Bridging the Gap between Preclinical and Clinical Studies Using Pharmacokinetic–Pharmacodynamic Modeling: An Analysis of GDC-0973, a MEK Inhibitor

scientific article published on April 10, 2012

Bridging the Gap between Preclinical and Clinical Studies Using Pharmacokinetic–Pharmacodynamic Modeling: An Analysis of GDC-0973, a MEK Inhibitor is …
instance of (P31):
scholarly articleQ13442814

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P356DOI10.1158/1078-0432.CCR-12-0445
P953full work available at URLhttps://aacrjournals.org/clincancerres/article-pdf/18/11/3090/2003372/3090.pdf
https://aacr.figshare.com/articles/journal_contribution/Supplementary_Figure_1_from_Bridging_the_Gap_between_Preclinical_and_Clinical_Studies_Using_Pharmacokinetic_Pharmacodynamic_Modeling_An_Analysis_of_GDC-0973_a_MEK_Inhibitor/22445549/1/files/39896591.pdf
P698PubMed publication ID22496205

P50authorBlake T AftabQ99363861
P2093author name stringJohn Prescott
Lillian Lee
Harvey Wong
Jean-Francois Martini
Peiwen Yu
Ron Aoyama
Marcia Belvin
Laurent Vernillet
Amy Peterson
Congfen Li
Yongchang Shi
Geoffrey Del Rosario
Klaus P. Hoeflich
Sanh Tan Lam
Edna F. Choo
Joseph A. Ware
P2860cites workClinical efficacy of a RAF inhibitor needs broad target blockade in BRAF-mutant melanomaQ24597152
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Roles of the Raf/MEK/ERK pathway in cell growth, malignant transformation and drug resistanceQ24645668
MEK1 mutations confer resistance to MEK and B-RAF inhibitionQ27777362
BRAF gene amplification can promote acquired resistance to MEK inhibitors in cancer cells harboring the BRAF V600E mutationQ27851610
Inhibition of Mutated, Activated BRAF in Metastatic MelanomaQ27860458
Mutations of the BRAF gene in human cancerQ27860760
Mechanism of activation of the RAF-ERK signaling pathway by oncogenic mutations of B-RAFQ28251989
BRAF mutation predicts sensitivity to MEK inhibitionQ29614281
Advances in targeting the Ras/Raf/MEK/Erk mitogen-activated protein kinase cascade with MEK inhibitors for cancer therapyQ33316645
Identifying optimal biologic doses of everolimus (RAD001) in patients with cancer based on the modeling of preclinical and clinical pharmacokinetic and pharmacodynamic dataQ33323274
Recovery of phospho-ERK activity allows melanoma cells to escape from BRAF inhibitor therapy.Q33906093
Raf proteins and cancer: B-Raf is identified as a mutational targetQ34648534
Diversity of mechanism-based pharmacodynamic modelsQ35107049
Drug delivery and transport to solid tumorsQ35563687
Of mice and men: values and liabilities of the athymic nude mouse model in anticancer drug developmentQ35761426
Targeting the mitogen-activated protein kinase cascade to treat cancerQ35968411
Tumor models for efficacy determinationQ36623519
B-Raf kinase inhibitors for cancer treatmentQ36875829
Novel mitogen-activated protein kinase kinase inhibitorsQ37828536
Resistance to MEK Inhibitors: Should We Co-Target Upstream?Q37859182
Potential Therapeutic Strategies to Overcome Acquired Resistance to BRAF or MEK Inhibitors in BRAF Mutant CancersQ37866945
Intermittent administration of MEK inhibitor GDC-0973 plus PI3K inhibitor GDC-0941 triggers robust apoptosis and tumor growth inhibitionQ39442875
Pharmacodynamics of 2-[4-[(1E)-1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl]-3-(pyridine-4-yl)-1H-pyrazol-1-yl]ethan-1-ol (GDC-0879), a potent and selective B-Raf kinase inhibitor: understanding relationships between systemic concentrations, phosphoryQ39894543
Antiarthritis Effect of a Novel Bruton's Tyrosine Kinase (BTK) Inhibitor in Rat Collagen-Induced Arthritis and Mechanism-Based Pharmacokinetic/Pharmacodynamic Modeling: Relationships between Inhibition of BTK Phosphorylation and EfficacyQ42741853
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
Pharmacokinetic–Pharmacodynamic Analysis of Vismodegib in Preclinical Models of Mutational and Ligand-Dependent Hedgehog Pathway ActivationQ44485080
Phase I and pharmacodynamic study of the oral MEK inhibitor CI-1040 in patients with advanced malignanciesQ46595207
Pharmacokinetic-pharmacodynamic modeling of biomarker response and tumor growth inhibition to an orally available cMet kinase inhibitor in human tumor xenograft mouse modelsQ46670098
P433issue11
P407language of work or nameEnglishQ1860
P921main subjectpharmacokineticsQ323936
pharmacodynamicsQ725307
P304page(s)3090-3099
P577publication date2012-04-10
P1433published inClinical Cancer ResearchQ332253
P1476titleBridging the gap between preclinical and clinical studies using pharmacokinetic-pharmacodynamic modeling: an analysis of GDC-0973, a MEK inhibitor
Bridging the Gap between Preclinical and Clinical Studies Using Pharmacokinetic–Pharmacodynamic Modeling: An Analysis of GDC-0973, a MEK Inhibitor
P478volume18

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