Research Topics
Species | Richard A GrahamSummaryAffiliation: Genentech Inc Country: USA Publications
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Detail Information
Publications
Single and multiple dose intravenous and oral pharmacokinetics of the hedgehog pathway inhibitor vismodegib in healthy female subjectsRichard A Graham
Genentech Inc, 1 DNA Way, South San Francisco, CA 94080, USA
Br J Clin Pharmacol 74:788-96. 2012..While recent publications have suggested the pharmacokinetics (PK) of vismodegib appear to be non-linear, there has not been a report describing the mechanisms of non-linearity...
Pharmacokinetics of hedgehog pathway inhibitor vismodegib (GDC-0449) in patients with locally advanced or metastatic solid tumors: the role of alpha-1-acid glycoprotein bindingRichard A Graham
Genentech Inc, South San Francisco, California 94080, USA
Clin Cancer Res 17:2512-20. 2011..We studied the role of GDC-0449 binding to plasma protein alpha-1-acid glycoprotein (AAG) to better understand these unusual pharmacokinetics...
A single dose mass balance study of the Hedgehog pathway inhibitor vismodegib (GDC-0449) in humans using accelerator mass spectrometryRichard A Graham
Genentech, Inc, South San Francisco, CA 94080, USA
Drug Metab Dispos 39:1460-7. 2011..We conclude that vismodegib and any associated metabolic products are mainly eliminated through feces after oral administration in healthy volunteers...
Determination of unbound vismodegib (GDC-0449) concentration in human plasma using rapid equilibrium dialysis followed by solid phase extraction and high-performance liquid chromatography coupled to mass spectrometryYuzhong Deng
Drug Metabolism and Pharmacokinetics, Genentech, South San Francisco, CA 94080, USA
J Chromatogr B Analyt Technol Biomed Life Sci 879:2119-26. 2011..0% of the nominal concentration values. Extraction recovery of vismodegib was between 77.9 and 84.0%. The assay provides a means for accurate assessment of unbound vismodegib plasma concentrations in clinical studies...
Daily dosing of vismodegib to steady state does not prolong the QTc interval in healthy volunteersRichard A Graham
Genentech, Inc, South San Francisco, CA 94080, USA
J Cardiovasc Pharmacol 61:83-9. 2013..Vismodegib was assessed as being of low risk for QT interval prolongation based on prior nonclinical and clinical experience. A dedicated study was conducted to further assess the potential for vismodegib to prolong the QTc interval...
Identification, characterization, and implications of species-dependent plasma protein binding for the oral Hedgehog pathway inhibitor vismodegib (GDC-0449)Anthony M Giannetti
Genentech Inc, 1 DNA Way, South San Francisco, California 94080, United States
J Med Chem 54:2592-601. 2011..Molecular docking studies reveal the reason for the signficiant species dependence on binding. These data highlight the utility of biophysical techniques in creating a comprehensive picture of protein binding across species...
Engineered thio-trastuzumab-DM1 conjugate with an improved therapeutic index to target human epidermal growth factor receptor 2-positive breast cancerJagath R Junutula
Genentech, Inc, South San Francisco, California 94080, USA
Clin Cancer Res 16:4769-78. 2010..Experimental Design and..
