Current industrial practices of assessing permeability and P-glycoprotein interaction

AAPS Journal

Volumn 8, Issue 1, 2006, Pages

  Balimane, Praveen V ^a   Han, Yong Hae ^a   Chong, Saeho ^a  

^a BRISTOL MYERS SQUIBB   (United States)

Author keywords

Caco 2 cells; Drug discovery; High throughput; P gp; PAMPA; Permeability; Transporters

Indexed keywords

ACEBUTOLOL; ALPRENOLOL; AMILORIDE; CEFALEXIN; CIMETIDINE; DESIPRAMINE; DEXAMETHASONE; ERYTHROMYCIN; ETOPOSIDE; FEXOFENADINE; FUROSEMIDE; GLYCOPROTEIN P; HYDRALAZINE; IBUPROFEN; KETOCONAZOLE; KETOPROFEN; METFORMIN; METOPROLOL; NAPROXEN; NORFLOXACIN; PHENYTOIN; PIROXICAM; PROPRANOLOL; SALAZOSULFAPYRIDINE; SULPIRIDE; TERBUTALINE; TIMOLOL; UNINDEXED DRUG; VERAPAMIL; VINCRISTINE;

ARTIFICIAL MEMBRANE; CELL MEMBRANE PERMEABILITY; CELL STRAIN CACO 2; COST EFFECTIVENESS ANALYSIS; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DISPOSITION; DRUG INDUSTRY; DRUG PENETRATION; DRUG POTENTIATION; DRUG TRANSPORT; HIGH THROUGHPUT SCREENING; HUMAN; IN VITRO STUDY; IN VIVO STUDY; INTESTINE MUCOSA PERMEABILITY; NONHUMAN; PREDICTION; PROTEIN INTERACTION; REVIEW; ANIMAL; ECONOMICS; INTESTINE ABSORPTION; METABOLISM; METHODOLOGY; PHARMACEUTICS; PHYSIOLOGY; TRANSPORT AT THE CELLULAR LEVEL;

ANIMALS; BIOLOGICAL TRANSPORT; CACO-2 CELLS; CELL MEMBRANE PERMEABILITY; DRUG INDUSTRY; HUMANS; INTESTINAL ABSORPTION; P-GLYCOPROTEIN; TECHNOLOGY, PHARMACEUTICAL;

EID: 33646640645     PISSN: 15221059     EISSN: 15221059     Source Type: Journal    
DOI: 10.1208/aapsj080101     Document Type: Review

References (52)

1. Food and Drug Administration. Challenges and Opportunity on the Critical Path to New Medical Products. FDA Report. Rockville, MD: Food and Drug Administration; 2004.
2. Kola I, Landis J. Can pharmaceutical industry reduce attrition rates? Nat Rev Drug Discov. 2004;3:711-715. PubMed DOI: 10.1038/nrd1470
3. Balimane PV, Chong S, Morrison RA. Current methodologies used for evaluation of intestinal permeability and absorption. J Pharmacol Toxicol Methods. 2000;44:301-312. PubMed DOI: 10.1016/ S1056-8719(00)00113-1
4. Hidalgo I. Assessing the absorption of new pharmaceuticals. Curr Top Med Chem. 2001;1:385-401. PubMed DOI: 10.2174/1568026013395010
5. Hillgren K, Kato A, Borchardt R. In vitro systems for studying intestinal drug absorption. Med Res Rev. 1995;15:83-109. PubMed
6. Lipinski C, Lombardo F, Dominy B, Feeney P. Experimental and computational approaches to estimate solubility and permeability in drug discovery and development settings. Adv Drug Deliv Rev. 2001;46:3-26. PubMed DOI: 10.1016/S0169-409X(OO)00129-0
7. Avdeef A. Physicochemical profiling (solubility, permeability and charge state). Curr Top Med Chem. 2001;1:277-351. PubMed DOI: 10.2174/ 1568026013395100
8. Lin J. Drug-drug interaction mediated by inhibition and induction of P-glycoprotein. Adv Drug Deliv Rev. 2003;55:53-81. PubMed DOI: 10.1016/ S0169-409X(02)00171-0
9. Polli J, Jerrett J, Studenberg J, et al. Role of P-gp on CNS disposition of amprenavir, an HIV protease inhibitor. Pharm Res. 1999;16:1206-1212. PubMed DOI: 10.1023/A:1018941328702
10. Kim R, Wendel C, Leake B, et al. Interrelationship between substrates and inhibitors of human CYP3A and P-gp. Pharm Res. 1999;16:408-414. PubMed DOI: 10.1023/A:1018877803319
11. Lin J, Yamazaki M. Role of P-glycoprotein in pharmacokinetics. Clin Pharmacokinet. 2004;42:59-98. PubMed
12. Simpson K, Jarvis B. Fexofenadine: a review of its use in the managemept of seasonal allergic rhinitis and chronic idiopathic urticaria. Drugs. 2000;59:301-321. PubMed
13. Watanabe T. Miyauchi S, Sawada Y, et al. Kinetic analysis of hepatobiliary transport of vincristine in perfused rat liver: possible roles of P-gp in biliary excretion of vincristine. J Hepatol. 1992;16:77-88. PubMed DOI: 10.1016/S0168-8278(05)80098-4
14. Adachi Y, Suzuki H, Sugiyama Y. Comparative studies on in vitro methods for evaluating in vivo function of MDR1 P-gp. Pharm Res. 2001;18:1660-1668. PubMed DOI: 10.1023/A:1013358126640
15. Perloff M, Stromer E, von Moltke L, Greenblatt D. Rapid assessment of P-gp inhibition and induction in vitro. Pharm Res. 2003;20:1177-1183. PubMed DOI: 10.1023/A:1025092829696
16. Polli J, Wring S, Humphreys J, et al. Rational use of in vitro P-gp assays in drug discovery. J Pharmacol Exp Ther. 2001:299:620-628. PubMed
17. Yamazaki M, Neway W, Ohe T, et al. In vitro substrate identification studies for P-gp mediated transport: species difference and predictability of in vivo results. J Pharmacol Exp Ther. 2001;296:723-735. PubMed
18. Kansy M, Senner F, Gubernator K. Physicochemical high throughput screening: parallel artificial membrane permeation assay in the description of passive absorption processes. J Med Chem. 1998;41:1007-1010. PubMed DOI: 10.1021/jm970530e
19. Kerns E. High throughput physicochemical profiling for drug discovery. J Pharm Sci. 2001;90:1838-1858. PubMed DOI: 10.1002/jps.1134
20. Ruell JA. Tsinman KL, Avdeef A. PAMPA - a drug absorption in vitro model. 5. Unstirred water layer in iso-pH mapping assays and pKa(flux) - optimized design (pOD-PAMPA). Eur J Pharm Sci. 2003;20:393-402. PubMed DOI: 10.1016/j.ejps.2003.08.006
21. Di L, Kerns EH, Fan K, McConnell OJ, Carter GT. High throughput artificial membrane permeability assay for blood-brain barrier. Eur J Med Chem. 2003;38:223-232. PubMed DOI: 10.1016/S0223-5234(03)00012-6
22. Artursson P. Cell cultures as models for drug absorption across the intestinal mucosa. Crit Rev Ther Drug Carrier Syst. 1991;8:305-330. PubMed
23. Artursson P, Karlsson J. Correlation between oral drug absorption in humans and apparent drug permeability coefficients in human intestinal epithelia (Caco-2) cells. Biochem Biophys Res Commun. 1991;175:880-890. PubMed DOI: 10.1016/0006-291X(91)91647-U
24. Rubas W, Cromwell M, Shahrokh Z, et al. Flux measurements across Caco-2 monolayers may predict transport in human large intestinal tissue. J Pharm Sci. 1996;85:165-169. PubMed DOI: 10.1021/js950267+
25. Aungst B, Nguyen N, Bulgarelli J, Oates-Lenz K. The influence of donor and reservoir additives on Caco-2 permeability and secretory transport of HIV protease inhibitors and other lipophilic compounds. Pharm Res. 2000;17:1175-1180 PubMed DOI: 10.10231/A:1026402410783
26. Balimane PV, Chong S. A combined cell based approach to identify P-glycoprotein substrates and inhibitors in a single assay. Int J Pharm. 2005;301:80-88. PubMed DOI: 10.1016/j.ijpharm.2005.05.034
27. Braun A, Hammerle S, Suda K, Rothen-Rutishauser B, Gunthert M, Wunderli-Allenspach H. Cell cultures as tools in biopharmacy. Eur J Pharm Sci. 2000;11:S51-S60. PubMed DOI: 10.1016/S0928-0987(00)00164-0
28. Horie K, Tang F, Borchardt R, Isolation and characterization of Caco-2 subclones expressing high levels of multidrug resistance efflux transporter. Pharm, Res. 2003-20:161-168. PubMed DOI: 10.1023/ A:1022359300826
29. Ungell AL. Caco-2 replace or refine? Drug Discov Today Technol. 2004;1:423-430. DOI: 10.1016/j.ddtec.2004.11.003
30. Balimane PV, Chong S. Cell culture-based models for intestinal permeability: a critique. Drug Discov Today. 2005; 10:335-343 PubMed DOI: 10.1016/S1359-6446(04)03354-9
31. Chong S, Dando S, Soucek K, Morrison R. In vitro permeability through Caco-2 cells is not quantitatively predictive of in vivo absorption for peptide-like drugs absorbed via the dipeptide transporter system, Pharm Res. 1996;13:120-123. PubMed DOI: 10.1023/A:1016045820933
32. Ano R, Kimura Y, Shima M, Matsuno R, Ueno T, Akamatsu M. Relationship between structure and high-throughput screening permeability of papetide derivatives and related compounds with artificial membranes: application to prediction of Caco-2 cell permeability. Bioorg Med Chem. 2004; 12:257-264. PubMed DOI: 10.1016/j.bmc.2003.10.002
33. Kerns E, Di L, Petusky S, Farris M, Ley R, Jupp P. Combined application of parallel artificial membrane permeability assay and Caco-2 permeability assays in drug discovery. J Pharm Sci. 2004;93:1440-1453. PubMed DOI: 1O.1002,/jps.20075
34. Dressman J, Berardi R, Dermentzoglou L, et al. Upper gastrointestinal (GI) pH in young, healthy men and women. Pharm Res. 1990;7:756-761. PubMed DOI: 10.1023/A:1015827908309
35. Russell T, Berardi R, Barnett J,.et al. Upper gastrointestinal pH in 79 healthy, elderly, North American men and women. Pharm Res. 1993;10:187-196. PubMed DOI: 10.1023/A:1018970323716
36. Anderle P, Huang Y, Sadee W. Intestinal membrane transport of drugs and nutrients: genomic membrane transporters using expression microarray, Eur J Pharm Sci. 2004;21:17-24. PubMed DOI: 10.1016/S0928-0987(03)00169-6
37. Behrens I, Kamm W, Dantzig A, Kissel T. Variation of peptide transporter (PepT1 and HPT1) expression in Caco-2 cells as a function of cell origin. J Pharm Sci. 2004;93:1743-1754. PubMed DOI: 10.1002/jps.20062
38. Sun D, Lennernas H, Welage L, et al. Comparison of human duodenum and Caco-2 gene expression profiles for 12 000 gene sequence tags and correlation with permeability of 26 drugs. Pharm Res. 2002; 19:1400-1416. PubMed DOI: 10.1023/A:1020483911355
39. Krishna G, Chen K, Lin C, Nomeir A. Permeability of lipophilic compounds in drug discovery using in vitro human absorption model, Caco-2. Int J Pharm. 2001;222:77-89. PubMed DOI: 10.1016/S0378-5173(01)00698-6
40. Saha P, Kou J. Effect of bovine serum albumin on drug permeability estimation across Caco-2 monolayers. Eur J Pharm Biopharm. 2002;54.319-324. PubMed DOI: 10.1016/S0939-6411(02)00089-9
41. Dimitrijevic D, Shaw A, Florence A. Effects of some non-ionic surfactants on transepithelial permeability in Caco-2 cells. J Pharm Pharmacol 2000;52:157-162. PubMed DOI: 10.1211/0022357001773805
42. Rege B, Yu L. Hussain A. Polli J. Effect of common excipients on Caco-2 transport of low-permeability drugs. J Pharm Sci. 2001:90:1776-1786. PubMed DOI: 1O.1002/jps.1127
43. Rege B, Kao J. Polli J. Effect of non-ionic-surfactants on membrane transport in Caco-2 cell monolayers. Eur J Pharm Sci. 2002;16:237-246 PubMed DOI: 10.1016/S0928-0987(02)00055-6
44. Ingels F, Augustijns P. Biological, pharmaceutical, and analytical considerations with respect to the transport media used in the absorption screening system, Caco-2. J Pharm Sci. 2003;92:1545-1558. PubMed DOI: 10.1002/jps.10408
45. Walter E, Kissel T, Heterogeneity in the human intestinal cell line Caco-2 leads to differences in transepithelial transport. Eur J Pharm Sci. 1995;3:215-230. DOI: 10.1016/0928-0987(95)00010-B
46. Maliepaard M, van Gastelen M, Tohgo A, et al. Circumvention of BCRP-mediated resistance to camptothecins in vitro using non-substrate drugs or the BCRP inhibitor GF120918. Clin Cancer Res. 2001;7:935-941. PubMed
47. Woehlecke H, Pohl A, Alder-Berens N, Lage H, Herrmann A. Enhanced exposure of phosphatidylserine in human gastric carcinoma cells overexpressing the half-size ABC transporter BCRP (ABCG2). Biochem J 2003;376:489-49. PubMed DOI: 10.1042/BJ20030886
48. Chen Z, Kawabe T, Ono M, et al. Effect of multidrug resistance-reversing agents on transporting activity of human canalicular multispecific organic anion transporter. Mol Pharmacol. 1999;56:1219-1228 PubMed
49. Dantzig A, Shepard R, Law K, et al. Selectivity of the multidrug resistance modulator, LY335979, for P-glycoprotein and effect on cytochrome P-450 activities. J Pharmacol Exp Ther. 1999;290:854-862. PubMed
50. Volk E, Schneider E. Wild type BCRP is a methotrexate polyglutamate transporter. Cancer Res. 2003;63:5538-5543 PubMed
51. Zhang S, Yang X, Morris M. Flavonoids are inhibitors of BCRP-mediated transport.Mol Pharmacol 2004;65:1208-1216. PubMed DOI: 10.1124/ mol.65.5.1208
52. Lee K, Ng C, Brouwer KL, Thakker DR, Secretory transport of ranitidine and famotidine across Caco-2 cell monolayers. J Pharmacol Exp Ther, 2002;303;574-580. PubMed DOI: 10.1124/jpet.102.038521