Selumetinib for the treatment of metastatic uveal melanoma: past and future perspectives

scientific article published on 5 April 2016

Selumetinib for the treatment of metastatic uveal melanoma: past and future perspectives is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.2217/FON-2015-0075
P698PubMed publication ID27044592

P2093author name stringRichard D Carvajal
Daniel K Manson
Kimberly M Komatsubara
P2860cites workDisruption of CRAF-mediated MEK activation is required for effective MEK inhibition in KRAS mutant tumorsQ24294914
Mutant Gq/11 promote uveal melanoma tumorigenesis by activating YAPQ24298571
Relief of Profound Feedback Inhibition of Mitogenic Signaling by RAF Inhibitors Attenuates Their Activity in BRAFV600E MelanomasQ24303940
Mutations in GNA11 in uveal melanomaQ24625723
Frequent somatic mutations of GNAQ in uveal melanoma and blue naeviQ24646052
Oncogenic mutations in GNAQ occur early in uveal melanomaQ24658558
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Novel Carboxamide-Based Allosteric MEK Inhibitors: Discovery and Optimization Efforts toward XL518 (GDC-0973)Q27684146
Mechanism of MEK inhibition determines efficacy in mutant KRAS- versus BRAF-driven cancersQ27685364
Phase I pharmacokinetic and pharmacodynamic study of the oral, small-molecule mitogen-activated protein kinase kinase 1/2 inhibitor AZD6244 (ARRY-142886) in patients with advanced cancersQ27851426
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Overexpression of DDX43 mediates MEK inhibitor resistance through RAS Upregulation in uveal melanoma cellsQ27853016
Effect of selumetinib vs chemotherapy on progression-free survival in uveal melanoma: a randomized clinical trialQ27853021
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Improved overall survival in melanoma with combined dabrafenib and trametinibQ27853091
Mutations of the BRAF gene in human cancerQ27860760
Modelling vemurafenib resistance in melanoma reveals a strategy to forestall drug resistanceQ28282963
Blockade of the MAP kinase pathway suppresses growth of colon tumors in vivoQ28368373
Phase II DeCOG-study of ipilimumab in pretreated and treatment-naïve patients with metastatic uveal melanomaQ28543960
Improved survival with MEK inhibition in BRAF-mutated melanomaQ29620663
Study design and rationale for a randomised, placebo-controlled, double-blind study to assess the efficacy of selumetinib (AZD6244; ARRY-142886) in combination with dacarbazine in patients with metastatic uveal melanoma (SUMIT).Q30384829
The National Cancer Data Base report on cutaneous and noncutaneous melanoma: a summary of 84,836 cases from the past decade. The American College of Surgeons Commission on Cancer and the American Cancer SocietyQ31995716
Hippo-independent activation of YAP by the GNAQ uveal melanoma oncogene through a trio-regulated rho GTPase signaling circuitry.Q33819083
Enhanced Inhibition of ERK Signaling by a Novel Allosteric MEK Inhibitor, CH5126766, That Suppresses Feedback Reactivation of RAF ActivityQ33971120
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Therapeutic implications of the emerging molecular biology of uveal melanoma.Q34173920
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Phase II, open-label, randomized trial of the MEK1/2 inhibitor selumetinib as monotherapy versus temozolomide in patients with advanced melanomaQ34633455
Selumetinib plus dacarbazine versus placebo plus dacarbazine as first-line treatment for BRAF-mutant metastatic melanoma: a phase 2 double-blind randomised studyQ34652628
Genomic Classification of Cutaneous MelanomaQ34670776
Pharmacokinetics and pharmacodynamics of AZD6244 (ARRY-142886) in tumor-bearing nude miceQ35096292
Incidence of uveal melanoma in the United States: 1973-1997.Q35128733
A phase I, open-label, randomized crossover study to assess the effect of dosing of the MEK 1/2 inhibitor Selumetinib (AZD6244; ARRY-142866) in the presence and absence of food in patients with advanced solid tumorsQ35563528
Paracrine Effect of NRG1 and HGF Drives Resistance to MEK Inhibitors in Metastatic Uveal MelanomaQ35812275
The MEK1/2 inhibitor, selumetinib (AZD6244; ARRY-142886), enhances anti-tumour efficacy when combined with conventional chemotherapeutic agents in human tumour xenograft modelsQ35835097
Combined PKC and MEK inhibition in uveal melanoma with GNAQ and GNA11 mutationsQ35915107
Targeting the mitogen-activated protein kinase cascade to treat cancerQ35968411
Improved antitumor activity of immunotherapy with BRAF and MEK inhibitors in BRAF(V600E) melanomaQ36612452
Activation of the MAPK pathway is a common event in uveal melanomas although it rarely occurs through mutation of BRAF or RAS.Q36615986
Galphaq binds two effectors separately in cells: evidence for predetermined signaling pathwaysQ36838853
Mitogenic signaling pathways induced by G protein-coupled receptorsQ36929839
Clinical activity of ipilimumab for metastatic uveal melanoma: a retrospective review of the Dana-Farber Cancer Institute, Massachusetts General Hospital, Memorial Sloan-Kettering Cancer Center, and University Hospital of Lausanne experienceQ37701881
Uveal melanoma: trends in incidence, treatment, and survivalQ37894345
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Treatment of NRAS-mutant melanoma.Q38386344
Multicenter phase II study of the oral MEK inhibitor, CI-1040, in patients with advanced non-small-cell lung, breast, colon, and pancreatic cancerQ38445646
MEK1 and MEK2 inhibitors and cancer therapy: the long and winding roadQ38591835
Inhibition of mutant GNAQ signaling in uveal melanoma induces AMPK-dependent autophagic cell deathQ39188117
Combination Small Molecule MEK and PI3K Inhibition Enhances Uveal Melanoma Cell Death in a Mutant GNAQ- and GNA11-Dependent MannerQ39325158
Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibitionQ39442875
GSK1120212 (JTP-74057) Is an Inhibitor of MEK Activity and Activation with Favorable Pharmacokinetic Properties for Sustained In Vivo Pathway InhibitionQ39606314
MEK1/2 Inhibitors AS703026 and AZD6244 May Be Potential Therapies for KRAS Mutated Colorectal Cancer That Is Resistant to EGFR Monoclonal Antibody TherapyQ39625657
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 preclQ40093939
Biological characterization of ARRY-142886 (AZD6244), a potent, highly selective mitogen-activated protein kinase kinase 1/2 inhibitorQ40164535
Galphaq binds to p110alpha/p85alpha phosphoinositide 3-kinase and displaces Ras.Q40355032
Regulation of Raf-1 by direct feedback phosphorylation.Q40467820
Dabrafenib and trametinib versus dabrafenib and placebo for Val600 BRAF-mutant melanoma: a multicentre, double-blind, phase 3 randomised controlled trialQ40875359
Phase I pharmacokinetic and pharmacodynamic study of the oral MAPK/ERK kinase inhibitor PD-0325901 in patients with advanced cancersQ43136770
The first-in-human study of the hydrogen sulfate (Hyd-sulfate) capsule of the MEK1/2 inhibitor AZD6244 (ARRY-142886): a phase I open-label multicenter trial in patients with advanced cancerQ43152544
Evaluation of the mTOR pathway in ocular (uvea and conjunctiva) melanomaQ43154862
The PI3K/Akt and mTOR/P70S6K signaling pathways in human uveal melanoma cells: interaction with B-Raf/ERK.Q43297233
High frequency of submicroscopic hemizygous deletion is a major mechanism of loss of expression of PTEN in uveal melanomaQ43509621
Absence of mutations of the BRAF gene and constitutive activation of extracellular-regulated kinase in malignant melanomas of the uveaQ43998617
Clinical responses to selumetinib (AZD6244; ARRY-142886)-based combination therapy stratified by gene mutations in patients with metastatic melanomaQ44004637
Phase I and pharmacodynamic study of the oral MEK inhibitor CI-1040 in patients with advanced malignanciesQ46595207
The mitogen-activated protein/extracellular signal-regulated kinase kinase inhibitor AZD6244 (ARRY-142886) induces growth arrest in melanoma cells and tumor regression when combined with docetaxelQ46825496
The RAS-BRAF kinase pathway is not involved in uveal melanomaQ47390207
Very long-term prognosis of patients with malignant uveal melanomaQ47423812
Lack of BRAF mutation in primary uveal melanoma.Q47807462
Activation of Akt/protein kinase B by G protein-coupled receptors. A role for alpha and beta gamma subunits of heterotrimeric G proteins acting through phosphatidylinositol-3-OH kinasegamma.Q47828172
First-in-human, phase I dose-escalation study of the safety, pharmacokinetics, and pharmacodynamics of RO5126766, a first-in-class dual MEK/RAF inhibitor in patients with solid tumors.Q54499836
P433issue11
P407language of work or nameEnglishQ1860
P921main subjectuveal melanomaQ356372
P304page(s)1331-1344
P577publication date2016-04-05
P1433published inFuture OncologyQ2781597
P1476titleSelumetinib for the treatment of metastatic uveal melanoma: past and future perspectives
P478volume12

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cites work (P2860)
Q47223959Frequent and Yet Unreported GNAQ and GNA11 Mutations are Found in Uveal Melanomas.
Q51418687GNA11 Q209L Mouse Model Reveals RasGRP3 as an Essential Signaling Node in Uveal Melanoma
Q64949664Heterogeneity in Mitogen-Activated Protein Kinase (MAPK) Pathway Activation in Uveal Melanoma With Somatic GNAQ and GNA11 Mutations.
Q47655869ICG-001 Exerts Potent Anticancer Activity Against Uveal Melanoma Cells
Q92458965Inhibition of NF-κB-Dependent Signaling Enhances Sensitivity and Overcomes Resistance to BET Inhibition in Uveal Melanoma
Q47708657Kinome-wide transcriptional profiling of uveal melanoma reveals new vulnerabilities to targeted therapeutics.
Q89337067Survival Rates in Patients After Treatment for Metastasis From Uveal Melanoma

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