Selumetinib

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Information
Drug Name
Selumetinib
Description
Entry(CIViC)
42
CIViC
Disease Mutation EL ET ED CS VO TR Pubmed Links
colorectal cancer KRAS MUTATION KRAS MUTATION D Predictive Supports Sensitivity/Response Somatic 3 21985784 Detail
melanoma BRAF p.Val640Glu (p.V640E)
( ENST00000288602.11, ENST00000496384.7, ENST00000644969.2, ENST00000646891.2 ) BRAF p.Val640Glu (p.V640E)
( ENST00000288602.11, ENST00000496384.7, ENST00000644969.2, ENST00000646891.2 )
D Predictive Supports Sensitivity/Response Somatic 2 26678033 Detail
uveal melanoma DDX43 OVEREXPRESSION
( ENST00000370336.5 ) DDX43 OVEREXPRESSION
( ENST00000370336.5 )
D Predictive Supports Resistance Somatic 4 24899684 Detail
acute myeloid leukemia KIT p.Leu863= (p.L863=)
( ENST00000689994.1, ENST00000687246.1, ENST00000288135.6, ENST00000412167.7, ENST00000686011.1, ENST00000687109.1, ENST00000687295.1, ENST00000689832.1, ENST00000690543.1, ENST00000692783.1 ) KIT p.Leu863= (p.L863=)
( ENST00000412167.7, ENST00000288135.6, ENST00000686011.1, ENST00000687109.1, ENST00000687246.1, ENST00000687295.1, ENST00000689832.1, ENST00000689994.1, ENST00000690543.1, ENST00000692783.1 )
B Predictive Supports Sensitivity/Response Common Germline 1 24178622 Detail
acute myeloid leukemia FLT3 ITD FLT3 ITD B Predictive Supports Resistance Somatic 2 24178622 Detail
melanoma TBK1 OVEREXPRESSION
( ENST00000331710.10 ) TBK1 OVEREXPRESSION
( ENST00000331710.10 )
D Predictive Supports Sensitivity/Response N/A 2 24962318 Detail
lung non-small cell carcinoma KRAS p.Gly12Cys (p.G12C)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Gly12Cys (p.G12C)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 )
B Predictive Supports Sensitivity/Response Somatic 3 26125448 Detail
lung non-small cell carcinoma KRAS p.Gly12Val (p.G12V)
( ENST00000688940.1, ENST00000692768.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000693229.1 ) KRAS p.Gly12Val (p.G12V)
( ENST00000693229.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1 )
B Predictive Supports Sensitivity/Response Somatic 1 26125448 Detail
lung non-small cell carcinoma STK11 LOSS
( ENST00000326873.12 ) STK11 LOSS
( ENST00000326873.12 )
D Predictive Supports Resistance Somatic 3 22425996 Detail
lung non-small cell carcinoma TP53 DELETERIOUS MUTATION TP53 DELETERIOUS MUTATION D Predictive Supports Sensitivity/Response Somatic 3 22425996 Detail
cancer ERBB3 OVEREXPRESSION
( ENST00000267101.8 ) ERBB3 OVEREXPRESSION
( ENST00000267101.8 )
D Predictive Supports Sensitivity/Response N/A 3 24685132 Detail
cancer ERBB3 OVEREXPRESSION
( ENST00000267101.8 ) ERBB3 OVEREXPRESSION
( ENST00000267101.8 )
D Predictive Supports Resistance N/A 4 24685132 Detail
melanoma MAP2K1 p.Pro124Ser (p.P124S)
( ENST00000685172.1, ENST00000692683.1, ENST00000685763.1, ENST00000307102.10, ENST00000693150.1, ENST00000689951.1, ENST00000691937.1, ENST00000686347.1, ENST00000691576.1 ) MAP2K1 p.Pro124Ser (p.P124S)
( ENST00000307102.10, ENST00000685172.1, ENST00000685763.1, ENST00000686347.1, ENST00000689951.1, ENST00000691576.1, ENST00000691937.1, ENST00000692683.1, ENST00000693150.1 )
D Predictive Supports Resistance Somatic 3 19915144 Detail
uveal melanoma GNA11 Q209 GNA11 Q209 B Predictive Does Not Support Sensitivity/Response Somatic 3 24938562 Detail
uveal melanoma GNAQ Q209 GNAQ Q209 B Predictive Does Not Support Sensitivity/Response Somatic 3 24938562 Detail
melanoma MAP2K1 p.Gln56Pro (p.Q56P)
( ENST00000307102.10, ENST00000689951.1, ENST00000691937.1, ENST00000686347.1, ENST00000691576.1, ENST00000685172.1, ENST00000685763.1, ENST00000692683.1, ENST00000693150.1 ) MAP2K1 p.Gln56Pro (p.Q56P)
( ENST00000307102.10, ENST00000685172.1, ENST00000685763.1, ENST00000686347.1, ENST00000689951.1, ENST00000691576.1, ENST00000691937.1, ENST00000692683.1, ENST00000693150.1 )
D Predictive Supports Resistance Somatic 3 19915144 Detail
colorectal cancer KRAS EXON 2 MUTATION KRAS EXON 2 MUTATION B Predictive Supports Sensitivity/Response Somatic 1 25322874 Detail
skin melanoma NRAS Q61 NRAS Q61 C Predictive Supports Sensitivity/Response Somatic 2 18390968 Detail
skin melanoma NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 ) NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 )
D Predictive Supports Sensitivity/Response Somatic 2 22194965 Detail
ovarian serous carcinoma MAP2K1 p.Gln56_Val60del (p.Q56_V60del)
( ENST00000307102.10, ENST00000685172.1, ENST00000685763.1, ENST00000686347.1, ENST00000689951.1, ENST00000691576.1, ENST00000691937.1, ENST00000692683.1, ENST00000693150.1 ) MAP2K1 p.Gln56_Val60del (p.Q56_V60del)
( ENST00000685172.1, ENST00000692683.1, ENST00000685763.1, ENST00000693150.1, ENST00000307102.10, ENST00000689951.1, ENST00000691937.1, ENST00000686347.1, ENST00000691576.1 )
C Predictive Supports Sensitivity/Response Somatic 4 26324360 Detail
thyroid gland carcinoma NF2 LOSS
( ENST00000338641.10 ) NF2 LOSS
( ENST00000338641.10 )
D Predictive Supports Sensitivity/Response Somatic 4 26359368 Detail
plexiform neurofibroma NF1 MUTATION NF1 MUTATION B Predictive Supports Sensitivity/Response Rare Germline 3 28029918 Detail
colorectal cancer KRAS p.Gly12Val (p.G12V)
( ENST00000688940.1, ENST00000692768.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000693229.1 ) KRAS p.Gly12Val (p.G12V)
( ENST00000693229.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1 )
D Predictive Supports Sensitivity/Response Somatic 3 22392911 Detail
colorectal cancer KRAS p.Gly13Asp (p.G13D)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000685328.1, ENST00000557334.6, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Gly13Asp (p.G13D)
( ENST00000556131.2, ENST00000557334.6, ENST00000256078.10, ENST00000311936.8, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 )
D Predictive Supports Sensitivity/Response Somatic 2 22392911 Detail
colorectal cancer NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 ) NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 )
D Predictive Supports Sensitivity/Response Somatic 3 22392911 Detail
colorectal cancer KRAS p.Ala146Thr (p.A146T)
( ENST00000256078.10, ENST00000311936.8, ENST00000557334.6, ENST00000685328.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Ala146Thr (p.A146T)
( ENST00000256078.10, ENST00000311936.8, ENST00000557334.6, ENST00000685328.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 )
D Predictive Supports Sensitivity/Response Somatic 3 22392911 Detail
colorectal cancer KRAS p.Ala146Val (p.A146V)
( ENST00000311936.8, ENST00000557334.6, ENST00000256078.10, ENST00000685328.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Ala146Val (p.A146V)
( ENST00000256078.10, ENST00000311936.8, ENST00000557334.6, ENST00000685328.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 )
D Predictive Supports Sensitivity/Response Somatic 3 22392911 Detail
colorectal cancer KRAS p.Gly12Cys (p.G12C)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Gly12Cys (p.G12C)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 )
D Predictive Supports Sensitivity/Response Somatic 2 22392911 Detail
colorectal cancer KRAS p.Gly12Asp (p.G12D)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Gly12Asp (p.G12D)
( ENST00000692768.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000693229.1 )
D Predictive Supports Sensitivity/Response Somatic 3 22392911 Detail
lung non-small cell carcinoma NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 ) NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 )
D Predictive Supports Sensitivity/Response Somatic 2 23515407 Detail
lung adenocarcinoma MAP2K1 p.Lys57Asn (p.K57N)
( ENST00000307102.10, ENST00000685172.1, ENST00000685763.1, ENST00000686347.1, ENST00000689951.1, ENST00000691576.1, ENST00000691937.1, ENST00000692683.1, ENST00000693150.1 ) MAP2K1 p.Lys57Asn (p.K57N)
( ENST00000686347.1, ENST00000693150.1, ENST00000307102.10, ENST00000692683.1, ENST00000685763.1, ENST00000685172.1, ENST00000691576.1, ENST00000691937.1, ENST00000689951.1 )
D Predictive Supports Sensitivity/Response Somatic 2 18632602 Detail
lung non-small cell carcinoma KRAS MUTATION KRAS MUTATION A Predictive Supports Resistance Somatic 5 28492898 Detail
uveal melanoma MET OVEREXPRESSION
( ENST00000318493.11 ) MET OVEREXPRESSION
( ENST00000318493.11 )
D Predictive Supports Resistance Somatic 3 25952648 Detail
lung non-small cell carcinoma KRAS p.Gly12Asp (p.G12D)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Gly12Asp (p.G12D)
( ENST00000692768.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000693229.1 )
D Predictive Supports Sensitivity/Response Somatic 4 19029981 Detail
colorectal cancer KRAS MUTATION KRAS MUTATION B Predictive Does Not Support Sensitivity/Response Somatic 3 26666244 Detail
lung non-small cell carcinoma KRAS MUTATION KRAS MUTATION B Predictive Does Not Support Sensitivity/Response Somatic 4 26802155 Detail
cancer HRAS MUTATION HRAS MUTATION D Predictive Supports Sensitivity/Response Somatic 3 26544513 Detail
lung adenocarcinoma RIT1 MUTATION RIT1 MUTATION D Predictive Supports Sensitivity/Response Somatic 3 24469055 Detail
colorectal cancer BRAF V600E AMPLIFICATION
( ENST00000288602.11 ) BRAF V600E AMPLIFICATION
( ENST00000288602.11 )
E Predictive Supports Resistance Somatic 4 21098728 Detail
colorectal cancer KRAS MUTATION KRAS MUTATION D Predictive Supports Sensitivity/Response Somatic 4 25199829 Detail
lung non-small cell carcinoma KRAS MUTATION KRAS MUTATION D Predictive Supports Sensitivity/Response Somatic 2 25199829 Detail
lung non-small cell carcinoma KRAS MUTATION KRAS MUTATION B Predictive Supports Sensitivity/Response Somatic 4 23200175 Detail
Annotation
Description Associated Genes Associated Variants Sensitivity Supported Source Links
Preclinial data from KRAS mutant colorectal cancer... KRAS KRAS MUTATION KRAS MUTATION Sensitivity true CIViC Evidence detail
49 BRAF-mutant melanoma cell lines from patients n... BRAF BRAF p.Val640Glu (p.V640E)
( ENST00000288602.11, ENST00000496384.7, ENST00000644969.2, ENST00000646891.2 ) BRAF p.Val640Glu (p.V640E)
( ENST00000288602.11, ENST00000496384.7, ENST00000644969.2, ENST00000646891.2 )
Sensitivity true CIViC Evidence detail
MEK inhibitor-resistant (selumetinib, PD0325901, G... DDX43 DDX43 OVEREXPRESSION
( ENST00000370336.5 ) DDX43 OVEREXPRESSION
( ENST00000370336.5 )
Resitance or Non-Reponse true CIViC Evidence detail
Patients with relapsed/refractory AML or 60 years ... KIT KIT p.Leu863= (p.L863=)
( ENST00000689994.1, ENST00000687246.1, ENST00000288135.6, ENST00000412167.7, ENST00000686011.1, ENST00000687109.1, ENST00000687295.1, ENST00000689832.1, ENST00000690543.1, ENST00000692783.1 ) KIT p.Leu863= (p.L863=)
( ENST00000412167.7, ENST00000288135.6, ENST00000686011.1, ENST00000687109.1, ENST00000687246.1, ENST00000687295.1, ENST00000689832.1, ENST00000689994.1, ENST00000690543.1, ENST00000692783.1 )
Sensitivity true CIViC Evidence detail
Forty-seven patients with relapsed/refractory AML ... FLT3 FLT3 ITD FLT3 ITD Resitance or Non-Reponse true CIViC Evidence detail
Preclinical study in melanoma cell lines. TBK1 dep... TBK1 TBK1 OVEREXPRESSION
( ENST00000331710.10 ) TBK1 OVEREXPRESSION
( ENST00000331710.10 )
Sensitivity true CIViC Evidence detail
83 patients from a phase II trial (docetaxel + pla... KRAS KRAS p.Gly12Cys (p.G12C)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Gly12Cys (p.G12C)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 )
Sensitivity true CIViC Evidence detail
83 patients from a phase II trial (docetaxel + pla... KRAS KRAS p.Gly12Val (p.G12V)
( ENST00000688940.1, ENST00000692768.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000693229.1 ) KRAS p.Gly12Val (p.G12V)
( ENST00000693229.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1 )
Sensitivity true CIViC Evidence detail
A clinical trial comparing selumetinib and docetax... STK11 STK11 LOSS
( ENST00000326873.12 ) STK11 LOSS
( ENST00000326873.12 )
Resitance or Non-Reponse true CIViC Evidence detail
A clinical trial comparing selumetinib and docetax... TP53 TP53 DELETERIOUS MUTATION TP53 DELETERIOUS MUTATION Sensitivity true CIViC Evidence detail
Preclinical study in KRAS mutant lung and colon ca... ERBB3 ERBB3 OVEREXPRESSION
( ENST00000267101.8 ) ERBB3 OVEREXPRESSION
( ENST00000267101.8 )
Sensitivity true CIViC Evidence detail
Preclinical study in KRAS mutant lung and colon ca... ERBB3 ERBB3 OVEREXPRESSION
( ENST00000267101.8 ) ERBB3 OVEREXPRESSION
( ENST00000267101.8 )
Resitance or Non-Reponse true CIViC Evidence detail
A375 cells expressing MAP2K1 P124S mutation confer... MAP2K1 MAP2K1 p.Pro124Ser (p.P124S)
( ENST00000685172.1, ENST00000692683.1, ENST00000685763.1, ENST00000307102.10, ENST00000693150.1, ENST00000689951.1, ENST00000691937.1, ENST00000686347.1, ENST00000691576.1 ) MAP2K1 p.Pro124Ser (p.P124S)
( ENST00000307102.10, ENST00000685172.1, ENST00000685763.1, ENST00000686347.1, ENST00000689951.1, ENST00000691576.1, ENST00000691937.1, ENST00000692683.1, ENST00000693150.1 )
Resitance or Non-Reponse true CIViC Evidence detail
101 patients with metastatic uveal melanoma were r... GNA11 GNA11 Q209 GNA11 Q209 Sensitivity false CIViC Evidence detail
101 patients with metastatic uveal melanoma were r... GNAQ GNAQ Q209 GNAQ Q209 Sensitivity false CIViC Evidence detail
A375 cells expressing MAP2K1 Q56P mutation conferr... MAP2K1 MAP2K1 p.Gln56Pro (p.Q56P)
( ENST00000307102.10, ENST00000689951.1, ENST00000691937.1, ENST00000686347.1, ENST00000691576.1, ENST00000685172.1, ENST00000685763.1, ENST00000692683.1, ENST00000693150.1 ) MAP2K1 p.Gln56Pro (p.Q56P)
( ENST00000307102.10, ENST00000685172.1, ENST00000685763.1, ENST00000686347.1, ENST00000689951.1, ENST00000691576.1, ENST00000691937.1, ENST00000692683.1, ENST00000693150.1 )
Resitance or Non-Reponse true CIViC Evidence detail
31 patients with KRAS exon 2 mutation (codons 12 a... KRAS KRAS EXON 2 MUTATION KRAS EXON 2 MUTATION Sensitivity true CIViC Evidence detail
Phase 1 trial in 57 patients with advanced cancers... NRAS NRAS Q61 NRAS Q61 Sensitivity true CIViC Evidence detail
Preclinical study in melanoma cell lines. NRAS Q61... NRAS NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 ) NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 )
Sensitivity true CIViC Evidence detail
Case report of a 51-year old patient with recurren... MAP2K1 MAP2K1 p.Gln56_Val60del (p.Q56_V60del)
( ENST00000307102.10, ENST00000685172.1, ENST00000685763.1, ENST00000686347.1, ENST00000689951.1, ENST00000691576.1, ENST00000691937.1, ENST00000692683.1, ENST00000693150.1 ) MAP2K1 p.Gln56_Val60del (p.Q56_V60del)
( ENST00000685172.1, ENST00000692683.1, ENST00000685763.1, ENST00000693150.1, ENST00000307102.10, ENST00000689951.1, ENST00000691937.1, ENST00000686347.1, ENST00000691576.1 )
Sensitivity true CIViC Evidence detail
NF2 loss promotes oncogenic RAS-signaling via YAP-... NF2 NF2 LOSS
( ENST00000338641.10 ) NF2 LOSS
( ENST00000338641.10 )
Sensitivity true CIViC Evidence detail
Treatment with selumetinib (NCT01362803) resulted ... NF1 NF1 MUTATION NF1 MUTATION Sensitivity true CIViC Evidence detail
In 28 out of 40 (70%) metastatic colorectal cancer... KRAS KRAS p.Gly12Val (p.G12V)
( ENST00000688940.1, ENST00000692768.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000693229.1 ) KRAS p.Gly12Val (p.G12V)
( ENST00000693229.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1 )
Sensitivity true CIViC Evidence detail
In 28 out of 40 (70%) metastatic colorectal cancer... KRAS KRAS p.Gly13Asp (p.G13D)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000685328.1, ENST00000557334.6, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Gly13Asp (p.G13D)
( ENST00000556131.2, ENST00000557334.6, ENST00000256078.10, ENST00000311936.8, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 )
Sensitivity true CIViC Evidence detail
In 28 out of 40 (70%) metastatic colorectal cancer... NRAS NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 ) NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 )
Sensitivity true CIViC Evidence detail
In 28 out of 40 (70%) metastatic colorectal cancer... KRAS KRAS p.Ala146Thr (p.A146T)
( ENST00000256078.10, ENST00000311936.8, ENST00000557334.6, ENST00000685328.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Ala146Thr (p.A146T)
( ENST00000256078.10, ENST00000311936.8, ENST00000557334.6, ENST00000685328.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 )
Sensitivity true CIViC Evidence detail
In 28 out of 40 (70%) metastatic colorectal cancer... KRAS KRAS p.Ala146Val (p.A146V)
( ENST00000311936.8, ENST00000557334.6, ENST00000256078.10, ENST00000685328.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Ala146Val (p.A146V)
( ENST00000256078.10, ENST00000311936.8, ENST00000557334.6, ENST00000685328.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 )
Sensitivity true CIViC Evidence detail
In 28 out of 40 (70%) metastatic colorectal cancer... KRAS KRAS p.Gly12Cys (p.G12C)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Gly12Cys (p.G12C)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 )
Sensitivity true CIViC Evidence detail
In 28 out of 40 (70%) metastatic colorectal cancer... KRAS KRAS p.Gly12Asp (p.G12D)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Gly12Asp (p.G12D)
( ENST00000692768.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000693229.1 )
Sensitivity true CIViC Evidence detail
Of the 4,562 patients with lung cancers, 30 showed... NRAS NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 ) NRAS p.Gln61Lys (p.Q61K)
( ENST00000369535.5 )
Sensitivity true CIViC Evidence detail
Mutational profiling of a large cohort of lung ade... MAP2K1 MAP2K1 p.Lys57Asn (p.K57N)
( ENST00000307102.10, ENST00000685172.1, ENST00000685763.1, ENST00000686347.1, ENST00000689951.1, ENST00000691576.1, ENST00000691937.1, ENST00000692683.1, ENST00000693150.1 ) MAP2K1 p.Lys57Asn (p.K57N)
( ENST00000686347.1, ENST00000693150.1, ENST00000307102.10, ENST00000692683.1, ENST00000685763.1, ENST00000685172.1, ENST00000691576.1, ENST00000691937.1, ENST00000689951.1 )
Sensitivity true CIViC Evidence detail
A phase 3 study of selumetinib and docetaxel in KR... KRAS KRAS MUTATION KRAS MUTATION Resitance or Non-Reponse true CIViC Evidence detail
In this study the authors screened for growth fact... MET MET OVEREXPRESSION
( ENST00000318493.11 ) MET OVEREXPRESSION
( ENST00000318493.11 )
Resitance or Non-Reponse true CIViC Evidence detail
The use of NVP-BEZ235 in conjunction with ARRY-142... KRAS KRAS p.Gly12Asp (p.G12D)
( ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000692768.1, ENST00000693229.1 ) KRAS p.Gly12Asp (p.G12D)
( ENST00000692768.1, ENST00000256078.10, ENST00000311936.8, ENST00000556131.2, ENST00000557334.6, ENST00000685328.1, ENST00000686969.1, ENST00000688940.1, ENST00000693229.1 )
Sensitivity true CIViC Evidence detail
A phase I study to determine the tolerability and... KRAS KRAS MUTATION KRAS MUTATION Sensitivity false CIViC Evidence detail
38 KRAS wild-type patients were randomized to erlo... KRAS KRAS MUTATION KRAS MUTATION Sensitivity false CIViC Evidence detail
A pre-clinical study in 10 solid cancer cell lines... HRAS HRAS MUTATION HRAS MUTATION Sensitivity true CIViC Evidence detail
RIT1 mutations were identified in approx. 2% of lu... RIT1 RIT1 MUTATION RIT1 MUTATION Sensitivity true CIViC Evidence detail
COLO201 and COLO206F cells harboring BRAF V600E mu... BRAF BRAF V600E AMPLIFICATION
( ENST00000288602.11 ) BRAF V600E AMPLIFICATION
( ENST00000288602.11 )
Resitance or Non-Reponse true CIViC Evidence detail
SiRNA Screening in 37 KRAS Mutant colorectal cance... KRAS KRAS MUTATION KRAS MUTATION Sensitivity true CIViC Evidence detail
SiRNA Screening in 37 KRAS Mutant colorectal cance... KRAS KRAS MUTATION KRAS MUTATION Sensitivity true CIViC Evidence detail
87 patients with KRAS mutant stage IIB-IV NSCLC af... KRAS KRAS MUTATION KRAS MUTATION Sensitivity true CIViC Evidence detail
NCT ID Status Phase Summary Start date Completion date
NCT03162627 Active, not recruiting Phase 1 Selumetinib and Olaparib in Solid Tumors August 4, 2017 August 30, 2026
NCT04590235 Active, not recruiting Phase 1 A Study of Selumetinib in Chinese Paediatric and Adult Subjects With Neurofibromatosis Type 1 (NF1) and Inoperable Plexiform Neurofibromas (PN) December 16, 2020 August 31, 2026
NCT01089101 Active, not recruiting Phase 1/Phase 2 Selumetinib in Treating Young Patients With Recurrent or Refractory Low Grade Glioma April 19, 2010 December 1, 2025
NCT03944772 Active, not recruiting Phase 2 Phase 2 Platform Study in Patients With Advanced Non-Small Lung Cancer Who Progressed on First-Line Osimertinib Therapy (ORCHARD) June 25, 2019 May 6, 2025
NCT05101148 Active, not recruiting Phase 1 Phase I Study to Assess the Effect of Food on the PK and Gastrointestinal Tolerability of Selumetinib in Adolescent Children With Neurofibromatosis Type 1 Related Plexiform Neurofibromas July 21, 2021 January 12, 2026
NCT04924608 Active, not recruiting Phase 3 Efficacy and Safety of Selumetinib in Adults With NF1 Who Have Symptomatic, Inoperable Plexiform Neurofibromas November 19, 2021 March 17, 2025
NCT03581487 Active, not recruiting Phase 1/Phase 2 Durvalumab, Tremelimumab, and Selumetinib in Treating Participants With Recurrent or Stage IV Non-small Cell Lung Cancer April 1, 2019 December 31, 2025
NCT02151084 Active, not recruiting Phase 2 A Study of Different Dosing Schedules of Selumetinib With Cisplatin/Gemcitabine (CIS/GEM) Versus CIS/GEM Alone in Biliary Cancer November 2014 December 2025
NCT02188264 Active, not recruiting Phase 1 Selumetinib and Cyclosporine in Treating Patients With Advanced Solid Tumors or Advanced or Metastatic Colorectal Cancer August 5, 2014 March 19, 2025
NCT02299999 Active, not recruiting Phase 2 SAFIR02_Breast - Efficacy of Genome Analysis as a Therapeutic Decision Tool for Patients With Metastatic Breast Cancer April 7, 2014 December 2024
NCT03392246 Active, not recruiting Phase 2 A Phase 2 Study of Osimertinib in Combination With Selumetinib in EGFR Inhibitor naïve Advanced EGFR Mutant Lung Cancer January 31, 2018 June 30, 2026
NCT02393690 Active, not recruiting Phase 2 Iodine I-131 With or Without Selumetinib in Treating Patients With Recurrent or Metastatic Thyroid Cancer May 4, 2015 December 31, 2023
NCT02407405 Active, not recruiting Phase 2 MEK 1/2 Inhibitor Selumetinib (AZD6244 Hydrogen Sulfate) in Adults With Neurofibromatosis Type 1 (NF1) and Inoperable Plexiform Neurofibromas January 7, 2016 January 1, 2025
NCT03213691 Active, not recruiting Phase 2 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) October 30, 2017 September 22, 2024
NCT01933932 Active, not recruiting Phase 3 Assess Efficacy & Safety of Selumetinib in Combination With Docetaxel in Patients Receiving 2nd Line Treatment for v-Ki-ras2 Kirsten Rat Sarcoma Viral Oncogene Homolog (KRAS) Positive NSCLC September 25, 2013 December 31, 2024
NCT02546661 Active, not recruiting Phase 1 Open-Label, Randomised, Multi-Drug, Biomarker-Directed, Phase 1b Study in Pts w/ Muscle Invasive Bladder Cancer October 3, 2016 June 28, 2024
NCT01364051 Active, not recruiting Phase 1 Cediranib Maleate and Selumetinib Sulfate in Treating Patients With Solid Malignancies May 25, 2011 March 7, 2025
NCT02664935 Active, not recruiting Phase 2 National Lung Matrix Trial: Multi-drug Phase II Trial in Non-Small Cell Lung Cancer May 2015 September 2024
NCT03259633 Approved for marketing An Intermediate Access Protocol for Selumetinib for Treatment of Neurofibromatosis Type 1
NCT01960374 Completed Phase 1 Dose-escalation Study to Assess Selumetinib Safety, Tolerability and PK October 2013 May 2014
NCT02025114 Completed Phase 1/Phase 2 Selumetinib in Combination With Gefitinib in NSCLC Patients September 2014 March 8, 2018
NCT02046850 Completed Phase 1 To Assess the Effect of Rifampicin on the Pharmacokinetics of Selumetinib in Healthy Male Volunteers February 2014 April 2014
NCT02056392 Completed Phase 1 To Assess the Effects of Single Oral Dose of Selumetinib [AZD6244; ARRY-142886] [Hyd-Sulfate]), on QTc Interval in Healthy Male Volunteers March 2014 August 2014
NCT02063204 Completed Phase 1 To Assess the Pharmacokinetics, Safety and Tolerability of Selumetinib in Renal Impaired Subjects and Healthy Subjects March 2014 July 2014
NCT02093728 Completed Phase 1 To Assess the Effect of Itraconazole and Fluconazole on the Pharmacokinetics of Selumetinib in Healthy Male Volunteers April 2014 June 2014
NCT02117167 Completed Phase 2 SAFIR02_Lung - Efficacy of Targeted Drugs Guided by Genomic Profiles in Metastatic NSCLC Patients April 23, 2014 December 2023
NCT02337530 Completed Phase 2 Selumetinib in Patients Receiving Pemetrexed and Platinum-based Chemotherapy in Advanced or Metastatic KRAS Wildtype or Unknown Non-Squamous NSCLC May 26, 2015 June 18, 2019
NCT02503358 Completed Phase 1 Selumetinib and Paclitaxel as Second-Line Treatment in Treating Patients With Stage IIIB-IV Non-small Cell Lung Cancer July 21, 2016 July 16, 2020
NCT02586987 Completed Phase 1 A Study to Assess the Safety, Tolerability and Anti-tumour Activity of Ascending Doses of Selumetinib in Combination With MEDI4736 and Selumetinib in Combination With MEDI4736 and Tremelimumab in Patients With Advanced Solid Tumours December 28, 2015 September 20, 2019
NCT01222689 Completed Phase 2 Selumetinib and Erlotinib Hydrochloride in Treating Patients With Locally Advanced or Metastatic Pancreatic Cancer November 2010 September 2014
NCT00553332 Completed Phase 2 Selumetinib in Treating Patients With Biliary Cancer That Cannot Be Removed By Surgery November 2007 January 2013
NCT00559949 Completed Phase 2 Selumetinib in Treating Patients With Papillary Thyroid Cancer That Did Not Respond to Radioactive Iodine December 2007 August 2016
NCT00588809 Completed Phase 2 Selumetinib in Treating Patients With Recurrent or Refractory Acute Myeloid Leukemia December 2007 December 2012
NCT00604721 Completed Phase 2 Selumetinib in Treating Patients With Locally Advanced or Metastatic Liver Cancer November 2007 June 2012
NCT00866177 Completed Phase 2 MEK Inhibitor AZD6244 in Treating Patients With Stage III or Stage IV Melanoma March 2009 September 2013
NCT00888134 Completed Phase 2 Selumetinib in Cancers With BRAF Mutations July 2009 January 2015
NCT01011933 Completed Phase 2 Selumetinib in Treating Patients With Recurrent or Persistent Endometrial Cancer September 2009 January 2016
NCT01061749 Completed Phase 1 Selumetinib and Cixutumumab in Treating Patients With Advanced Solid Malignancies November 2009 September 2014
NCT01085214 Completed Phase 2 AZD6244 (Selumetinib) in Treating Patients With Multiple Myeloma March 2010 March 2012
NCT01143402 Completed Phase 2 Temozolomide or Selumetinib in Treating Patients With Metastatic Melanoma of the Eye June 2010 May 2016
NCT01160718 Completed Phase 2 Fulvestrant With or Without AZD6244 in Treating Patients With Advanced Breast Cancer That Progressed After Aromatase Inhibitor Therapy August 2010 September 2016
NCT01206140 Completed Phase 2 Selumetinib With or Without Temsirolimus in Treating Patients With Metastatic, Recurrent, or Locally Advanced Soft Tissue Sarcoma That Cannot Be Removed By Surgery October 2010 April 2015
NCT01217450 Completed Phase 1 Selumetinib and Cetuximab in Treating Patients With Refractory Solid Tumors October 2012 May 2014
NCT00551070 Completed Phase 2 Selumetinib Sulfate in Treating Woman With Recurrent Low-Grade Ovarian Cancer or Peritoneum Cancer December 17, 2007 November 13, 2020
NCT01242605 Completed Phase 1 ABC-04 a Study of Cisplatin, Gemcitabine and Selumetinib in Patients With Advanced Biliary Tract Cancer February 2012 May 2016
NCT01658943 Completed Phase 2 Selumetinib and Akt Inhibitor MK2206 or mFOLFOX Therapy Comprising Oxaliplatin and Fluorouracil in Treating Patients With Metastatic Pancreatic Cancer Previously Treated With Chemotherapy August 2012 June 2015
NCT01783197 Completed Phase 1 Study of Selumetinib in Patients With Previously Treated or Untreated Advanced/Metastatic NSCLC June 4, 2013 April 2, 2019
NCT01809210 Completed Phase 1 Assess Safety & Efficacy of Selumetinib When Given in Combination With Standard First Line Treatment for Advanced Non-small Cell Lung Cancer April 4, 2013 January 4, 2016
NCT03326388 Completed Phase 1/Phase 2 Intermittent Dosing Of Selumetinib In Childhood NF1 Associated Tumours September 26, 2019 February 14, 2024
NCT03433183 Completed Phase 2 SARC031: MEK Inhibitor Selumetinib (AZD6244) in Combination With the mTOR Inhibitor Sirolimus for Patients With Malignant Peripheral Nerve Sheath Tumors October 2, 2019 October 1, 2023
NCT03745989 Completed Phase 1 Study of MK-8353 + Selumetinib in Advanced/Metastatic Solid Tumors (MK-8353-014) February 22, 2019 March 19, 2021
NCT03833427 Completed Phase 1 Study of Selumetinib (MK-5618) in Combination With Pembrolizumab (MK-3475) in Participants With Advanced/Metastatic Solid Tumors (MK-5618-001) March 18, 2019 June 28, 2022
NCT04495127 Completed Phase 1 Selumetinib Paediatric NF1 Japan Study August 31, 2020 March 24, 2023
NCT06188741 Not yet recruiting Phase 2 Selumetinib for the Prevention of Plexiform Neurofibroma Growth in NF Type 1 August 1, 2024 August 1, 2031
NCT05253131 Not yet recruiting Phase 2 Trial of Selumetinib and Bromodomain Inhibitor With Durvalumab for Sarcomas December 15, 2024 December 15, 2030
NCT03801369 Recruiting Phase 2 Olaparib in Combination With Either Durvalumab, Selumetinib, or Capivasertib or Ceralasertib Alone in Treating Patients With Metastatic Triple Negative Breast Cancer December 12, 2018 December 31, 2027
NCT02813135 Recruiting Phase 1/Phase 2 European Proof-of-Concept Therapeutic Stratification Trial of Molecular Anomalies in Relapsed or Refractory Tumors August 3, 2016 August 2027
NCT03326310 Recruiting Phase 1 Selumetinib and Azacitidine in High Risk Chronic Blood Cancers September 4, 2018 September 4, 2025
NCT03095248 Suspended Phase 2 Trial of Selumetinib in Patients With Neurofibromatosis Type II Related Tumors May 8, 2017 June 2025
NCT01519427 Terminated Phase 2 Selumetinib and Akt Inhibitor MK2206 in Treating Patients With Stage III or Stage IV Melanoma Who Failed Prior Therapy With Vemurafenib or Dabrafenib January 2012 May 2013
NCT01949870 Terminated Phase 1 Selumetinib (AZD6244, ARRY-142886) J-BTC Phase 1 Study October 2013 August 2014
NCT01278615 Terminated Phase 2 Selumetinib in Treating Patients With Relapsed or Refractory Diffuse Large B-cell Lymphoma December 2010 May 2014
NCT01166126 Terminated Phase 2 Temsirolimus/AZD 6244 for Treatment-naive With BRAF Mutant Unresectable Stage IV October 2010 June 2012
NCT01843062 Terminated Phase 3 Comparing Complete Remission After Treatment With Selumetinib/Placebo in Patient With Differentiated Thyroid Cancer August 27, 2013 March 6, 2019
NCT03705507 Terminated Phase 1/Phase 2 International Trial of Selumetinib in Combination With Dexamethasone for the Treatment of Acute Lymphoblastic Leukaemia May 18, 2018 May 3, 2023
NCT01752569 Terminated Phase 1/Phase 2 A Study of Selumetinib in Patients With Kaposi's Sarcoma June 15, 2012 December 20, 2017
NCT02450656 Unknown status Phase 1/Phase 2 Afatinib and Selumetinib in Advanced KRAS Mutant and PIK3CA Wildtype Non-small Cell Lung Cancer June 2015 December 2019
NCT03004105 Withdrawn Phase 2 MEDI4736 With Selumetinib for KRAS Mutant Non-Small Cell Lung Cancer (NSCLC) May 2018 May 2024
NCT05825365 Withdrawn Phase 2 Selumetinib in Chinese Paediatric With Post-operative NF1-PNs, PhaseⅡ, Double-Blinded, Placebo-Controlled Study August 31, 2023 June 30, 2026
NCT01859182 Withdrawn Phase 2 Selumetinib and Akt Inhibitor MK-2206 in Treating Patients With Refractory or Advanced Gallbladder or Bile Duct Cancer That Cannot Be Removed By Surgery January 2013 May 2013