Rapid assessment of drug metabolism in the drug discovery process

European Journal of Pharmaceutical Sciences

Volumn 11, Issue SUPPL. 2, 2000, Pages

  Bertrand, Marc ^a   Jackson, Peter ^a   Walther, Bernard ^a  

^a INSTITUT DE RECHERCHES INTERNATIONALES SERVIER   (France)

Author keywords

Caco 2; HTS; Metabolism; Modeling; PBPK; Screening

Indexed keywords

DRUG METABOLITE; DRUG METABOLIZING ENZYME;

CELL STRAIN CACO 2; CONFERENCE PAPER; DRUG ABSORPTION; DRUG DEVELOPMENT; DRUG INTERACTION; DRUG METABOLISM; DRUG PENETRATION; DRUG SCREENING; DRUG SOLUBILITY; HUMAN; HUMAN CELL; MODEL; PHARMACOKINETICS; PRIORITY JOURNAL;

ANIMAL; BIOLOGICAL AVAILABILITY; BIOPHARMACEUTICS; CACO-2 CELLS; CYTOCHROME P-450 ENZYME SYSTEM; DRUG DESIGN; DRUG EVALUATION, PRECLINICAL; HUMAN; MICROSOMES; PREDICTIVE VALUE OF TESTS;

EID: 0033800945     PISSN: 09280987     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0928-0987(00)00165-2     Document Type: Conference Paper

References (22)

1. High-throughput measurement of solubility profiles
2. Simultaneous pharmacokinetic screening of a mixture of compounds in the dog Using API LC/MS/MS analysis for increased throughput
3. Development of Caco-2 cells expressing high levels of cDNA-derived cytochrome CYP3A4
4. Microtiter plate assays for inhibition of human, drug-metabolizing cytochromes CYP
5. Effects of ethanol, dexamethasone and RU 486 on expression of cytochromes CYP 2B, 2E, 3A and glutathione transferase in a rat hepatoma cell line (Fao)
6. Photometric microtiter assay of inorganic phosphate in the presence of acid-labile organic phosphates
7. Long-term primary cultures of adult human hepatocytes
8. A small scale shake flask method for determination of intrinsic drug solubility
9. In vitro screening system for oral absorption for poorly water-soluble drugs
10. Effects of administration of the chemoprotective agent oltipraz on CYP1A Z and CYP2B in rat liver and rat hepatocytes in culture
11. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings
12. Development of quantitative structure-pharmacokinetic relationships
13. Physiologically based pharmacokinetic modelling of a homologous series of barbiturates in the rat: a sensitivity analysis
14. A reporter gene assay to assess the molecular mechanisms of xenobiotic-dependent induction of the human CYP3A4 gene in vitro
15. Preclinical drug metabolism in the age of high-throughput screening: an industrial perspective
16. Expression of enzymatically active CYP3A4 by Caco-2 cells grown on extracellular matrix-coated permeable supports in the presence of 1α,25-dihydroxyvitamin D3
17. Comparison of four experimental techniques for studying drug absorption kinetics in the anesthetized rat in situ
18. Interaction of the P-glycoprotein multidrug transporter (MDR1) with high affinity peptide chemosensitizers in isolated membranes, reconstituted systems, and intact cells
19. High throughput liquid chromatography/mass spectrometry bioanalysis using 96-well disk solid phase extraction plate for the sample preparation
20. A systems approach to molecular structure, intermolecular recognition, and emergence-dissolvence in medicinal research
21. Metabolic screening using on-line ultrafiltration mass spectrometry