The drug efflux-metabolism alliance: Biochemical aspects

Advanced Drug Delivery Reviews

Volumn 50, Issue SUPPL. 1, 2001, Pages

  Benet, Leslie Z ^a,b   Cummins, Carolyn L ^a  

^a UNIVERSITY OF CALIFORNIA   (United States)

^b NONE   (United States)

Author keywords

Cytochrome P450 3A; Drug efflux; Intestine; Metabolism; P glycoprotein

Indexed keywords

ABSORPTION; BIOCHEMISTRY; CELLS; ENZYMES; METABOLISM; PROTEINS;

BIOAVAILABILITY;

DRUG DOSAGE;

ALPHA TOCOPHEROL; BUTYRIC ACID; CLARITHROMYCIN; CYCLOSPORIN A; CYTOCHROME P450 3A; DIGOXIN; ELACRIDAR; FELODIPINE; GLYCOPROTEIN P; IMMUNOSUPPRESSIVE AGENT; INDINAVIR; KETOCONAZOLE; MIDAZOLAM; NELFINAVIR; NIFEDIPINE; PACLITAXEL; PHORBOL 13 ACETATE 12 MYRISTATE; PROTEINASE INHIBITOR; QUINIDINE; RAPAMYCIN; RIFAMPICIN; SAQUINAVIR; TACROLIMUS; TRAMAZOLINE; VINCA ALKALOID; XENOBIOTIC AGENT;

CELL STRAIN CACO 2; CONFERENCE PAPER; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; DRUG METABOLISM; DRUG TRANSPORT; HUMAN; HUMAN CELL; IN VITRO STUDY; INTESTINE; INTESTINE ABSORPTION; KNOCKOUT MOUSE; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN INDUCTION; PROTEIN PROTEIN INTERACTION; PROTEIN SYNTHESIS INHIBITION;

ANIMALS; ARYL HYDROCARBON HYDROXYLASES; BIOLOGICAL AVAILABILITY; CYTOCHROME P-450 CYP3A; CYTOCHROME P-450 ENZYME SYSTEM; HUMANS; IMMUNOSUPPRESSIVE AGENTS; INTESTINAL ABSORPTION; OXIDOREDUCTASES, N-DEMETHYLATING; P-GLYCOPROTEIN; PHARMACEUTICAL PREPARATIONS;

EID: 0035478419     PISSN: 0169409X     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0169-409X(01)00178-8     Document Type: Conference Paper

References (41)

1. Intestinal drug metabolism and anti-transport processes: A potential paradigm shift in oral drug delivery
2. Active secretion and enterocytic drug metabolism barriers to drug absorption
3. Pharmacokinetics: The dynamics of drug absorption, distribution, and elimination
4. Overlapping substrate specificities and tissue distribution of cytochrome P450 3A and P-glycoprotein: Implications for drug delivery and activity in cancer chemotherapy
5. Modulators and substrates of P-glycoprotein and cytochrome P4503A coordinately upregulate these proteins in human colon carcinoma cells
6. Effect of food on the pharmacokinetics of cyclosporine in healthy subjects following oral and intravenous administration
7. Absorption kinetics of cyclosporine in healthy volunteers
8. High fat meals increase the clearance of cyclosporine
9. Transport and metabolism of cyclosporine in isolated rat hepatocytes: The effects of lipids
10. Effects of low-density lipoprotein and ethinyl estradiol on cyclosporine metabolism in isolated rat liver perfusions
11. Bioavailability of cyclosporine with concomitant rifampin administration is markedly less than predicted by hepatic enzyme induction
12. Identification of rifampin-inducible P450IIIA4 (CYP3A4) in human small bowel enterocytes
13. CYP3A gene expression in human gut epithelium
14. Differentiation of absorption and first-pass gut and hepatic metabolism in humans: Studies with cyclosporine
15. The effects of ketoconazole on the intestinal metabolism and bioavailability of cyclosporine
16. Modulation of multidrug resistance gene expression by dexamethasone in cultured hepatoma cells
17. P-glycoprotein: A major determinant of rifampicin-inducible expression of cytochrome P4503A in mice and humans
18. The orphan nuclear receptor SXR coordinately regulates drug metabolism and efflux
19. Tacrolimus oral bioavailability doubles with coadministration of ketoconazole
20. Effects of rifampin on tacrolimus pharmacokinetics in healthy volunteers
21. Sirolimus oral bioavailability increases ten-fold with concomitant ketoconazole
22. Effect of water-soluble vitamin E on cyclosporine pharmacokinetics in healthy volunteers
23. Inhibition of P-glycoprotein by D-α-tocopheryl polyethylene glycol 1000 succinate (TPGS)
24. Role of P-glycoprotein and cytochrome P450 3A in limiting oral absorption of peptides and peptidomimetics
25. Intestinal MDR transport proteins and P-450 enzymes as barriers to oral drug delivery
26. The gut as a barrier to drug absorption
27. Enhanced oral bioavailability of paclitaxel in mice treated with the P-glycoprotein blocker SDZ PSC 833
28. Pharmacokinetic interactions between HIV protease inhibitors in rats
29. Effect of dexamethasone on the intestinal first-pass metabolism of indinavir in rats: Evidence of cytochrome P-4503A and P-glycoprotein induction
30. Effects of ketoconazole on digoxin absorption and disposition in rats
31. Effect of PSC 833, a P-glycoprotein modulator, on the disposition of vincristine and digoxin in rats
32. Effects of ketoconazole on the intestinal metabolism, transport and oral bioavailability of K02, a novel vinylsulfone peptidomimetic cysteine protease inhibitor and a P450 3A, P-glycoprotein dual substrate, in male Sprague-Dawley rats
33. Limited oral bioavailability and active epithelial excretion of paclitaxel (Taxol) caused by P-glycoprotein in the intestine
34. The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors
35. Effect of saquinavir on the pharmacokinetics and pharmacodynamics of oral and intravenous midazolam
36. The contribution of intestinal and hepatic CYP3A to the interaction between midazolam and clarithromycin
37. The role of intestinal P-glycoprotein in the interaction of digoxin and rifampin
38. Intestinal drug absorption and metabolism in cell cultures: Caco-2 and beyond
39. Evidence for different ABC-transporters in caco-2 cells modulating drug uptake
40. Characterizing the expression of CYP3A4 and efflux transporters (P-gp, MRP1, and MRP2) in CYP3A4-transfected caco-2 cells after induction with sodium butyrate and the phorbol ester 12-O-tetradecanoylphorbol-13-acetate
41. 3-modified caco-2 cell monolayers