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Targeting the PI3K/Akt/mTOR pathway with the pan-Akt inhibitor GDC-0068 in PIK3CA-mutant breast cancer brain metastases

Neuro-oncology (Charlottesville, Va.), 2019-11, Vol.21 (11), p.1401-1411

2019

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Preclinical characterization of the absorption and disposition of the brain penetrant PI3K/mTOR inhibitor paxalisib and prediction of its pharmacokinetics and efficacy in human

Xenobiotica, 2024-02, Vol.54 (2), p.64-74

2024

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RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy

Cancer discovery, 2022-01, Vol.12 (1), p.204-219

2022

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Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma

Bioorganic & medicinal chemistry letters, 2019-08, Vol.29 (16), p.2294-2301

2019

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Understanding the Effect of Hydroxypropyl‐β‐Cyclodextrin on Fenebrutinib Absorption in an Itraconazole–Fenebrutinib Drug–Drug Interaction Study

Clinical pharmacology and therapeutics, 2020-12, Vol.108 (6), p.1224-1232

2020

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Evaluating the Pharmacokinetics and Systemic Effects of a Permeability Enhancer Sodium N-[8-(2-hydroxybenzoyl)amino] Caprylate in Rats

Journal of pharmaceutical sciences, 2020-08, Vol.109 (8), p.2629-2636

2020

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Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR

ACS medicinal chemistry letters, 2016-04, Vol.7 (4), p.351-356

2016

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Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma

Drug metabolism and disposition, 2016-12, Vol.44 (12), p.1881-1889

2016

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The Design and Identification of Brain Penetrant Inhibitors of Phosphoinositide 3‑Kinase α

Journal of medicinal chemistry, 2012-09, Vol.55 (18), p.8007-8020

2012

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Targeting the PI3K Pathway in the Brain-Efficacy of a PI3K Inhibitor Optimized to Cross the Blood―Brain Barrier

Clinical cancer research, 2012-11, Vol.18 (22), p.6239-6248

2012

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Preclinical assessment of the absorption and disposition of the phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor GDC-0980 and prediction of its pharmacokinetics and efficacy in human

Drug metabolism and disposition, 2012-09, Vol.40 (9), p.1785

2012

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Identification, Characterization, and Implications of Species-Dependent Plasma Protein Binding for the Oral Hedgehog Pathway Inhibitor Vismodegib (GDC-0449)

Journal of medicinal chemistry, 2011-04, Vol.54 (8), p.2592-2601

2011

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Semi-Automated Protein Binding Methodology Using Equilibrium Dialysis and A Novel Mixed-Matrix Cassette Approach

Journal of pharmaceutical sciences, 2010-12, Vol.99 (12), p.5070-5078

2010

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Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941

Drug metabolism and disposition, 2010-09, Vol.38 (9), p.1422

2010

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Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human

Xenobiotica, 2011-12, Vol.41 (12), p.1088-1099

2011

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Expression and activity of the efflux transporters ABCB1, ABCC2 and ABCG2 in the human colorectal carcinoma cell line LS513

European journal of pharmaceutical sciences, 2009-06, Vol.37 (3), p.463-468

2009

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Practical permeability-based hepatic clearance classification system (HepCCS) in drug discovery

Future medicinal chemistry, 2014-01, Vol.6 (18), p.1995-2012

2014

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Preclinical absorption, distribution, metabolism, excretion, and pharmacokinetic-pharmacodynamic modelling of N-(4-(3-((3S,4R)-1-ethyl-3-fluoropiperidine-4-ylamino)-1H-pyrazolo[3,4-b]pyridin-4-yloxy)-3-fluorophenyl)-2-(4-fluorophenyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide, a novel MET kinase inhibitor

Xenobiotica, 2011-04, Vol.41 (4), p.327-339

2011

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Preclinical stereoselective disposition and toxicokinetics of two novel MET inhibitors

Xenobiotica, 2012-05, Vol.42 (5), p.456-465

2012

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Preclinical absorption, distribution, metabolism, excretion, and pharmacokinetic–pharmacodynamic modelling of N -(4-(3-((3S,4R)-1-ethyl-3-fluoropiperidine-4-ylamino)-1 H -pyrazolo[3,4- b ]pyridin-4-yloxy)-3-fluorophenyl)-2-(4-fluorophenyl)-3-oxo-2,3-dihydropyridazine-4-carboxamide, a novel MET kinase inhibitor

Xenobiotica, 2011-04, Vol.41 (4), p.327-339

2011

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Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human

Xenobiotica, 2011-12, Vol.41 (12), p.1088-1099

2011

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Ternary complex dissociation kinetics contribute to mutant-selective EGFR degradation

Cell chemical biology, 2023-02, Vol.30 (2), p.175-187.e15

2023

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Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)

Journal of medicinal chemistry, 2012-05, Vol.55 (9), p.4101-4113

2012

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Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design

Journal of medicinal chemistry, 2016-03, Vol.59 (6), p.2760-2779

2016

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A whole cell assay to measure caspase-6 activity by detecting cleavage of lamin A/C

PloS one, 2012-01, Vol.7 (1), p.e30376

2012

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Targeting the PI3K/Akt/mTOR pathway with the pan-Akt inhibitor GDC-0068 in PIK3CA-mutant breast cancer brain metastases

Preclinical characterization of the absorption and disposition of the brain penetrant PI3K/mTOR inhibitor paxalisib and prediction of its pharmacokinetics and efficacy in human

RTK-Dependent Inducible Degradation of Mutant PI3Kα Drives GDC-0077 (Inavolisib) Efficacy

Design of a brain-penetrant CDK4/6 inhibitor for glioblastoma

Understanding the Effect of Hydroxypropyl‐β‐Cyclodextrin on Fenebrutinib Absorption in an Itraconazole–Fenebrutinib Drug–Drug Interaction Study

Evaluating the Pharmacokinetics and Systemic Effects of a Permeability Enhancer Sodium N-[8-(2-hydroxybenzoyl)amino] Caprylate in Rats

Discovery of Clinical Development Candidate GDC-0084, a Brain Penetrant Inhibitor of PI3K and mTOR

Brain Distribution and Efficacy of the Brain Penetrant PI3K Inhibitor GDC-0084 in Orthotopic Mouse Models of Human Glioblastoma

The Design and Identification of Brain Penetrant Inhibitors of Phosphoinositide 3‑Kinase α

Targeting the PI3K Pathway in the Brain-Efficacy of a PI3K Inhibitor Optimized to Cross the Blood―Brain Barrier

Preclinical assessment of the absorption and disposition of the phosphatidylinositol 3-kinase/mammalian target of rapamycin inhibitor GDC-0980 and prediction of its pharmacokinetics and efficacy in human

Identification, Characterization, and Implications of Species-Dependent Plasma Protein Binding for the Oral Hedgehog Pathway Inhibitor Vismodegib (GDC-0449)

Semi-Automated Protein Binding Methodology Using Equilibrium Dialysis and A Novel Mixed-Matrix Cassette Approach

Role of P-glycoprotein and breast cancer resistance protein-1 in the brain penetration and brain pharmacodynamic activity of the novel phosphatidylinositol 3-kinase inhibitor GDC-0941

Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human

Expression and activity of the efflux transporters ABCB1, ABCC2 and ABCG2 in the human colorectal carcinoma cell line LS513

Practical permeability-based hepatic clearance classification system (HepCCS) in drug discovery

Preclinical stereoselective disposition and toxicokinetics of two novel MET inhibitors

Preclinical pharmacokinetics of the novel PI3K inhibitor GDC-0941 and prediction of its pharmacokinetics and efficacy in human

Ternary complex dissociation kinetics contribute to mutant-selective EGFR degradation

Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152)

Discovery of GluN2A-Selective NMDA Receptor Positive Allosteric Modulators (PAMs): Tuning Deactivation Kinetics via Structure-Based Design

A whole cell assay to measure caspase-6 activity by detecting cleavage of lamin A/C

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