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

(S)-1-{4-[2-(2-Amino-pyrimidin-5-yl)-7-methyl-4-morpholin-4-yl-thieno[3,2-d]pyrimidin-6-ylmethyl]-piperazin-1-yl}-2-hydroxy-propan-1-one (GDC-0980) is a potent and selective inhibitor of phosphatidylinositol 3-kinase (PI3K) and mammalian target of rapamycin, two key components of the PI3K pathway, t...

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Veröffentlicht in:	Drug metabolism and disposition 2012-09, Vol.40 (9), p.1785-1796
Hauptverfasser:	Salphati, Laurent, Pang, Jodie, Plise, Emile G., Lee, Leslie B., Olivero, Alan G., Prior, Wei Wei, Sampath, Deepak, Wong, Susan, Zhang, Xiaolin
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Animals Antineoplastic Agents - administration & dosage Antineoplastic Agents - blood Antineoplastic Agents - pharmacokinetics Area Under Curve ATP Binding Cassette Transporter, Subfamily B - deficiency ATP Binding Cassette Transporter, Subfamily B - genetics ATP Binding Cassette Transporter, Subfamily B - metabolism ATP Binding Cassette Transporter, Subfamily G, Member 2 ATP-Binding Cassette Sub-Family B Member 4 ATP-Binding Cassette Transporters - deficiency ATP-Binding Cassette Transporters - genetics Biological Availability Biotransformation Brain - metabolism Breast Neoplasms - drug therapy Breast Neoplasms - enzymology Breast Neoplasms - genetics Breast Neoplasms - pathology Bridged Bicyclo Compounds, Heterocyclic - administration & dosage Bridged Bicyclo Compounds, Heterocyclic - blood Bridged Bicyclo Compounds, Heterocyclic - pharmacokinetics Cell Membrane Permeability Dogs Drug Dosage Calculations Female Half-Life Hepatocytes - metabolism Humans Injections, Intravenous Intestinal Absorption Liver - metabolism Macaca fascicularis Madin Darby Canine Kidney Cells Male MCF-7 Cells Metabolic Clearance Rate Mice Mice, Knockout Models, Biological Phosphatidylinositol 3-Kinase - metabolism Phosphoinositide-3 Kinase Inhibitors Protein Binding Protein Kinase Inhibitors - administration & dosage Protein Kinase Inhibitors - blood Protein Kinase Inhibitors - pharmacokinetics Pyrimidines - administration & dosage Pyrimidines - blood Pyrimidines - pharmacokinetics Rats Rats, Sprague-Dawley Receptor, ErbB-2 - genetics Receptor, ErbB-2 - metabolism Species Specificity Tissue Distribution TOR Serine-Threonine Kinases - antagonists & inhibitors TOR Serine-Threonine Kinases - metabolism Transfection Xenograft Model Antitumor Assays
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