Prediction of human hepatic clearance using an in vitro plated hepatocyte clearance model. 2009

Piyun Chao, and Jeffrey Barminko, and Eric Novik, and Yi Han, and Timothy Maguire, and K-C Cheng
Hurel Corporation, Beverly Hills, California 91201, USA.

Previously we have used human hepatocytes in suspension by measuring the parent loss for prediction of metabolic clearance according to a 1(st)-order kinetic model. In this study, we evaluated a novel integrative approach using plated human hepatocytes to include both uptake processes and metabolism in a single assay. Test articles were added in the medium, and the intrinsic clearance was determined based on the disappearance of the parent compound from the medium. Three different methods: direct, well-stirred, and parallel tube were tested for scaling purpose. With 30 randomly selected compounds with clinical clearance data, the scaled clearance showed reasonable linear correlation with r(2) values of 0.67, 0.72, and 0.70 for direct, well-stirred and parallel tube models, respectively. When human serum albumin (HSA) was added to the incubation medium a shift to lower in vitro clearance was observed for most of the compounds, suggesting that protein binding may have an effect on the metabolic clearance. In the presence of 4% of HSA, which is equivalent to the albumin concentration in the human plasma, the in vitro clearance data have the best prediction of human clearance when using the well-stirred method, followed by the parallel tube method and direct method. This study demonstrates the utility of using plated human hepatocyte as an integrated system for the prediction of human metabolic clearance. In addition, evaluation of the protein binding shift in the clearance showed that a significant number of compounds may not follow the equilibrium assumption according to the well-stirred model.

UI MeSH Term Description Entries
D008099 Liver A large lobed glandular organ in the abdomen of vertebrates that is responsible for detoxification, metabolism, synthesis and storage of various substances. Livers
D008657 Metabolic Clearance Rate Volume of biological fluid completely cleared of drug metabolites as measured in unit time. Elimination occurs as a result of metabolic processes in the kidney, liver, saliva, sweat, intestine, heart, brain, or other site. Total Body Clearance Rate,Clearance Rate, Metabolic,Clearance Rates, Metabolic,Metabolic Clearance Rates,Rate, Metabolic Clearance,Rates, Metabolic Clearance
D008862 Microsomes, Liver Closed vesicles of fragmented endoplasmic reticulum created when liver cells or tissue are disrupted by homogenization. They may be smooth or rough. Liver Microsomes,Liver Microsome,Microsome, Liver
D008954 Models, Biological Theoretical representations that simulate the behavior or activity of biological processes or diseases. For disease models in living animals, DISEASE MODELS, ANIMAL is available. Biological models include the use of mathematical equations, computers, and other electronic equipment. Biological Model,Biological Models,Model, Biological,Models, Biologic,Biologic Model,Biologic Models,Model, Biologic
D011237 Predictive Value of Tests In screening and diagnostic tests, the probability that a person with a positive test is a true positive (i.e., has the disease), is referred to as the predictive value of a positive test; whereas, the predictive value of a negative test is the probability that the person with a negative test does not have the disease. Predictive value is related to the sensitivity and specificity of the test. Negative Predictive Value,Positive Predictive Value,Predictive Value Of Test,Predictive Values Of Tests,Negative Predictive Values,Positive Predictive Values,Predictive Value, Negative,Predictive Value, Positive
D011485 Protein Binding The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments. Plasma Protein Binding Capacity,Binding, Protein
D002478 Cells, Cultured Cells propagated in vitro in special media conducive to their growth. Cultured cells are used to study developmental, morphologic, metabolic, physiologic, and genetic processes, among others. Cultured Cells,Cell, Cultured,Cultured Cell
D004364 Pharmaceutical Preparations Drugs intended for human or veterinary use, presented in their finished dosage form. Included here are materials used in the preparation and/or formulation of the finished dosage form. Drug,Drugs,Pharmaceutical,Pharmaceutical Preparation,Pharmaceutical Product,Pharmaceutic Preparations,Pharmaceutical Products,Pharmaceuticals,Preparations, Pharmaceutical,Preparation, Pharmaceutical,Preparations, Pharmaceutic,Product, Pharmaceutical,Products, Pharmaceutical
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D012709 Serum Albumin A major protein in the BLOOD. It is important in maintaining the colloidal osmotic pressure and transporting large organic molecules. Plasma Albumin,Albumin, Serum

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