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SELUMETINIB Drug Record

  • Summary
  • Interactions
  • Claims
  • SELUMETINIB chembl:CHEMBL1614701 Antineoplastic

    Alternate Names:

    ARRY-886
    SELUMETINIB
    ARRY-142886
    AZD-6244
    KOSELUGO
    AZD 6244
    AZD6244
    NSC 741O78
    ARRY 142886
    ARRY142886
    drugbank:11689
    pubchem.compound:10127622
    chembl:CHEMBL1614701
    chemidplus:606143-52-6

    Drug Info:

    Pharmaceutical Developer AstraZenica
    Source Reported Drug Name(s) AZD6244/selumetinib
    Drug Class MEK Inhibitor
    Notes allosteric inhibitor
    Drug Class Kinase Inhibitors
    (11 More Sources)

    Publications:

    Grisham et al., 2015, Extreme Outlier Analysis Identifies Occult Mitogen-Activated Protein Kinase Pathway Mutations in Patients With Low-Grade Serous Ovarian Cancer., J. Clin. Oncol.
    Emery et al., 2009, MEK1 mutations confer resistance to MEK and B-RAF inhibition., Proc. Natl. Acad. Sci. U.S.A.
    Marks et al., 2008, Novel MEK1 mutation identified by mutational analysis of epidermal growth factor receptor signaling pathway genes in lung adenocarcinoma., Cancer Res.
    Crystal et al., 2014, Patient-derived models of acquired resistance can identify effective drug combinations for cancer., Science
    Oddo et al., 2016, Molecular Landscape of Acquired Resistance to Targeted Therapy Combinations in BRAF-Mutant Colorectal Cancer., Cancer Res.
    Nikolaev et al., 2011, Exome sequencing identifies recurrent somatic MAP2K1 and MAP2K2 mutations in melanoma., Nat. Genet.
    Gannon et al., 2016, Identification of an "Exceptional Responder" Cell Line to MEK1 Inhibition: Clinical Implications for MEK-Targeted Therapy., Mol. Cancer Res.
    Choi et al., 2012, Oncogenic MAP2K1 mutations in human epithelial tumors., Carcinogenesis
    Narita et al., 2014, Novel ATP-competitive MEK inhibitor E6201 is effective against vemurafenib-resistant melanoma harboring the MEK1-C121S mutation in a preclinical model., Mol. Cancer Ther.
    Catalanotti F et al., 2013, Phase II trial of MEK inhibitor selumetinib (AZD6244, ARRY-142886) in patients with BRAFV600E/K-mutated melanoma., Clin Cancer Res
    Yeh et al., 2007, Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitor., Clin. Cancer Res.
    Dombi et al., 2016, Activity of Selumetinib in Neurofibromatosis Type 1-Related Plexiform Neurofibromas., N. Engl. J. Med.
    Davies et al., 2007, AZD6244 (ARRY-142886), a potent inhibitor of mitogen-activated protein kinase/extracellular signal-regulated kinase kinase 1/2 kinases: mechanism of action in vivo, pharmacokinetic/pharmacodynamic relationship, and potential for combination in preclinical models., Mol. Cancer Ther.
    Beadnell et al., 2016, The Mitogen-Activated Protein Kinase Pathway Facilitates Resistance to the Src Inhibitor Dasatinib in Thyroid Cancer., Mol. Cancer Ther.
    Kiessling et al., 2015, Mutant HRAS as novel target for MEK and mTOR inhibitors., Oncotarget
    Shi et al., 2014, A novel AKT1 mutant amplifies an adaptive melanoma response to BRAF inhibition., Cancer Discov
    Bonnevaux et al., 2016, Concomitant Inhibition of PI3Kβ and BRAF or MEK in PTEN-Deficient/BRAF-Mutant Melanoma Treatment: Preclinical Assessment of SAR260301 Oral PI3Kβ-Selective Inhibitor., Mol. Cancer Ther.
    Whittaker et al., 2015, Combined Pan-RAF and MEK Inhibition Overcomes Multiple Resistance Mechanisms to Selective RAF Inhibitors., Mol. Cancer Ther.
    Ho et al., 2013, Selumetinib-enhanced radioiodine uptake in advanced thyroid cancer., N. Engl. J. Med.
    McNew et al., 2016, MEK and TAK1 Regulate Apoptosis in Colon Cancer Cells with KRAS-Dependent Activation of Proinflammatory Signaling., Mol. Cancer Res.
    Sweetlove et al., 2015, Inhibitors of pan-PI3K Signaling Synergize with BRAF or MEK Inhibitors to Prevent BRAF-Mutant Melanoma Cell Growth., Front Oncol
    Beloueche-Babari et al., 2013, Acute tumour response to the MEK1/2 inhibitor selumetinib (AZD6244, ARRY-142886) evaluated by non-invasive diffusion-weighted MRI., Br. J. Cancer
    Friedman et al., 2015, Landscape of Targeted Anti-Cancer Drug Synergies in Melanoma Identifies a Novel BRAF-VEGFR/PDGFR Combination Treatment., PLoS ONE
    Olow et al., 2016, BRAF Status in Personalizing Treatment Approaches for Pediatric Gliomas., Clin. Cancer Res.
    Kirkwood et al., 2012, Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanoma., Clin. Cancer Res.
    Peng et al., 2015, Inhibition of RAF Isoforms and Active Dimers by LY3009120 Leads to Anti-tumor Activities in RAS or BRAF Mutant Cancers., Cancer Cell
    Fangusaro J et al., 2019, Selumetinib in paediatric patients with BRAF-aberrant or neurofibromatosis type 1-associated recurrent, refractory, or progressive low-grade glioma: a multicentre, phase 2 trial., Lancet Oncol
    Cheng et al., 2015, Paracrine Effect of NRG1 and HGF Drives Resistance to MEK Inhibitors in Metastatic Uveal Melanoma., Cancer Res.
    Qu et al., 2014, Antitumor activity of selective MEK1/2 inhibitor AZD6244 in combination with PI3K/mTOR inhibitor BEZ235 in gefitinib-resistant NSCLC xenograft models., J. Exp. Clin. Cancer Res.
    de Martino et al., 2014, Impact of ERBB2 mutations on in vitro sensitivity of bladder cancer to lapatinib., Cancer Biol. Ther.
    Kaufman et al., 2017, A Transcriptional Signature Identifies LKB1 Functional Status as a Novel Determinant of MEK Sensitivity in Lung Adenocarcinoma., Cancer Res.
    Chen et al., 2012, A murine lung cancer co-clinical trial identifies genetic modifiers of therapeutic response., Nature
    Eberlein et al., 2015, Acquired Resistance to the Mutant-Selective EGFR Inhibitor AZD9291 Is Associated with Increased Dependence on RAS Signaling in Preclinical Models., Cancer Res.
    Nakanishi et al., 2015, ERK Signal Suppression and Sensitivity to CH5183284/Debio 1347, a Selective FGFR Inhibitor., Mol. Cancer Ther.
    Dhawan et al., 2016, Small molecule stabilization of the KSR inactive state antagonizes oncogenic Ras signalling., Nature
    Takekuma et al., 2016, A long-term surviving patient with recurrent low-grade serous ovarian carcinoma treated with the MEK1/2 inhibitor, selumetinib., Gynecol Oncol Res Pract
    Jänne et al., 2015, Impact of KRAS codon subtypes from a randomised phase II trial of selumetinib plus docetaxel in KRAS mutant advanced non-small-cell lung cancer., Br. J. Cancer
    Papadimitrakopoulou et al., 2016, The BATTLE-2 Study: A Biomarker-Integrated Targeted Therapy Study in Previously Treated Patients With Advanced Non-Small-Cell Lung Cancer., J. Clin. Oncol.
    Qian et al., 2014, Whole genome gene copy number profiling of gastric cancer identifies PAK1 and KRAS gene amplification as therapy targets., Genes Chromosomes Cancer
    Jänne et al., 2013, Selumetinib plus docetaxel for KRAS-mutant advanced non-small-cell lung cancer: a randomised, multicentre, placebo-controlled, phase 2 study., Lancet Oncol.
    Jänne et al., 2017, Selumetinib Plus Docetaxel Compared With Docetaxel Alone and Progression-Free Survival in Patients With KRAS-Mutant Advanced Non-Small Cell Lung Cancer: The SELECT-1 Randomized Clinical Trial., JAMA
    Hayes et al., 2016, Long-Term ERK Inhibition in KRAS-Mutant Pancreatic Cancer Is Associated with MYC Degradation and Senescence-like Growth Suppression., Cancer Cell
    Holt et al., 2012, Enhanced apoptosis and tumor growth suppression elicited by combination of MEK (selumetinib) and mTOR kinase inhibitors (AZD8055)., Cancer Res.
    Engelman et al., 2008, Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers., Nat. Med.
    Hofmann et al., 2012, K-RAS mutant pancreatic tumors show higher sensitivity to MEK than to PI3K inhibition in vivo., PLoS ONE
    García-García et al., 2015, MEK plus PI3K/mTORC1/2 Therapeutic Efficacy Is Impacted by TP53 Mutation in Preclinical Models of Colorectal Cancer., Clin. Cancer Res.
    Depreeuw et al., 2015, Characterization of patient-derived tumor xenograft models of endometrial cancer for preclinical evaluation of targeted therapies., Gynecol. Oncol.
    Riquelme et al., 2016, Modulation of EZH2 Expression by MEK-ERK or PI3K-AKT Signaling in Lung Cancer Is Dictated by Different KRAS Oncogene Mutations., Cancer Res.
    Kim et al., 2016, Phosphoproteomics Reveals MAPK Inhibitors Enhance MET- and EGFR-Driven AKT Signaling in KRAS-Mutant Lung Cancer., Mol. Cancer Res.
    Deming et al., 2016, A phase I study of selumetinib (AZD6244/ARRY-142866), a MEK1/2 inhibitor, in combination with cetuximab in refractory solid tumors and KRAS mutant colorectal cancer., Invest New Drugs
    Hochster et al., 2015, Phase II study of selumetinib (AZD6244, ARRY-142886) plus irinotecan as second-line therapy in patients with K-RAS mutated colorectal cancer., Cancer Chemother. Pharmacol.
    Ebi et al., 2011, Receptor tyrosine kinases exert dominant control over PI3K signaling in human KRAS mutant colorectal cancers., J. Clin. Invest.
    Lamba et al., 2014, RAF suppression synergizes with MEK inhibition in KRAS mutant cancer cells., Cell Rep
    Migliardi et al., 2012, Inhibition of MEK and PI3K/mTOR suppresses tumor growth but does not cause tumor regression in patient-derived xenografts of RAS-mutant colorectal carcinomas., Clin. Cancer Res.
    Weigelt et al., 2011, PIK3CA mutation, but not PTEN loss of function, determines the sensitivity of breast cancer cells to mTOR inhibitory drugs., Oncogene
    Ohashi et al., 2013, Characteristics of lung cancers harboring NRAS mutations., Clin. Cancer Res.
    Ambrosini et al., 2012, Identification of unique MEK-dependent genes in GNAQ mutant uveal melanoma involved in cell growth, tumor cell invasion, and MEK resistance., Clin. Cancer Res.
    Khalili et al., 2012, Combination small molecule MEK and PI3K inhibition enhances uveal melanoma cell death in a mutant GNAQ- and GNA11-dependent manner., Clin. Cancer Res.
    Wu et al., 2012, The protein kinase C inhibitor enzastaurin exhibits antitumor activity against uveal melanoma., PLoS ONE
    Landis et al., 1989, GTPase inhibiting mutations activate the alpha chain of Gs and stimulate adenylyl cyclase in human pituitary tumours., Nature
    Ho et al., 2012, Impact of combined mTOR and MEK inhibition in uveal melanoma is driven by tumor genotype., PLoS ONE
    Wu et al., 2012, Protein kinase C inhibitor AEB071 targets ocular melanoma harboring GNAQ mutations via effects on the PKC/Erk1/2 and PKC/NF-κB pathways., Mol. Cancer Ther.
    Van Raamsdonk et al., 2010, Mutations in GNA11 in uveal melanoma., N. Engl. J. Med.
    Van Raamsdonk et al., 2009, Frequent somatic mutations of GNAQ in uveal melanoma and blue naevi., Nature
    Onken et al., 2008, Oncogenic mutations in GNAQ occur early in uveal melanoma., Invest. Ophthalmol. Vis. Sci.
    Kalinec et al., 1992, Mutated alpha subunit of the Gq protein induces malignant transformation in NIH 3T3 cells., Mol. Cell. Biol.
    MacConaill et al., 2014, Prospective enterprise-level molecular genotyping of a cohort of cancer patients., J Mol Diagn
    Patel et al., 2011, Therapeutic implications of the emerging molecular biology of uveal melanoma., Clin. Cancer Res.
    Chang et al., 2016, Identifying recurrent mutations in cancer reveals widespread lineage diversity and mutational specificity., Nat. Biotechnol.
    Chen et al., 2014, Combined PKC and MEK inhibition in uveal melanoma with GNAQ and GNA11 mutations., Oncogene
    Garcia-Rendueles et al., 2015, NF2 Loss Promotes Oncogenic RAS-Induced Thyroid Cancers via YAP-Dependent Transactivation of RAS Proteins and Sensitizes Them to MEK Inhibition., Cancer Discov
    Ko et al., 2016, A Multicenter, Open-Label Phase II Clinical Trial of Combined MEK plus EGFR Inhibition for Chemotherapy-Refractory Advanced Pancreatic Adenocarcinoma., Clin. Cancer Res.
    Yoon et al., 2009, Combination of EGFR and MEK1/2 inhibitor shows synergistic effects by suppressing EGFR/HER3-dependent AKT activation in human gastric cancer cells., Mol. Cancer Ther.
    Sun et al., 2014, Intrinsic resistance to MEK inhibition in KRAS mutant lung and colon cancer through transcriptional induction of ERBB3., Cell Rep
    Ambrosini et al., 2014, Overexpression of DDX43 mediates MEK inhibitor resistance through RAS Upregulation in uveal melanoma cells., Mol. Cancer Ther.
    Ichihara et al., 2017, SFK/FAK Signaling Attenuates Osimertinib Efficacy in Both Drug-Sensitive and Drug-Resistant Models of EGFR-Mutant Lung Cancer., Cancer Res.
    Challa et al., 2016, IKBKE Is a Substrate of EGFR and a Therapeutic Target in Non-Small Cell Lung Cancer with Activating Mutations of EGFR., Cancer Res.
    Berger et al., 2014, Oncogenic RIT1 mutations in lung adenocarcinoma., Oncogene
    Smida et al., 2016, MEK inhibitors block growth of lung tumours with mutations in ataxia-telangiectasia mutated., Nat Commun
    Johannessen et al., 2013, A melanocyte lineage program confers resistance to MAP kinase pathway inhibition., Nature
    Wang et al., 2017, ATXN1L, CIC, and ETS Transcription Factors Modulate Sensitivity to MAPK Pathway Inhibition., Cell Rep
  • SELUMETINIB   GNA11

    Interaction Score: 2.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Clinical Status early trials
    Pathway activation
    Variant Effect gain-of-function

    PMIDs:
    21444680 26619011 24141786 2549426 22733540 25157968 1328859 22808163 21083380


    Sources:
    DoCM

  • SELUMETINIB   RIT1

    Interaction Score: 1.77

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24469055


    Sources:
    CIViC

  • SELUMETINIB   DDX43

    Interaction Score: 1.77

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24899684


    Sources:
    CIViC

  • SELUMETINIB   GNAQ

    Interaction Score: 1.77

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical - Cell culture
    Response Type sensitive

    PMIDs:
    22550165 22733540 22253748 2549426 22808163 22653968 21083380 19078957 18719078 1328859 25157968


    Sources:
    JAX-CKB DoCM

  • SELUMETINIB   CIC

    Interaction Score: 1.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28178529


    Sources:
    CIViC

  • SELUMETINIB   NF1

    Interaction Score: 0.88

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    28029918 31151904


    Sources:
    ClearityFoundationBiomarkers CIViC

  • SELUMETINIB   MAP2K1

    Interaction Score: 0.81

    Interaction Types & Directionality:
    allosteric modulator
    inhibitor (inhibitory)

    Interaction Info:
    Reported Cancer Type Melanoma
    Indication/Tumor Type melanoma
    Response Type resistant

    PMIDs:
    26324360 19915144 18632602 25394791 27312529 22197931 26582713 22327936 24448821 23444215 17332304 28029918 17699718


    Sources:
    TALC MyCancerGenome ClearityFoundationClinicalTrial JAX-CKB ChemblInteractions COSMIC CIViC CancerCommons MyCancerGenomeClinicalTrial TTD

  • SELUMETINIB   CDH1

    Interaction Score: 0.71

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Erlotinib + Selumetinib
    Indication/Tumor Type pancreatic ductal adenocarcinoma
    Response Type sensitive

    PMIDs:
    26251290


    Sources:
    JAX-CKB

  • SELUMETINIB   NF2

    Interaction Score: 0.71

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    26359368


    Sources:
    CIViC

  • SELUMETINIB   EZH2

    Interaction Score: 0.5

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy DZNep + Selumetinib
    Indication/Tumor Type lung adenocarcinoma
    Response Type sensitive

    PMIDs:
    26676756


    Sources:
    JAX-CKB

  • SELUMETINIB   KRAS

    Interaction Score: 0.41

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    combination therapy Osimertinib + Selumetinib
    Indication/Tumor Type thyroid cancer
    combination therapy Dasatinib + Selumetinib

    PMIDs:
    25870145 27222538 26438159 27312529 27556948 27231576 26351322 26125448 27480147 24935174 23200175 28492898 26725216 27655129 24939055 22271687 19029981 22952903 26272063 26232337 26676756 27422710 26666244 25322874 21985784 25199829 22392911


    Sources:
    ClearityFoundationBiomarkers JAX-CKB CIViC MyCancerGenomeClinicalTrial

  • SELUMETINIB   MAP2K2

    Interaction Score: 0.4

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:
    Notes
    Mechanism of Interaction Dual specificity mitogen-activated protein kinase kinase 2 inhibitor
    Direct Interaction yes

    PMIDs:
    17332304 28029918 17699718


    Sources:
    TALC MyCancerGenome ClearityFoundationClinicalTrial ChemblInteractions MyCancerGenomeClinicalTrial TTD

  • SELUMETINIB   BRAF

    Interaction Score: 0.36

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type melanoma
    Response Type decreased response
    Approval Status Preclinical

    PMIDs:
    24265152 27196754 26351322 23406027 27655129 26137449 22197931 24448821 23942066 26461489 27222538 27312529 19915144 27217440 22048237 26343583 31151904


    Sources:
    ClearityFoundationBiomarkers JAX-CKB CIViC

  • SELUMETINIB   MAP2K5

    Interaction Score: 0.35

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • SELUMETINIB   STK11

    Interaction Score: 0.31

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical - Cell culture
    Response Type sensitive

    PMIDs:
    27821489 22425996


    Sources:
    JAX-CKB CIViC

  • SELUMETINIB   NRAS

    Interaction Score: 0.3

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type resistant
    Approval Status Phase I

    PMIDs:
    23406027 25870145 26343583 22392911 23515407


    Sources:
    JAX-CKB CIViC OncoKB

  • SELUMETINIB   MAP2K4

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • SELUMETINIB   MAP2K7

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • SELUMETINIB   MAP2K6

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • SELUMETINIB   MAP2K3

    Interaction Score: 0.29

    Interaction Types & Directionality:
    inhibitor (inhibitory)

    Interaction Info:

    PMIDs:
    None found


    Sources:
    MyCancerGenomeClinicalTrial

  • SELUMETINIB   HRAS

    Interaction Score: 0.21

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung squamous cell carcinoma
    Response Type sensitive
    Approval Status Preclinical - Cell line xenograft

    PMIDs:
    27222538 26544513


    Sources:
    JAX-CKB CIViC

  • SELUMETINIB   ERBB3

    Interaction Score: 0.18

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24685132 25952648


    Sources:
    CIViC

  • SELUMETINIB   FGFR2

    Interaction Score: 0.1

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type decreased response
    Indication/Tumor Type endometrial carcinoma
    Approval Status Preclinical - Cell culture

    PMIDs:
    26438159 19755509


    Sources:
    JAX-CKB

  • SELUMETINIB   PIK3CA

    Interaction Score: 0.09

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Response Type predicted – sensitive
    Indication/Tumor Type endometrial cancer
    combination therapy Selumetinib + ZSTK474

    PMIDs:
    26232337 26137449 21358673 26272063 24939055 22271687


    Sources:
    JAX-CKB

  • SELUMETINIB   PTEN

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Selumetinib + BEZ235
    Indication/Tumor Type endometrial cancer
    Response Type sensitive

    PMIDs:
    27196754 21358673 26232337


    Sources:
    JAX-CKB

  • SELUMETINIB   MET

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Selumetinib + BEZ235
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    25952648 24939055


    Sources:
    JAX-CKB CIViC

  • SELUMETINIB   MITF

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    24185007


    Sources:
    CIViC

  • SELUMETINIB   ATM

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:

    PMIDs:
    27922010


    Sources:
    CIViC

  • SELUMETINIB   ALK

    Interaction Score: 0.07

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Ceritinib + Selumetinib
    Indication/Tumor Type non-small cell lung carcinoma
    Response Type sensitive

    PMIDs:
    25394791


    Sources:
    JAX-CKB

  • SELUMETINIB   SRC

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Dasatinib + Selumetinib
    Indication/Tumor Type thyroid cancer
    Response Type sensitive

    PMIDs:
    27222538


    Sources:
    JAX-CKB

  • SELUMETINIB   EGFR

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    combination therapy Osimertinib + Selumetinib
    Indication/Tumor Type lung adenocarcinoma
    Approval Status Preclinical

    PMIDs:
    24939055 28416483 25870145 27287717 27312529


    Sources:
    JAX-CKB

  • SELUMETINIB   FGFR3

    Interaction Score: 0.06

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type urinary bladder cancer
    Response Type no benefit
    Approval Status Preclinical

    PMIDs:
    26438159


    Sources:
    JAX-CKB

  • SELUMETINIB   FGFR1

    Interaction Score: 0.04

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type lung squamous cell carcinoma
    Response Type no benefit
    Approval Status Preclinical - Cell culture

    PMIDs:
    26438159


    Sources:
    JAX-CKB

  • SELUMETINIB   ERBB2

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Evidence Type Actionable
    Approval Status Preclinical
    Response Type decreased response

    PMIDs:
    24971884


    Sources:
    JAX-CKB

  • SELUMETINIB   TP53

    Interaction Score: 0.02

    Interaction Types & Directionality:
    n/a

    Interaction Info:
    Indication/Tumor Type colorectal cancer
    Response Type decreased response
    Approval Status Preclinical - Pdx

    PMIDs:
    26343583 26272063 22425996


    Sources:
    JAX-CKB CIViC

  • CancerCommons: AZD6244

    • Version: 25-July-2013

    Alternate Names:
    AZD6244 PubChem Drug Name
    10127622 PubChem Drug ID
    Selumetinib Drug Trade Name

    Drug Info:
    Drug Class MEK Inhibitor
    Source Reported Drug Name(s) AZD6244/selumetinib
    Pharmaceutical Developer AstraZenica

    Publications:

  • MyCancerGenome: SELUMETINIB

    • Version: 20-Jun-2017

    Alternate Names:
    AZD6244 Development Name
    ARRY-142886 Development Name
    SELUMETINIB Generic Name

    Drug Info:
    Drug Class Kinase Inhibitors
    Notes allosteric inhibitor

    Publications:

  • JAX-CKB: Selumetinib

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Kiessling et al., 2015, Mutant HRAS as novel target for MEK and mTOR inhibitors., Oncotarget
    Beadnell et al., 2016, The Mitogen-Activated Protein Kinase Pathway Facilitates Resistance to the Src Inhibitor Dasatinib in Thyroid Cancer., Mol. Cancer Ther.
    García-García et al., 2015, MEK plus PI3K/mTORC1/2 Therapeutic Efficacy Is Impacted by TP53 Mutation in Preclinical Models of Colorectal Cancer., Clin. Cancer Res.

  • DoCM: SELUMETINIB

    • Version: 27-September-2017

    Alternate Names:

    Drug Info:

    Publications:
    Landis et al., 1989, GTPase inhibiting mutations activate the alpha chain of Gs and stimulate adenylyl cyclase in human pituitary tumours., Nature
    Wu et al., 2012, Protein kinase C inhibitor AEB071 targets ocular melanoma harboring GNAQ mutations via effects on the PKC/Erk1/2 and PKC/NF-κB pathways., Mol. Cancer Ther.
    Ho et al., 2012, Impact of combined mTOR and MEK inhibition in uveal melanoma is driven by tumor genotype., PLoS ONE

  • CIViC: SELUMETINIB

    • Version: 14-September-2020

    Alternate Names:

    Drug Info:

    Publications:
    Jänne et al., 2013, Selumetinib plus docetaxel for KRAS-mutant advanced non-small-cell lung cancer: a randomised, multicentre, placebo-controlled, phase 2 study., Lancet Oncol.
    Engelman et al., 2008, Effective use of PI3K and MEK inhibitors to treat mutant Kras G12D and PIK3CA H1047R murine lung cancers., Nat. Med.
    Lamba et al., 2014, RAF suppression synergizes with MEK inhibition in KRAS mutant cancer cells., Cell Rep

  • TALC: SELUMETINIB

    • Version: 12-May-2016

    Alternate Names:
    SELUMETINIB Primary Drug Name
    SELUMETINIB Drug Generic Name
    AZD6244 Drug Synonym

    Drug Info:

    Publications:

  • TTD: AZD6244

    • Version: 2020.06.01

    Alternate Names:
    D0T5DP TTD Drug ID

    Drug Info:

    Publications:

  • ChemblDrugs: chembl:CHEMBL1614701

    • Version: ChEMBL_27

    Alternate Names:

    Drug Info:

    Publications:

  • ChemblInteractions: CHEMBL1614701

    • Version: chembl_23

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: AZD6244

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationBiomarkers: SELUMETINIB

    • Version: 26-July-2013

    Alternate Names:

    Drug Info:

    Publications:

  • MyCancerGenomeClinicalTrial: SELUMETINIB

    • Version: 30-February-2014

    Alternate Names:

    Drug Info:

    Publications:

  • OncoKB: Selumetinib

    • Version: 23-July-2020

    Alternate Names:

    Drug Info:

    Publications:

  • ClearityFoundationClinicalTrial: SELUMETINIB

    • Version: 15-June-2013

    Alternate Names:

    Drug Info:

    Publications:

  • COSMIC: Selumetinib

    • Version: 4-Sep-2020

    Alternate Names:

    Drug Info:

    Publications:

Disclaimer: This resource is intended for purely research purposes. It should not be used for emergencies or medical or professional advice.

A finding of a drug-gene interaction or potentially druggable category does not necessarily indicate effectiveness (or lack thereof) of any drug or treatment regimen. A finding of no interaction or no potentially druggable category does not necessarily indicate lack of effectiveness of any drug or treatment regimen. Drug-gene interactions or potentially druggable categories are not presented in ranked order of potential or predicted efficacy.

The dgidb.org website does not provide any medical or healthcare products, services or advice, and is not for medical emergencies or urgent situations. IF YOU THINK YOU MAY HAVE A MEDICAL EMERGENCY, CALL YOUR DOCTOR OR 911 IMMEDIATELY. Information contained on this website is not a substitute for a doctor's medical judgment or advice. We recommend that you discuss your specific, individual health concerns with your doctor or health care professional.

DGIdb (v4.2.0 - sha1 afd9f30b) • Last updated 2020-10-21