclinical Actionable In a preclinical study, melanoma cells harboring BRAF V600E and MAP2K1 P124S demonstrated decreased sensitivity to Selumetinib (AZD6244) compared to cells harboring BRAF V600E alone in culture (PMID: 22197931). 22197931
KRAS G12V PTPN11 loss pancreatic ductal adenocarcinoma sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, CRISPR-Cas9-mediated knock-out of PTPN11 abolished reactivation of MAPK signaling in the presence of Selumetinib (AZD6244) in pancreatic ductal adenocarcinoma cells harboring KRAS G12V in culture, resulted in enhanced growth inhibition (PMID: 29808009). 29808009
BRAF V600E MAP2K1 V211D melanoma resistant Selumetinib Preclinical Actionable In a preclinical study, melanoma cells harboring BRAF V600E and expressing MAP2K V211D demonstrated resistance to growth inhibition by Selumetinib (AZD6244) in cell culture (PMID: 19915144). 19915144
MET amp non-small cell lung carcinoma sensitive Selumetinib Preclinical Actionable In a preclinical study, Selumetinib (AZD6244) suppressed the growth of an Iressa (gefitinib)-resistant NSCLC cell line with MET amplification (PMID: 24939055). 24939055
HRAS G13R KRAS G12R SRC T341M thyroid cancer sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) inhibited growth of Sprycel (dasatinib)-resistant thyroid cancer cell lines harboring KRAS G13R, HRAS G12R, and an acquired SRC T341M mutation in culture (PMID: 27222538). 27222538
KRAS Q61K lung adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS Q61K mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
MAP2K1 L115P melanoma resistant Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) did not inhibit proliferation of melanoma cells expressing Map2k1 L115P (PMID: 19915144). 19915144
KRAS G13D colorectal adenocarcinoma predicted - sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD-6244) inhibited proliferation of colorectal adenocarcinoma cells harboring KRAS G13D in culture (PMID: 26438159). 26438159
MAP2K1 K57N Advanced Solid Tumor sensitive 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
TP53 D259Y melanoma sensitive Selumetinib Preclinical Actionable In a preclinical study, Selumetinib (AZD6244) inhibited proliferation of human melanoma cells harboring TP53 D259Y in culture (PMID: 26343583). 26343583
KRAS G12S lung adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS G12S mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
FGFR2 amp stomach cancer resistant Selumetinib Preclinical Actionable In a preclinical study, Selumetinib (AZD-6244) did not inhibit growth of gastric cancer cells with FGFR2 amplification in culture (PMID: 19755509). 19755509
BRAF mutant thyroid cancer sensitive Selumetinib Phase I Actionable In a Phase I study, selumetinib demonstrated an increase in iodine uptake and retention in a subgroup of patients with thyroid cancer that was refractory to radioiodine; including patients with BRAF and NRAS mutations disease (PMID: 23406027). 23406027
GNAQ Q209P uveal melanoma sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) induced cell-cycle arrest and decreased viability of uveal melanoma cells harboring GNAQ Q209P in culture (PMID: 22550165). 22550165
STK11 inact mut Advanced Solid Tumor sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, the presence of an STK11 inactivating mutation and STK11 loss expression signature was associated with increased sensitivity to Selumetinib (AZD6244) in human tumor cell lines in culture (PMID: 27821489). 27821489
FGFR1 amp non-small cell lung carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified non-small cell lung carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
KRAS G12V pancreatic ductal adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, pancreatic ductal adenocarcinoma cells harboring KRAS G12V demonstrated reduced sensitivity to Selumetinib (AZD6244) in culture when compared to the combined therapy of Selumetinib (AZD6244) and SHP099 (PMID: 30045908). 30045908
Unknown unknown triple-receptor negative breast cancer not applicable Selumetinib Preclinical - Cell line xenograft Actionable In a preclinical study, the Mek inhibitor Selumetinib (AZD6244) inhibited tumorigenicity and invasiveness of triple-receptor negative breast cancer cell lines in culture and in cell line xenograft models (PMID: 26384399). 26384399
BRAF mutant colon cancer predicted - sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) resulted in some reduced cell growth in colon cancer cells harboring a BRAF mutation in culture (PMID: 27655129). 27655129
KRAS G12R lung adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS G12R mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
MAP2K1 C121S Advanced Solid Tumor sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 C121S displayed sensitivity to the Mek inhibitor, Selumetinib (AZD6244), as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
NRAS Q61L melanoma decreased response Selumetinib Preclinical Actionable In a preclinical study, Selumetinib (AZD6244) modestly inhibited proliferation of human melanoma cells harboring NRAS Q61L in culture (PMID: 26343583). 26343583
KRAS mutant lung adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS mutations due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
ERBB2 D277H ERBB2 S310F urinary bladder cancer decreased response Selumetinib Preclinical Actionable In a preclinical study, bladder cancer cells over expressing both ERBB2 (HER2) D277H and S310F demonstrated reduced sensitivity to Selumetinib (AZD6244) in culture (PMID: 24971884). 24971884
HRAS mutant Advanced Solid Tumor predicted - sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, human solid tumor cell lines harboring HRAS mutations demonstrated increased sensitivity to growth inhibition by Selumetinib (AZD6244) in culture compared to cell lines with wild-type HRAS (PMID: 26544513). 26544513
Unknown unknown uveal melanoma not applicable Selumetinib Phase II Actionable In a Phase II trial, Selumetinib (AZD6244) improved median progression-free survival (15.9 vs 7 weeks, HR=0.46, p<0.001) but not overall survival (11.8 vs 9.1 months, HR=0.66, p=0.09) compared to chemotherapy in patients with uveal melanoma, but also caused high adverse event rate (PMID: 24938562; NCT01143402). 24938562
GNA11 mutant uveal melanoma no benefit Selumetinib Phase II Actionable In a Phase II trial, Selumetinib (AZD6244) did not improved overall survival (10.9 vs 9.1 months, p=0.59) compared to chemotherapy in patients with uveal melanoma harboring GNAQ or GNA11 exon 5 mutations (n=83) (PMID: 24938562; NCT01143402). 24938562
NRAS G13D melanoma sensitive Selumetinib Preclinical Actionable In a preclinical study, Selumetinib (AZD6244) inhibited proliferation of human melanoma cells harboring NRAS G13D in culture (PMID: 26343583). 26343583
MAP2K1 F129L Advanced Solid Tumor sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 F129L displayed sensitivity to the Mek inhibitor, Selumetinib (AZD6244), as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
KRAS G12R pancreatic ductal adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, pancreatic ductal adenocarcinoma cells harboring KRAS G12R demonstrated reduced sensitivity to Selumetinib (AZD6244) in culture when compared to the combined therapy of Selumetinib (AZD6244) and SHP099 (PMID: 30045908). 30045908
MAP2K1 Q56P BRAF V600E melanoma resistant Selumetinib Preclinical Actionable In a preclinical study, melanoma cells harboring the MAP2K1 Q56P mutation in the presence of BRAF V600E were resistant to the MEK inhibitor, selumetinib (AZD6244), in cell culture (PMID: 19915144). 19915144
BRAF G469R NRAS Q61K melanoma decreased response Selumetinib Preclinical Actionable In a preclinical study, Selumetinib (AZD6244) modestly inhibited proliferation of human melanoma cells harboring BRAF G469R and NRAS Q61K in culture (PMID: 26343583). 26343583
FGFR2 K310R FGFR2 N549K endometrial carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring both FGFR2 K310R and N549K were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
KRAS G12C pancreatic adenocarcinoma sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, a pancreatic adenocarcinoma cell line harboring KRAS G12C demonstrated sensitivity to growth inhibition by Selumetinib (AZD6244) in culture (PMID: 28957417). 28957417
BRAF wild-type melanoma no benefit Selumetinib Phase II Actionable In a Phase II trial, a favorable response rate to Selumetinib (AZD6244) was observed in mutant BRAF, but not BRAF wild-type, melanoma patients (PMID: 22048237). 22048237
GNAQ Q209L uveal melanoma sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) induced cell-cycle arrest and decreased viability of uveal melanoma cells harboring GNAQ Q209L in culture (PMID: 22550165). 22550165
BRAF V600E colorectal cancer sensitive Selumetinib Preclinical - Cell line xenograft Actionable In a preclinical study, Selumetinib (AZD6244) decreased tumor growth in a cell line xenograft model of colorectal cancer harboring BRAF V600E (PMID: 23942066). 23942066
HRAS G12R KRAS G13R thyroid cancer sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) inhibited growth of thyroid cancer cell lines harboring KRAS G13R and HRAS G12R in culture (PMID: 27222538). 27222538
KRAS G12D PTPN11 loss pancreatic ductal adenocarcinoma sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, CRISPR-Cas9-mediated knock-out of PTPN11 abolished reactivation of MAPK signaling in the presence of Selumetinib (AZD6244) in pancreatic ductal adenocarcinoma cells harboring KRAS G12D, resulted in enhanced growth inhibition in culture (PMID: 29808009). 29808009
KRAS G12V ovarian serous carcinoma predicted - sensitive Selumetinib Case Reports/Case Series Actionable In a clinical case study, treatment with Selumetinib (AZD6244) resulted in lack of tumor progression for greater than 7 years in a patient with low grade serous ovarian carcinoma harboring KRAS G12V (PMID: 27231576). 27231576
MAP2K1 I111S Advanced Solid Tumor sensitive Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Map2k1 I111S displayed sensitivity to the Mek inhibitor, Selumetinib (AZD6244), as demonstrated by reversal of active Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
MAP2K1 V211D Advanced Solid Tumor resistant Selumetinib Preclinical Actionable In a preclinical study, Map2k1 V211D displayed resistance to the Mek inhibitor, Selumetinib (AZD6244), as demonstrated by constitutive activation of Map2k1 in transformed human kidney cells (PMID: 29753091). 29753091
KRAS G12D pancreatic ductal adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, pancreatic ductal adenocarcinoma cells harboring KRAS G12D demonstrated reduced sensitivity to Selumetinib (AZD6244) in culture when compared to the combined therapy of Selumetinib (AZD6244) and SHP099 (PMID: 30045908). 30045908
BRAF V600E MAP2K1 C121S melanoma decreased response Selumetinib Preclinical Actionable In a preclinical study, melanoma cell lines harboring BRAF V600E mutation and overexpressing MAP2K1 C121S were less sensitive than those overexpressing wild-type MAP2K1 to Selumetinib (AZD6244)-induced inhibition of Mapk pathway activation and cell proliferation in culture (PMID: 24448821). 24448821
KRAS G12V lung adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, Selumetinib (AZD6244) only moderately inhibited survival of lung adenocarcinoma cells harboring KRAS G12V mutation due to the adaptive activation of Met, Egfr, and Akt signaling in cells (PMID: 27422710). 27422710
FGFR1 amp lung squamous cell carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung squamous cell carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
BRAF V600E melanoma sensitive Selumetinib Phase II Actionable In a Phase II trial, a favorable response rate to selumetinib (AZD6244) was observed in mutant BRAF but not BRAF wild-type melanoma patients (PMID: 22048237). 22048237
GNAQ exon5 uveal melanoma no benefit Selumetinib Phase II Actionable In a Phase II trial, Selumetinib (AZD6244) did not improved overall survival (10.9 vs 9.1 months, p=0.59) compared to chemotherapy in patients with uveal melanoma harboring GNAQ or GNA11 exon 5 mutations (n=83) (PMID: 24938562; NCT01143402). 24938562
FGFR2 S252W endometrial carcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring FGFR2 S252W demonstrated decreased sensitivity to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
KRAS mutant gastric adenocarcinoma sensitive Selumetinib Preclinical Actionable In a preclinical study, gastric cancer cell lines with Kras mutations were sensitive to Selumetinib (AZD6244) (PMID: 24935174). 24935174
KRAS Q61R pancreatic ductal adenocarcinoma decreased response Selumetinib Preclinical - Cell culture Actionable In a preclinical study, pancreatic ductal adenocarcinoma cells harboring KRAS Q61R demonstrated reduced sensitivity to Selumetinib (AZD6244) in culture when compared to the combined therapy of Selumetinib (AZD6244) and SHP099 (PMID: 30045908). 30045908
FGFR2 amp colorectal adenocarcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, FGFR2 amplified colorectal adenocarcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
NRAS mutant thyroid cancer sensitive Selumetinib Phase I Actionable In a Phase I study, selumetinib demonstrated an increase in iodine uptake and retention in a subgroup of patients with thyroid cancer that was refractory to radioiodine; including patients with BRAF and NRAS mutations disease (PMID: 23406027). 23406027
FGFR2 N549K endometrial carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, endometrial carcinoma cells harboring FGFR2 N549K were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
FGFR1 amp lung small cell carcinoma no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, FGFR1 amplified lung small cell carcinoma cells were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
Unknown unknown multiple myeloma no benefit Selumetinib Phase II Actionable In a Phase II clinical trial, Selumetinib (AZD6244) demonstrated safety and tolerability but had minimal activity with a complete response achieved in 5.6% (2/36) of refractory multiple myeloma patients (PMID: 26446942). 26446942
KRAS G12D lung adenocarcinoma decreased response Selumetinib Preclinical Actionable In a preclinical study, the treatment of a mouse model lung adenocarcinoma harboring the KRAS G12D mutant with selumetinib, a MEK inhibitor, resulted in modest tumor regression (PMID: 19029981). 19029981
MAP2K1 P124L melanoma resistant Selumetinib Preclinical Actionable In a preclinical study, transformed human melanoma cells expressing MAP2K1 P124L demonstrated resistance to the MEK inhibitor, Selumetinib (AZD6244) (PMID: 19915144). 19915144
NRAS Q61K melanoma sensitive Selumetinib Preclinical Actionable In a preclinical study, Selumetinib (AZD6244) inhibited proliferation of human melanoma cell lines harboring NRAS Q61K in culture (PMID: 26343583). 26343583
FGFR3 Y373C myeloid neoplasm no benefit Selumetinib Preclinical - Cell culture Actionable In a preclinical study, myeloma cells harboring FGFR3 Y373C were not sensitive to Selumetinib (AZD-6244) in culture (PMID: 26438159). 26438159
MAP2K1 K57N lung adenocarcinoma sensitive Selumetinib Preclinical Actionable In a preclinical study, selumetinib (AZD6244) inhibited phosphorylation of ERK in cells expressing MAP2K1 K57N and inhibited MAP2K1 K57N-dependent growth in cell culture (PMID: 18632602). 18632602
Clinical Trial Phase Therapies Title Recruitment Status
NCT02407405 Phase II Selumetinib Selumetinib in Treating Patients With Neurofibromatosis Type 1 and Plexiform Neurofibromas That Cannot Be Removed by Surgery Recruiting
NCT01843062 Phase III Selumetinib Study Comparing Complete Remission After Treatment With Selumetinib/Placebo in Patient With Differentiated Thyroid Cancer Completed
NCT03109301 Phase II Selumetinib A Phase II Trial of the Mitogen Activated Protein Kinase Kinase (MEK1/2) Inhibitor Selumetinib (AZD6244 Hydrogen Sulfate) in Patients With Neurofibromatosis Type 1 (NF1) Mutated Gastrointestinal Stromal Tumors (GIST) Withdrawn
NCT01089101 Phase Ib/II Selumetinib Selumetinib in Treating Young Patients With Recurrent or Refractory Low Grade Glioma Recruiting
NCT01362803 Phase Ib/II Selumetinib AZD6244 Hydrogen Sulfate for Children With Nervous System Tumors Active, not recruiting
NCT02839720 Phase II Selumetinib Selumetinib in Treating Patients With Neurofibromatosis Type 1 and Dermal Neurofibroma Recruiting
NCT03095248 Phase II Selumetinib Trial of Selumetinib in Patients With Neurofibromatosis Type II Related Tumors Recruiting
NCT03213691 Phase II Selumetinib Selumetinib Sulfate in Treating Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphoma, or Histiocytic Disorders With Activating MAPK Pathway Mutations (A Pediatric MATCH Treatment Trial) Recruiting
NCT02768766 Phase I Selumetinib Intermittent Selumetinib for Uveal Melanoma Recruiting
NCT03155620 Phase II Tazemetostat Larotrectinib LY3023414 Vemurafenib Palbociclib Olaparib Ulixertinib Erdafitinib Selumetinib Ensartinib Targeted Therapy Directed by Genetic Testing in Treating Pediatric Patients With Relapsed or Refractory Advanced Solid Tumors, Non-Hodgkin Lymphomas, or Histiocytic Disorders (The Pediatric MATCH Screening Trial) Recruiting
NCT02337530 Phase II Selumetinib Cisplatin + Pemetrexed Selumetinib in Patients Receiving Pemetrexed and Cisplatin in Advanced or Metastatic KRAS Wildtype or Unknown Non-Squamous Non-Small Cell Lung Cancer Active, not recruiting
NCT02393690 Phase II Selumetinib Iodine I-131 With or Without Selumetinib in Treating Patients With Recurrent or Metastatic Thyroid Cancer Recruiting
NCT01306045 Phase II Erlotinib Lapatinib MK2206 Sunitinib Selumetinib Molecular Profiling and Targeted Therapy for Advanced Non-Small Cell Lung Cancer, Small Cell Lung Cancer, and Thymic Malignancies Recruiting
NCT03259633 Expanded access Selumetinib An Intermediate Access Protocol for Selumetinib for Treatment of Neurofibromatosis Type 1 Available
NCT01783197 Phase I Selumetinib Study of Selumetinib in Patients With Previously Treated or Untreated Advanced/Metastatic NSCLC Completed
NCT03040986 Phase II Selumetinib Selumetinib Sulfate in Treating Patients With Locally Advanced or Metastatic Pancreatic Cancer With KRAS G12R Mutations Active, not recruiting
NCT02188264 Phase I Cyclosporine Selumetinib Selumetinib and Cyclosporine in Treating Patients With Advanced Solid Tumors or Advanced or Metastatic Colorectal Cancer Active, not recruiting