Preclinical in vitro screening assays for drug-like properties

Drug Discovery Today: Technologies

Volumn 2, Issue 2, 2005, Pages 179-185

  Li, Albert P ^a  

^a ADMET Group LLC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIHISTAMINIC AGENT; CYTOCHROME P450; CYTOCHROME P450 INHIBITOR; DRUG METABOLIZING ENZYME; KETOCONAZOLE; MANNITOL; ORAL CONTRACEPTIVE AGENT; RIFAMPICIN; TERFENADINE; XENOBIOTIC AGENT;

ARTICLE; CARDIOTOXICITY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CYTOTOXICITY; DRUG DISPOSITION; DRUG ELIMINATION; DRUG EXCRETION; DRUG METABOLISM; DRUG POTENTIATION; DRUG SCREENING; ENZYME INDUCTION; ENZYME INHIBITION; HEART ARRHYTHMIA; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HUMAN; IN VITRO STUDY; INTESTINE MUCOSA PERMEABILITY; LIVER CELL; LIVER MICROSOME; LIVER TOXICITY; NEPHROTOXICITY; NONHUMAN; PHYSICAL CHEMISTRY; QT PROLONGATION; TOXICITY TESTING;

EID: 21744456214     PISSN: 17406749     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ddtec.2005.05.024     Document Type: Review

References (22)

1. A.P. Li Screening for human ADME/Tox drug properties in drug discovery Drug Discov. Today 6 2001 357-366
2. A.P. Li In vitro approaches to evaluate ADMET drug properties Curr. Top. Med. Chem. 4 2004 701-706
3. C.A. Lipinski Drug-like properties and the causes of poor solubility and permeability J. Pharmacol. Toxicol. Methods 44 2000 235-249
4. D.C. Baumgart and A.U. Dignass Intestinal permeability Gut 35 1 Suppl. 1994 S18-S22
5. A. Avdeef et al. Caco-2 permeability of weakly basic drugs predicted with the double-sink PAMPA pK flux a method Eur. J. Pharm. Sci. 24 2005 333-349
6. I.J. Hidalgo Assessing the absorption of new pharmaceuticals Curr. Top. Med. Chem. 1 2001 385-401
7. Y. Li et al. Increasing the throughput and productivity of Caco-2 cell permeability assays using liquid chromatography-mass spectrometry: application to resveratrol absorption and metabolism Comb. Chem. High Throughput Screen 6 2003 757-767
8. L. Barthe et al. Gastrointestinal absorption of drugs: Methods and studies Fundam. Clin. Pharmacol. 13 1999 154-168
9. Iwao, T. et al. (2004) Absorption and metabolic extraction of diltiazem from the perfused rat small intestine. Drug Metab. Pharmacokinet. 19, 430-437
10. A.P. Li et al. Present status of the application of cryopreserved hepatocytes in the evaluation of xenobiotics: Consensus of an international expert panel Chem. Biol. Interact. 121 1999 117-123
11. L.J. Loretz et al. Optimization of cryopreservation procedures for rat and human hepatocytes Xenobiotica 19 1989 489-498
12. A.P. Li et al. Cryopreserved human hepatocytes: Characterization of drug-metabolizing enzyme activities and applications in higher throughput screening assays for hepatotoxicity, metabolic stability, and drug-drug interaction potential Chem. Biol. Interact. 121 1999 17-35
13. A.P. Li and M. Jurima-Romet Overview: Pharmacokinetic drug-drug interactions Adv. Pharmacol. 43 1997 1-6
14. J. Raucy et al. A cell-based reporter gene assay for determining induction of CYP3A4 in a high-volume system J. Pharmacol. Exp. Ther. 303 2002 412-423
15. G. Lemaire et al. A PXR reporter gene assay in a stable cell culture system: CYP3A4 and CYP2B6 induction by pesticides Biochem. Pharmacol. 68 2004 2347-2358
16. A.P. Li et al. Effects of cytochrome P450 inducers on 17alpha-ethinyloestradiol (EE2) conjugation by primary human hepatocytes Br. J. Clin. Pharmacol. 48 1999 733-742
17. Y. Shitara et al. Inhibition of transporter-mediated hepatic uptake as a mechanism for drug-drug interaction between cerivastatin and cyclosporin A J. Pharmacol. Exp. Ther. 304 2003 610-616
18. Y. Shitara et al. Function of uptake transporters for taurocholate and estradiol 17beta-D-glucuronide in cryopreserved human hepatocytes Drug Metab. Pharmacokinet. 18 2003 33-41
19. W. Kemnitzer et al. Discovery of 4-aryl-4H-chromenes as a new series of apoptosis inducers using a cell- and caspase-based high-throughput screening assay. 1. Structure-activity relationships of the 4-aryl group J. Med. Chem. 47 2004 6299-6310
20. T. Meyer et al. QT-screen: High-throughput cardiac safety pharmacology by extracellular electrophysiology on primary cardiac myocytes Assay Drug Dev. Technol. 2 2004 507-514
21. A.P. Li et al. A novel in vitro system, the integrated discrete multiple organ cell culture (IdMOC) system, for the evaluation of human drug toxicity: Comparative cytotoxicity of tamoxifen towards normal human cells from five major organs and MCF-7 adenocarcinoma breast cancer cells Chem. Biol. Interact. 150 2004 129-136
22. P.P. Annaert and K.L. Brouwer Assessment of drug interactions in hepatobiliary transport using rhodamine 123 in sandwich-cultured rat hepatocytes Drug Metab. Dispos. 33 2005 294-388 (epub 2004 Dec. 17)