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Interplay of Dissolution, Solubility, and Nonsink Permeation Determines the Oral Absorption of the Hedgehog Pathway Inhibitor GDC-0449 in Dogs: An Investigation Using Preclinical Studies and Physiologically Based Pharmacokinetic Modeling

Harvey Wong, Xiling Song, Cornelis E C A Hop, 2010, Drug Metabolism and Disposition.

Design of Selective PAK1 Inhibitor G-5555: Improving Properties by Employing an Unorthodox Low-pK a Polar Moiety.

Xianrui Zhao, Ignacio Aliagas, Ronen Marmorstein, 2015, ACS medicinal chemistry letters.

Significant Species Difference in Amide Hydrolysis of GDC-0834, a Novel Potent and Selective Bruton's Tyrosine Kinase Inhibitor

John C. Davis, P. Kuebler, J. Lubach, 2011, Drug Metabolism and Disposition.

Implementation of the CYP Index for the Design of Selective Tryptophan-2,3-dioxygenase Inhibitors.

Benjamin D. Sellers, Rohan V Mendonca, Sanjeev Kumar, 2020, ACS medicinal chemistry letters.

Novel nanoparticles formulation for cassette dosing via intravenous injection in rats for high throughput pharmacokinetic screening and potential applications.

Y. Ran, H. Wong, K. Chou, 2012, Journal of nanoscience and nanotechnology.

A reversed sulfonamide series of selective RORc inverse agonists.

Bohdan Waszkowycz, Emanuela Gancia, Peter Lockey, 2014, Bioorganic & medicinal chemistry letters.

Pyridones as Highly Selective, Noncovalent Inhibitors of T790M Double Mutants of EGFR.

C. Eigenbrot, Ivana Yen, S. Sideris, 2016, ACS medicinal chemistry letters.

DMD053926 2104..2113

A. Tolcher, W. Fairbrother, E. Kadel, 2013 .

In Vitro and In Vivo Evaluation of Amorphous Solid Dispersions Generated by Different Bench-Scale Processes, Using Griseofulvin as a Model Compound

Y. Ran, J. Lubach, H. Wong, 2013, The AAPS Journal.

Discovery of a potent small-molecule antagonist of inhibitor of apoptosis (IAP) proteins and clinical candidate for the treatment of cancer (GDC-0152).

Zhaoyang Wen, Brigitte Maurer, Vickie Tsui, 2012, Journal of medicinal chemistry.

Discovery of 1-{4-[3-fluoro-4-((3s,6r)-3-methyl-1,1-dioxo-6-phenyl-[1,2]thiazinan-2-ylmethyl)-phenyl]-piperazin-1-yl}-ethanone (GNE-3500): a potent, selective, and orally bioavailable retinoic acid receptor-related orphan receptor C (RORc or RORγ) inverse agonist.

Adam R. Johnson, P. Lockey, W. Ouyang, 2015, Journal of medicinal chemistry.

4-Aminoindazolyl-dihydrofuro[3,4-d]pyrimidines as non-covalent inhibitors of mutant epidermal growth factor receptor tyrosine kinase.

C. Eigenbrot, Ivana Yen, S. Sideris, 2016, Bioorganic & medicinal chemistry letters.

Discovery of oxa-sultams as RORc inverse agonists showing reduced lipophilicity, improved selectivity and favorable ADME properties.

Adam R. Johnson, A. Barnard, H. Wong, 2016, Bioorganic & medicinal chemistry letters.

Cyclodextrin Reduces Intravenous Toxicity of a Model Compound.

A. Narang, W. Fairbrother, H. Wong, 2019, Journal of pharmaceutical sciences.

Pharmacokinetic–Pharmacodynamic Analysis of Vismodegib in Preclinical Models of Mutational and Ligand-Dependent Hedgehog Pathway Activation

T. Januario, F. D. de Sauvage, R. Yauch, 2011, Clinical Cancer Research.

Chemically Diverse Group I p21-Activated Kinase (PAK) Inhibitors Impart Acute Cardiovascular Toxicity with a Narrow Therapeutic Window.

I. Aliagas, K. Hoeflich, Weiru Wang, 2016, Journal of medicinal chemistry.

Pharmacological Induction of RAS-GTP Confers RAF Inhibitor Sensitivity in KRAS Mutant Tumors.

Dhara N. Amin, R. Neve, Ivana Yen, 2018, Cancer cell.

Discovery of a Noncovalent, Mutant-Selective Epidermal Growth Factor Receptor Inhibitor.

Siew K. Yeap, C. Eigenbrot, Ivana Yen, 2016, Journal of medicinal chemistry.

Noncovalent Mutant Selective Epidermal Growth Factor Receptor Inhibitors: A Lead Optimization Case Study.

Belen Dominguez-Fernandez, C. Eigenbrot, Ivana Yen, 2015, Journal of medicinal chemistry.

Discovery of Selective and Noncovalent Diaminopyrimidine-Based Inhibitors of Epidermal Growth Factor Receptor Containing the T790M Resistance Mutation

Siew K. Yeap, C. Eigenbrot, Ivana Yen, 2014, Journal of medicinal chemistry.

Noncovalent wild-type-sparing inhibitors of EGFR T790M.

J. Settleman, K. Politi, S. Sideris, 2013, Cancer discovery.

Antitumor Activity of Targeted and Cytotoxic Agents in Murine Subcutaneous Tumor Models Correlates with Clinical Response

Harvey Wong, Cornelis E C A Hop, F. Theil, 2012, Clinical Cancer Research.

Leveraging the Pre-DFG Residue Thr-406 To Obtain High Kinase Selectivity in an Aminopyrazole-Type PAK1 Inhibitor Series.

F. Diederich, G. Manning, I. Aliagas, 2015, ACS medicinal chemistry letters.

Microsoft Word-54693261-file00

F. Theil, H. Wong, C. Hop, 2010 .

GDC-0449-a potent inhibitor of the hedgehog pathway.

K. Kotkow, L. Rubin, D. Sutherlin, 2009, Bioorganic & medicinal chemistry letters.

Preclinical assessment of the absorption, distribution, metabolism and excretion of GDC-0449 (2-chloro-N-(4-chloro-3-(pyridin-2-yl)phenyl)-4-(methylsulfonyl)benzamide), an orally bioavailable systemic Hedgehog signalling pathway inhibitor

H. Wong, E. Plise, Y. Shin, 2009, Xenobiotica; the fate of foreign compounds in biological systems.

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a 5-Fluoro-4-(3H)-quinazolinone Aryl Urea pan-RAF Kinase Inhibitor.

C. Eigenbrot, Ivana Yen, S. Malek, 2021, Journal of medicinal chemistry.

Stereoselective supercritical fluidic chromatography –mass spectrometry (SFC-MS) as a fast bioanalytical tool to assess chiral inversion in vivo and in vitro

Yuan Chen, Liuxi Chen, B. Dean, 2019, International Journal of Mass Spectrometry.

Tetrahydrofuran-Based Transient Receptor Potential Ankyrin 1 (TRPA1) Antagonists: Ligand-Based Discovery, Activity in a Rodent Asthma Model, and Mechanism-of-Action via Cryogenic Electron Microscopy.

M. Volgraf, A. Rohou, Jun Chen, 2021, Journal of medicinal chemistry.

SAHA Enhances Synaptic Function and Plasticity In Vitro but Has Limited Brain Availability In Vivo and Does Not Impact Cognition

Kimberly Scearce-Levie, Dani Brunner, Qiang Zhou, 2013, PloS one.

Rate-Determining and Rate-Limiting Steps in the Clearance and Excretion of a Potent and Selective p21-Activated Kinase Inhibitor: A Case Study of Rapid Hepatic Uptake and Slow Elimination in Rat

J. Rudolph, Ning Liu, M. Durk, 2016, Drug metabolism letters.

Systemic concentrations can limit the oral absorption of poorly soluble drugs: an investigation of non-sink permeation using physiologically based pharmacokinetic modeling.

Po-Chang Chiang, Harvey Wong, H. Wong, 2013, Molecular pharmaceutics.

Quantifying KRAS G12C Covalent Drug Inhibitor Activity in Mouse Tumors Using Mass Spectrometry.

W. Forrest, M. Merchant, Yichin Liu, 2023, Analytical chemistry.

Discovery of imidazo[1,5-a]pyridines and -pyrimidines as potent and selective RORc inverse agonists.

Adam R. Johnson, W. Ouyang, A. Barnard, 2015, Bioorganic & medicinal chemistry letters.

Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors.

I. Aliagas, K. Hoeflich, Weiru Wang, 2015, Journal of medicinal chemistry.

In Vitro and In Vivo Evaluation of Amorphous Solid Dispersions Generated by Different Bench-Scale Processes, Using Griseofulvin as a Model Compound

Y. Ran, J. Lubach, H. Wong, 2013, The AAPS Journal.

Learning and Confirming with Preclinical Studies: Modeling and Simulation in the Discovery of GDC-0917, an Inhibitor of Apoptosis Proteins Antagonist

A. Tolcher, W. Fairbrother, E. Kadel, 2013, Drug Metabolism and Disposition.

Identification of N-sulfonyl-tetrahydroquinolines as RORc inverse agonists.

Adam R. Johnson, P. Savy, P. Lockey, 2015, Bioorganic & medicinal chemistry letters.

Reduction in lipophilicity improved the solubility, plasma-protein binding, and permeability of tertiary sulfonamide RORc inverse agonists.

Adam R. Johnson, P. Lockey, W. Ouyang, 2014, Bioorganic & medicinal chemistry letters.

Corrigendum to “GDC-0449—A potent inhibitor of the hedgehog pathway” [Bioorg. Med. Chem. Lett. 19 (2009) 5576]

K. Kotkow, L. Rubin, D. Sutherlin, 2010 .

Abstract A11: Antitumor activity of targeted and cytotoxic agents in xenograft models correlates with clinical response: A pharmacokinetic-pharmacodynamic analysis.

L. Friedman, H. Wong, E. Choo, 2011 .

Targeting KRAS Mutant Cancers via Combination Treatment: Discovery of a Pyridopyridazinone pan-RAF Kinase Inhibitor.

C. Eigenbrot, Ivana Yen, S. Malek, 2021, ACS medicinal chemistry letters.

Structure-Guided Design of Group I Selective p21-Activated Kinase Inhibitors.

I. Aliagas, K. Hoeflich, Weiru Wang, 2015, Journal of medicinal chemistry.

Pharmacokinetic–Pharmacodynamic Analysis of Vismodegib in Preclinical Models of Mutational and Ligand-Dependent Hedgehog Pathway Activation

T. Januario, F. D. de Sauvage, R. Yauch, 2011, Clinical Cancer Research.